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Quercetin Enhances 5-fluorouracil Sensitivity by Regulating the Autophagic Flux and Inducing Drp-1 Mediated Mitochondrial Fragmentation in Colorectal Cancer Cells Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-03-15 Mei Li, Jiaoxiu Fan, Min Hu, Junyu Xu, Ziyue He, Jun Zeng
Background:: While chemotherapy treatment demonstrates its initial effectiveness in eliminating the majority of the tumor cell population, nevertheless, most patients relapse and eventually succumb to the disease upon its recurrence. One promising approach is to explore novel, effective chemotherapeutic adjuvants to enhance the sensitivity of cancer cells to conventional chemotherapeutic agents. In
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siRNA Targeting ECE-1 Partially Reverses Pulmonary Arterial Hypertensionassociated Damage in a Monocrotaline Model Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-03-11 Citlali Margarita Blancas-Napoles, Sandra Edith Cabrera-Becerra, Vivany Maydel Sierra-Sánchez, Sergio Adrian Ocampo-Ortega, Vanessa Giselle Garcia-Rubio, Rodrigo Romero-Nava, Fengyang Huang, Enrique Hong, Asdrúbal Aguilera-Méndez, Santiago Villafaña
Aims:: The aim of this study was to develop a possible treatment for pulmonary arterial hypertension. Background:: Pulmonary arterial hypertension (PAH) is a rare disease characterised by a pulmonary arterial pressure greater than 20 mmHg. One of the factors that contribute to PAH is an increase in the production of endothelin-1, a polypeptide that increases vascular resistance in the pulmonary arteries
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RNA Interference-based Therapies for the Reduction of Cardiovascular Risk Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-03-05 Natalia Nazarenko, Jiyoung Seo, Sanjana Nagraj, Leonidas Palaiodimos, Damianos G. Kokkinidis
:: Globally, there remains an unwavering increase in the incidence of cvd - from 271 million in 1990 to 523 million in 2019. Among the several modifiable and non-modifiable risk factors of heart disease, dyslipidemia is an important and prevalent risk factor mediated by both genetics and lifestyle factors. Hence, lowering lipid levels, specifically, ldl-c levels (low-density lipoprotein cholesterol)
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A Promising Breakthrough: The Potential of VORASIDENIB in the Treatment of Low-grade Glioma Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-03-01 Alice Bombino, Marcello Magnani, Alfredo Conti
Introduction:: Gliomas are common malignant brain tumors characterized by diffuse brain infiltration. World Health Organization grade II and grade III diffuse gliomas are considered lower-grade gliomas (LGGs) and have isocitrate dehydrogenase (IDH) mutations. LGGs are challenging due to their infiltrative nature, making them capable of progressing into higher-grade malignancies. Vorasidenib is a novel
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Ginsenoside Compound K Reduces Psoriasis-related Inflammation by Activation of the Glucocorticoid Receptor in Keratinocytes Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-02-22 Wu Wang, Xiujin Xu, Mei Yang, Mengya Jiang, Dandan Wang, Caihong Tang, Wei Wei, Jingyu Chen
Aim: To investigate the effects and mechanism of Ginsenoside Compound K (GCK) on psoriasis, focusing on the glucocorticoid receptor (GR) in keratinocytes. Methods: An imiquimod (IMQ)-induced psoriasis-like dermatitis mouse model was generated to evaluate the anti-inflammatory effect of GCK. Hematoxylin and eosin (H&E) staining was used to assess skin pathological changes. Protein expression of K17
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IMPDH2 Positively Impacts the Proliferation Potential of Hepatoblastoma Cells by Activating JunB Signaling Pathway Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-02-22 Li Yuan, Liang Zeng, Feng Ye, Kai Chen, Zhengrong Chen, Liping Li
Background: Amplification of inosine monophosphate dehydrogenase II, EC 1,1,1,205 (IMPDH2) has been reported in various cancers, which results in transformation and tumorigenicity. In our current work, we have explored the oncogenic properties and the underlying pathophysiology of IMPDH2 in hepatoblastoma (HB). Methods: To investigate IMPDH2 expression in HB tissues and prognostic significance in HB
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Impact of Nicosulfuron on Sperm Quality: Insights into Testicular Cell Apoptosis and NF-κB Signaling Pathway in Mice Testes Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-02-07 Jianqiu Han, Chen Zhao, Qing Shen, Yalei Qi, Yanjia Zhang, Faisal Raza, Yongmei Li, Hajra Zafar, Tengfei Liu, Juan Tan, Honghui Han, Xueyun Ma
Background:: Nicosulfuron, a widely used herbicide in crops, has raised concerns due to its escalating presence as an environmental pollutant, particularly in soil and water. The potential adverse effects of nicosulfuron on animals, including reproductive toxicity, have garnered attention. Objective:: The study aimed to evaluate the reproductive toxicity of nicosulfuron in male mice. Methods:: Male
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Nrf2 Mediates Effect of Resveratrol in Ischemia-reperfusion Injury Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-02-07 Ali Mohammad Pourbagher-Shahri, Tahereh Farkhondeh, Amir Masoud Jafari-Nozad, Majid Darroudi, Kobra Naseri, Masoumeh Amirian, Saeed Samarghandian
:: Ischemia-Reperfusion Injury (IRI) is a paradoxical phenomenon where removing the source of injury can cause additional damage. Ischemia reduces ATP production and intracellular pH, reducing oxidative reactions, increasing lactic acid release, and activating anaerobic metabolism. Reperfusion restores aerobic respiration and increases ROS production, leading to malfunction of transmembrane transport
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Sanguinarine Attenuates Lung Cancer Progression via Oxidative Stress-induced Cell Apoptosis Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-02-07 Asmat Ullah, Anum Razzaq, Mohammad Y. Alfaifi, Serag Eldin I. Elbehairi, Farid Menaa, Najeeb Ullah, Somia Shehzadi, Touseef Nawaz, Haroon Iqbal
Background:: Lung cancer (LC) incidence is rising globally and is reflected as a leading cause of cancer-associated deaths. Lung cancer leads to multistage carcinogenesis with gradually increasing genetic and epigenetic changes. Aims:: Sanguinarine (sang) mediated the anticancer effect in LCC lines by involving the stimulation of reactive oxygen species (ROS), impeding Bcl2, and enhancing Bax and other
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Advancements in the Research of GEF-H1: Biological Functions and Tumor Associations Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-02-07 Liqi Li, Yunyun Li, Xiaoshu Zhou
:: Guanine nucleotide exchange factor H1 (GEF-H1) is a unique protein modulated by the GDP/GTP exchange. As a regulator of the Rho-GTPase family, GEF-H1 can be activated through a microtubule-depended mechanism and phosphorylation regulation, enabling it to perform various pivotal biological functions across multiple cellular activities. These include the regulation of Rho-GTPase, cytoskeleton formation
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Curcumin and Berberine Arrest Maturation and Activation of Dendritic Cells Derived from Lupus Erythematosus Patients Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-29 Amin Reza Nikpoor, Mahmoud Mahmoudi, Abbas Shapouri-Moghaddam, Zahra Rezaieyazdi, Samaneh Mollazadeh, Nafiseh Tabasi, Atena Mansouri, Reyhane modarres Moghadam, Amir Abbas Momtazi, Soran K Najmaldin, Ramiar Kamal Kheder, Seyed-Alireza Esmaeili
Background:: Systemic lupus erythematosus (SLE) is a complex autoimmune disease recognized by elevated activity of autoimmune cells, loss of tolerance, and decreased regulatory T cells producing inhibitory cytokines. Despite many efforts, the definitive treatment for lupus has not been fully understood. Curcumin (CUR) and berberine (BBR) have significant immunomodulatory roles and anti-inflammatory
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Alnustone: A review of its sources, pharmacology, and pharmacokinetics Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-29 Zahra Salari, Maryam Alavi, Hojjat Rezaii-zadeh, Abdelhakim Bouyahya, Ammar Alfergah, Sahar Afsari Sardari, Ehsan Amiri-Ardekani
: Alnustone (4(E)-,6(E)-1,7-Diphenyl-hepta-4,6-dien-3-one) is a non-phenolic natural diarylheptanoid, which was first isolated and identified from the male flower of Alnus pendula (Betulaceae). It can also be isolated from Curcuma xanthorrhiza Roxb (Zingiberaceae) rhizomes and Alpinia katsumadai Hayata (Zingiberaceae) seeds. It was first synthesized through a five-step process from β-phenyl propionyl
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A Review of the Dual Role of MicroRNA-21 in Cardiovascular Diseases: Risk Factor or a Potential Therapeutic Target Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-29 Amir Masoud Jafari-Nozad, Negin Rostami, Melika Esmaeili, Haniye Vahdati, Serajoddin Hosseini, Tahereh Farkhondeh, Saeed Samarghandian
: Cardiovascular diseases [CVD] are the number one reason for morbidity and mortality in the modern world, and their incidence is increasing at an incredible pace. Increasing evidence has shown the significant functions of microRNAs in the cardiovascular system and has highlighted their potential application as a new era of diagnostic and therapeutic targets for CVD that can improve the prognosis and
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Anticancer Properties of Baicalin against Breast Cancer and other Gynecological Cancers: Therapeutic Opportunities based on Underlying Mechanisms Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-29 Mohammad Hossein Pourhanifeh, Hossein Farrokhi-Kebria, Parsa Mostanadi, Tahereh Farkhondeh, Saeed Samarghandian
: Gynecological cancers are serious life-threatening diseases responsible for high morbidity and mortality around the world. Chemotherapy, radiotherapy, and surgery are considered standard therapeutic modalities for these cancers. Since the mentioned treatments have undesirable side effects and are not effective enough, further attempts are required to explore potent complementary and/or alternative
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Depression-like Behavior Induced by Repeated Administration of Dexamethasone to Lipopolysaccharide-inflamed Mice Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-29 Fumiya Shibagaki, Naoko Kojima, Akane Furukawa, Noritaka Nakamichi
Background:: Over the years, animal models of depression have been developed by loading chronic stress, inducing neuroinflammation, or administering drugs that induce depression; however, these results have poor reproducibility. Therefore, it is necessary to develop animal models that exhibit definitive symptoms of depression for studies on potential therapeutics. Objective:: This study was aimed at
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Molecular Insight into the Apoptotic Mechanism of Cancer Cells: An Explicative Review Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-19 Dipanjan Karati, Dileep Kumar
:: Mitosis of somatic cells produces a daughter cell. Apoptosis, a naturally programmed cellular death mechanism, kills abnormal cells produced by mitosis. Cancer can develop when this equilibrium is disrupted, either by an upsurge in cell propagation or a reduction in tissue demise. Cancer therapy aims to cause cancer cells to die while inflicting little harm to healthy cells. This review of apoptotic
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Calpain Inhibitor Calpeptin Improves Pancreatic Fibrosis in Mice with Chronic Pancreatitis by Inhibiting the Activation of Pancreatic Stellate Cells Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-15 Jie Shen, Wenqin Xiao, Guanzhao Zong, Pengli Song, Chuanyang Wang, Jingpiao Bao, Qi Peng, Zhu Mei, Jingjing Wang, Ruiyan Wang, Jing Jiang, Rong Wan, Jianbo Ni, Xingpeng Wang, Guoyong Hu
Background:: Pancreatic fibrosis is a hallmark feature of chronic pancreatitis (CP), resulting in persistent damage to the pancreas. The sustained activation of pancreatic stellate cells (PSCs) plays a pivotal role in the progression of pancreatic fibrosis and is a major source of extracellular matrix (ECM) deposition during pancreatic injury. Methods:: Calpain is a calcium-independent lysosomal neutral
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Creatine in Cognitive Performance: A Commentary Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-15 Jasper Okoro Godwin Elechi, Diana Marisol Abrego Guandique, Roberto Cannataro
:: Given the importance of cognition in everyday life, medicines that improve cognition safely and affordably are highly wanted. Creatine is an amino acid-derived substance that aids in the restoration of adenosine triphosphate (ATP), which provides energy to muscle and brain tissue. Although the relationship between creatine and cognitive performance is still debatable, here is a brief description
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An Essential Role of c-Fos in Notch1-mediated Promotion of Proliferation of KSHV-Infected SH-SY5Y Cells Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-15 Huiling Xu, Jinghong Huang, Lixia Yao, Wenyi Gu, Aynisahan Ruzi, Yufei Ding, Ying Li, Weihua Liang, Jinfang Jiang, Zemin Pan, Dongdong Cao, Naiming Zhou, Dongmei Li, Jinli Zhang
Background:: This study aimed to investigate the influence of Notch1 on c-Fos and the effect of c-Fos on the proliferation of Kaposi's sarcoma-associated herpesvirus (KSHV)-infected neuronal cells. Methods:: Real-time PCR and western blotting were used to determine c-Fos expression levels in KSHV-infected (SK-RG) and uninfected SH-SY5Y cells. C-Fos levels were measured again in SK-RG cells with or
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The Regulatory Mechanism of Hypoxia-inducible Factor 1 and its Clinical Significance Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2024-01-15 Chun-Li Yin, Yu-Jie Ma
:: Hypoxia-inducible factor (HIF) is a nuclear protein that plays a crucial role in oxygen homeostasis through its transcriptional activity and thousands of target gene profiles. Through transcriptional and post-transcriptional regulation, the downstream target genes of HIF can trigger multiple pathological responses in the body, including energy metabolism, cytopenia, and angiogenesis. There are three
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Screening and Identification of ESR1 as a Target of Icaritin in Hepatocellular Carcinoma: Evidence from Bibliometrics and Bioinformatic Analysis Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-12-27 Yinghui Zhou, Jia Gu, Huiying Yu, Fengyang Chen, Chao Long, Maiweilan Maihemuti, Tingsong Chen, Wei Zhang
Background: In 2022, icaritin a Traditional Chinese Medicine with estrogen-like activities was recommended by the CSCO guidelines as a systematic treatment for patients with advanced HCC due to its clinical safety and efficacy. However the mechanism and targets of icaritin are unclear. In this study we aimed to reveal the target of icaritin in HCC Methods: First literature related to icaritin was downloaded
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Arsenic Exposure and Amyloid Precursor Protein Processing: A Focus on Alzheimer's Disease Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-11-06 Ravikant Sharma, MD. Abubakar, Priya Bisht, Mahesh Rachamalla, Arun Kumar, Krishna Murti, Velayutham Ravichandiran, Nitesh Kumar
Background:: Arsenic is present in above permissible safe limits in groundwater, soil, and food, in various areas of the world. This is increasing exposure to humankind and affecting health in various ways. Alternation in cognition is one among them. Epidemiological research has reflected the impact of arsenic exposure on children in the form of diminished cognition. Aims:: Considering this fact, the
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All-trans Retinoic Acid Increased Transglutaminase 2 Expressions in BV-2 Cells and Cultured Astrocytes Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-11-02 Katsura Takano-Kawabe, Tatsuhiko Izumo, Tomoki Minamihata Minamihata, Mitsuaki Moriyama
Background:: Activation of microglia and astrocytes has been observed in Alzheimer’s disease (AD). Transglutaminase 2 (TG2) is reported to be activated in AD and involved in cell proliferation, differentiation, and inflammation. Moreover, amyloid β (Aβ) aggregation is detected as a characteristic pathology in the AD brain, and is known to be a substrate of TG2. All-trans retinoic acid (ATRA) can modify
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Deregulated MicroRNAs involved in P53 Signaling Pathway in Breast Cancer with Focus on Triple-negative Breast Cancer Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-11-02 yasaman Naeimzadeh, zahra Heidari, Vahid Razban, Sahar Khajeh
Background:: Breast cancer (BC), as a heterogenous disease, is the most common cancer among women worldwide. Triple-negative breast cancer (TNBC) is the most aggressive and malignant subtype with a poor prognosis and a high rate of relapse and metastasis that is closely linked to epithelial–mesenchymal transition (EMT). It is well-documented that miRNAs play oncogenic (oncomiR) or tumor-suppressive
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SGLT2 Inhibitors and Diabetic Kidney Disease: Targeting Multiple and Interrelated Signaling Pathways for Renal Protection Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-31 Georgios Papaetis
: Almost 20-40% of all patients suffering from diabetes mellitus experience chronic kidney disease, which is related to higher mortality (cardiovascular and all-cause). The implication of several pathophysiological mechanisms (hemodynamic, tubular, metabolic and inflammatory) in the pathogenesis of diabetic kidney disease generates an urgent need to develop multitarget therapeutic strategies to face
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Regulating miRNAs Expression by Resveratrol: Novel Insights based on Molecular Mechanism and Strategies for Cancer Therapy Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-31 Atoosa Keshavarzmotamed, Vahide Mousavi, Niloufar Masihipour, Atefe Rahmati, Rohollah Mousavi Dehmordi, Behrooz Ghezelbash, Mina Alimohammadi, Alireza Mafi
: Resveratrol, a polyphenolic phytoalexin found in a wide range of plants, including grapes, berries, and peanuts, is an extensively researched phytochemical with unique pharmacological capabilities and amazing potential to affect many targets in various cancers. Resveratrol's anti-cancer activities are due to its targeting of a variety of cellular and molecular mechanisms and crucial processes involved
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Review of the Role of Metabolic Factors in Determining the Post-surgical Adhesion and its Therapeutic Implications, with a Focus on Extracellular Matrix and Oxidative Stress Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-27 Mahmoud Tavakkoli, Rozita Khodashahi, Mohsen Aliakbarian, Hoda Rahimi, Kiarash Ashrafzadeh, Gordon Ferns, Ebrahim Khaleghi, Mohammad-Hassan Arjmand
: The potential role of metabolic reprogramming in fibrogenesis has recently attracted interest. Extracellular matrix stiffness, inflammation, and subsequent oxidative stress are essential mediators in the causation of fibrosis. The prevention of post-surgical adhesion is a challenge in medicine. It is defined as a fibrotic disorder in which adhesive bands develop after abdominal or pelvic surgery
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Gentiopicroside Ameliorated Ductular Reaction and Inflammatory Response in DDC-induced Murine Cholangiopathies Model Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-26 Juan Hao, Jian Wu, Quanjun Yang, Kan Lu, Yi Xu, Yiyue Chen, Jibo Liu, Xiaohong Shao, Chunling Zhu, Yaqin Ding, Xin Xie
Background:: Cholangiopathies comprise a spectrum of diseases without curative treatments. Pharmacological treatments based on bile acid (BA) metabolism regulation represent promising therapeutic strategies for the treatment of cholangiopathies. Gentiopicroside (GPS), derived from the Chinese medicinal herb Gentianae Radix, exerts pharmacological effects on bile acid metabolism regulation and oxidative
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Maprotiline Prompts an Antitumour Effect by Inhibiting PD-L1 Expression in Mice with Melanoma Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-19 Lirui Liang, Yang Li, Yang Jiao, Chunjing Zhang, Mingguang Shao, Hanyu Jiang, Zunge Wu, Haoqi Chen, Jiaming Guo, Huijie Jia, Tiesuo Zhao
background: Research has revealed that the expression of PD-L1 is significantly upregulated in tumour cells and that the binding of programmed cell death protein 1 (PD-1) to programmed cell death 1 ligand 1 (PD-L1) inhibits the response of T cells, thereby suppressing tumour immunity. Therefore, blocking PD-L1/PD-1 signalling has become an important target in clinical immunotherapy. Some old drugs
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Dual Role of Pregnane X Receptor in Nonalcoholic Fatty Liver Disease Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-19 Yuan Xu, Ziming An, Shufei Wang, Yiming Ni, Mingmei Zhou, Qin Feng, Xiaojun Gou, Meiling Xu, Ying Qi
: The incidence of nonalcoholic fatty liver disease (NAFLD) has been rising worldwide in parallel with diabetes and metabolic syndrome. NAFLD refers to a spectrum of liver abnormalities with a variable course, ranging from nonalcoholic fatty liver (NAFL) to nonalcoholic steatohepatitis (NASH), eventually leading to cirrhosis and hepatocellular carcinoma. Pregnane X receptor (PXR), a member of the nuclear
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Co-treatment of Astragaloside IV with Vitamin D in Diabetic Peripheral Neuropathic Rats: Protective Effects and Potential Mechanisms Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-19 Fengyan Tang, Bo Zhao, Li Zhang, Faisal Raza, Hajra Zafar, Shao Zhong, Lin Li, Wenhua Zhu, Lingna Fang, Bing Lu, Liwen Shen, Ping Guo, Nengxing Yu, Quanmin Li
Objective: The potential mechanism underlying the protective effect of Astragaloside IV (AS-IV) co-treatment with 1, 25-dihydroxy-vitamin D (Vit-D) on neuropathy in diabetic high-fat rats was investigated Methods: The rat diabetic hyperlipidemia (DH) model was established via streptozotocin and a high-fat diet (HFD). After co-treatment (of AS-IV and Vit-D at respective doses of 50 mg/kg via oral gavage
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Targeting FGFR3 is a useful Therapeutic Strategy for Rheumatoid Arthritis Treatment Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-19 Shan-Fu Yu, Tien-Tsai Cheng, Gong-Kai Huang, Chung-Yuan Hsu, Ying-Hsien Kao, Yueh-Hua Chung
background: Rheumatoid arthritis (RA) is a systemic inflammatory disease in which TNF-α plays an important role. Fibroblast growth factor receptor 3 (FGFR3) is reportedly involved in RA by regulating expression of inflammatory cytokines. objective: This study examined the expression profile of FGFR3 in human synovial biopsy tissues and evaluated its gene silencing effects on behaviors of synovial cells
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RBM3 Accelerates Wound Healing of Skin in Diabetes through ERK1/2 Signaling Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-19 Jianguo Feng, Menghong Long, Xin Zhao, Pijun Yan, Yunxiao Lin, Maohua Wang, Wenhua Huang
background: With increasing risk of infections and other serious complications, the underlying molecular mechanism of diabetic wound healing impairment has not been completely understood. Cold shock proteins (CSPs) including CIRP and RBM3 are highly expressed in the skin, however, it is unknown whether CSPs are involved in impaired diabetic skin wound healing. objective: To examine the functions of
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Artemisinin Attenuates Isoproterenol-induced Cardiac Hypertrophy via the ERK1/2 and p38 MAPK Signaling Pathways Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-10-19 Renxing Song, Chunming Xiong, Juncai Bai, Zhenzhou Bai, Wei Liu
Background: Artemisinin (ART) is mainly derived from Artemisia annua, a traditional Chinese medicinal plant, and has been found to affect cellular biochemical processes, such as proliferation, angiogenesis, and apoptosis, in addition to its antimalarial properties. However, its effect on cardiac hypertrophy and the underlying mechanisms remain unclear. Objective: This study aimed to investigate the
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Current strategies for the management of psoriasis with potential pharmacological pathways using herbals and immuno-biologicals Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-09-19 Kiran Singh Sharma, Sumit Kumar
Background: Psoriasis is an acute to chronic multifunctional inflammatory skin disorder mediated through T-cell activation, dendritic cell intervention, local vascular variations, atypical keratinocyte proliferation, and neutrophil activation, leading to a skin disorder with no permanent cure. Objective: This review aims to find a potent, secure, and dependable medication, with a more scientific examination
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PF-04449913 Inhibits Proliferation and Metastasis of Colorectal Cancer Cells by Down-regulating MMP9 Expression through the ERK/p65 Pathway Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-09-19 Yejiao Ruan, Guangrong Lu, Yaojun Yu, Yue Luo, Hao Wu, Yating Shen, Zejun Gao, Yao Shen, Zhenzhai Cai, Liyi Li
INTRODUCTION: Colorectal cancer remains a life-threatening malignancy with increasing morbidity and mortality worldwide. Therefore, new and effective anti-colorectal cancer therapeutics are urgently needed. METHOD: In this study, we have studied the anti-tumor properties and potential mechanisms of PF-04449913. Colorectal cancer cell viability was reduced by PF-04449913 in a dose-dependent manner.
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Targeting mutant-p53 for cancer treatment: Are we there yet? Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-09-15 Dhi Vya Lim, Wei Hwei Woo, Jing Xuan Lim, Xin Yee Loh, Hui Ting Soh, Seng Yung Adrian Lim, Zheng Yang Lee, Hui Yin Yow, Sharina Binti Hamzah, Sellappans Renukha, Jhi Biau Foo
Background: Mutations in the TP53 gene are the most common among genetic alterations in human cancers, resulting in the formation of mutant p53 protein (mutp53). Mutp53 promotes proliferation, migration, invasion, and metastasis in cancer cells. Not only does the initiation of oncogenesis ensue due to mutp53, but resistance towards chemotherapy and radiotherapy in cancer cells also occurs. This review
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A Deeply Quiescent Subset of CML LSC Depend on FAO Yet Avoid Deleterious ROS by Suppressing Mitochondrial Complex I Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-09-11 Nyam-Osor Chimge, Min-Hsuan Chen, Cu Nguyen, Yuqi Zhao, Xiwei Wu, Paulina Garcia Gonzalez, Heather Ogana, Samantha Hurwitz, Jia-Ling Teo, Xiaolong Chen, Juan Du, Victor Jin, Yong-Mi Kim, Masaya Ono, Rafael J Argüello, Michael kahn
Background and Objective: Disease relapse and therapy resistance remain serious impediments to treating cancer. Leukemia stem cells (LSC) are therapy resistant and the cause of relapse. A state of deep quiescence appears to enable cancer stem cells (CSC) to acquire new somatic mutations essential for disease progression and therapy resistance. Both normal hematopoietic stem cells (HSC) and LSC share
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At the Crossroads of TNFα Signaling and Cancer Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-09-11 Sonal M. Manohar
: Tumor necrosis factor-alpha (TNFα) is a pleiotropic pro-inflammatory cytokine of the TNF superfamily. It regulates key cellular processes such as death, and proliferation besides its well-known role in immune response through activation of various intracellular signaling pathways (such as MAPK, Akt, NF-κB, etc.) via complex formation by ligand-activated TNFα receptors. TNFα tightly regulates the
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Research Progress of the Molecular Mechanism of Antithyroid Cancer Activity of Shikonin Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-09-06 Chunguang Sun, Lin Liao
: Thyroid cancer is one of the most common endocrine neoplasms. Treatment methods include surgical resection, radioactive iodine therapy, inhibition of thyroid-stimulating hormone, and inhibition of kinase-based target therapies. These treatments induced adverse effects. Lithospermum officinale possesses antioxidant, anticancer, burn-healing, and anti-inflammatory activities, and Shikonin is the main
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Antiarrhythmic Potential of Epicardial Botulinum Toxin Injection for Suppression of Postoperative Atrial Fibrillation Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-09-06 Michael Spartalis, Eleftherios Spartalis, Dimitrios Iliopoulos, Gerasimos Siasos
: Following heart surgery, postoperative atrial fibrillation (AF) is the most prevalent kind of secondary AF and the most frequent adverse event. Postoperative AF is related to a number of unfavorable cardiac outcomes, such as heart failure, stroke, and death. However, the pharmacological treatment for postoperative AF is only relatively efficient and is frequently linked to detrimental complications
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Differential Kat3 Coactivator Usage Regulates Brain Metabolism and Neuronal Differentiation Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-28 Erasmus Kofi Poku, Masaya Ono, Yusuke Higuchi, Junie Chea, Elizabeth Melendez, Jia-Ling Teo, Cu Nguyen, Nyam-Osor Chimge, Michael Kahn
Introduction: Our previous work has demonstrated significant effects on the oxidative stress response, mitochondrial function, and oxidative phosphorylation in the livers and intestines of p300 S89A knockin (S89AKI) mice. We now show that this mutation is also associated with brain metabolic defects and neuronal differentiation. Methods: p300 S89A edited P19 cells, and S89AKI mice demonstrated metabolic
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The effect of fingolimod on renal ischemia/reperfusion injury in a rat model Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-25 Sepideh Zununi Vahed, Yasin Bagheri, Elham Ahmadian, Seyyedeh Mina Hejazian, Maryam Raeesi, Mahmoodreza Ardalan
Background: Ischemia/reperfusion injury (IRI) is a leading cause of acute kidney injury (AKI) that induces inflammation and oxidative stress. The main goal of the current study was to assess the impact of fingolimod on kidney IRI in rats. Methods: For this purpose, 18 male Wistar rats (220–250g) were divided into three groups including (i) Sham, (ii) I/R, and (iii) fingolimod+I/R. The last group was
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Physalin B Reduces Tau Phosphorylation and Cell Apoptosis in HEK293 Cells by Activating FoxO1 Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-24 Wei Zhang, Yating Shi, Mingti Lv, Yimin Zhang, Wei Ren, Ruling Shi, Hecheng Wang, Linlin Shan
Background: Physalin B (PB) is one of the main active compounds of Solanaceae plants, with a wide range of biological activities. PB reportedly has the potential to treat Alzheimer’s disease (AD). Objective: In this study, we investigated the effect of PB on Tau phosphorylation and cell apoptosis using Tau-expressing HEK293 cells (HEK293/Tau) as a cellular model. Methods: The optimum concentration
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Grp94 Inhibitor HCP1 Suppressed the Replication of SVA in BHK-21 Cells and PK-15 Cells Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-23 Shuo Wang, XiaoLing Cui, Ren Hui, Wen Yao, BaoXiang Zhao, Jun Li, JunYing Miao
Background: Glucoregulatory protein 94 (Grp94) is necessary for the post-viral life cycle and plays a quality control role in viral proteins, but the role of Grp94 in regulating viral replication in host cells is not well known. Therefore, finding a compound that can regulate Grp94 will help us to study the mechanism of viral replication. Previously, we synthesized a coumarin pyrazoline derivative
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The Targeted Therapies for Osteosarcoma via Six Major Pathways Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-21 Zhen Zhang, Shuxing Wang, Quanlei Ren, Guoqing Li, Xiaoxuan Zhao, Xing Zhao
: Osteosarcoma is the most common primary bone malignancy and has a high tendency of local invasion. Although a lot of studies have focused on chemotherapy and combination chemotherapy regimens in recent years, still, there is no particularly perfect regimen for the treatment of relapsed or metastatic OS, and the prognosis is still relatively poor. As a new therapeutic method, targeted therapy provides
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Apelin receptor dimerization and oligomerization Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-18 Mahboobeh Yeganeh-Hajahmadi, Yasamin Moosavi-Saeed, Farzaneh Rostamzadeh
: Apelin and its receptor are expressed in many tissues and play an important role in maintaining the homeostasis of the cardiovascular system and body fluids. Also, the association of this system with many diseases, such as diabetes, hypertension, obesity, cancer, diabetic retinopathy, etc., has been determined. This system is considered a therapeutic goal in many mentioned diseases. G protein-coupled
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Hepatic Ischemia-reperfusion Injury: Protective Approaches and Treatment Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-16 Kuldeep Singh, Jeetendra Kumar Gupta, Shivendra Kumar, Anurag, Soumyadip Mukherjee, Aman Patel
Ischemia and reperfusion damage to the liver is one of the major causes of hepatic dysfunction and liver failure after a liver transplant. The start of hepatic ischemia-reperfusion damage is linked to metabolic acidosis, Kupffer cells, neutrophils, excessive calcium, and changes in the permeability of the mitochondrial membrane. Hypoxia activates Kupffer cells, resulting in the production of reactive
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Mitochondria-Targeted Uncouplers Decrease Inflammatory Reactions in Endothelial Cells by Enhancing Methylation of the ICAM1 Gene Promoter Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-08-17 Roman A. Zinovkin, Liudmila A. Zinovkina, Ciara I. Makievskaya, Ivan I. Galkin
Introduction: The study aimed to investigate the effects of low concentrations of mitochondrial uncouplers in endothelial cells on the CpG dinucleotide methylation of the ICAM1 gene promoter. The excessive inflammatory response in the endothelium is responsible for the development of many cardiovascular diseases. Mitochondria are important regulators of endothelial cell functions. Mild uncoupling of
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Mediating role of miR-451/ETV4/MMP13 signaling axis on epithelial-mesenchymal transition in promoting non-small cell lung cancer progression Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-21 Xi Yu, Xue-Jiao Qian, Jing-Wen Wang, Jiang-Bo Liu
Background: Lung cancer is a leading cause of cancer mortality. It is one of the most abundant cancer types clinically, with 2 million new cases diagnosed yearly. Aims: Using clinically collected non-small cell lung cancer (NSCLC) samples, we sought to hypothesize an innovative intact signaling cascade for the disorder. Methods: We dissected snap-frozen NSCLC tissues along with sibling-paired nearby
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E7386 is not a Specific CBP/β-Catenin Antagonist Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-20 Yusuke Higuchi, Cu Nguyen, Nyam-Osor Chimge, Ching Ouyang, Jia-Ling Teo, Michael Kahn
Background and Objective: The first clinically evaluated CBP/β-catenin antagonist, PRI-724, displayed an excellent safety profile administered intravenously via continuous infusion. Eisai recently disclosed a third-generation, orally available, reportedly CBP/β-catenin antagonist, E7386. However, several structural features and the reported cytotoxicity of E7386 were unexpected for a specific CBP/β-catenin
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CD73 Blockade Alleviated Hepatic Fibrosis via Inhibiting Hepatic Stellate Cells Proliferation and Activation Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-13 Lan Yang, Zhao-Wei Gao, Xia-Nan Wu, Chong Liu, Juan Zhang, Hui-Zhong Zhang, Ke Dong
Background: Liver fibrosis is associated with the activation of hepatic stellate cells (HSCs). Inhibition of HSCs activation is a strategy for alleviating hepatic fibrogenesis. CD73 is involved in liver disease development, while the mechanism remains unclear. Objective: This study aimed to investigate the effect of CD73 targeting inhibition on liver fibrosis. Methods: Intraperitoneal injection of
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Antimicrobial Resistance of Clinical Klebsiella pneumoniae Isolates: Involvement of AcrAB and OqxAB Efflux Pumps Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-13 Osman Albarri, Manaf AlMatar, Işil Var, Fatih Köksal
Background: Over the last several decades, the AcrAB and OqxAB efflux pumps have been found to cause multidrug resistance (MDR) in various bacteria, most notably Klebsiella pneumoniae. Antibiotic resistance surges with increased expression of the acrAB and oqxAB efflux pumps. Methods: In accordance with CLSI guidelines, a disk diffusion test was carried out using 50 K. pneumoniae isolates obtained
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Perspectives on the Role of P21-Activated Kinase 1 (PAK1) in the Intestinal Anti-inflammatory and Antitumor Potential of Artepillin C Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-13 Luisa Mota da Silva
The Brazilian biodiversity may bring new perspectives to the therapy of Inflammatory Bowel Diseases (IBD) and intestinal cancer. The effect of Brazilian Green Propolis in reducing ulcerative colitis in mice has already been described, as well as high amounts of the prenylated compound Artepellin C (ARC). The search for new pharmacological targets for IBD is also advancing. Among possibilities is the
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Fenbufen Alleviates Severe Acute Pancreatitis by Suppressing Caspase-1/Caspase-11-mediated Pyroptosis in Mice Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-13 Shien Shen, Wenqin Xiao, Weiliang Jiang, Kai Li, Xingya Guo, Guanzhao Zong, Chuanyang Wang, Jingpiao Bao, Jiahui Chen, Zhiyuan Cheng, Jie Shen, Rong Wan
Aim: In the present study, we aimed to investigate the effects of Fenbufen treatment on the SAP model induced by caerulein and lipopolysaccharide. Background: Severe acute pancreatitis (SAP) is an extremely dangerous disease with high mortality, which is associated with inflammatory response and acinar cell death. The caspase family plays an important role in cell death, such as caspase-1 and caspase-11
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Targeting Cellular Senescence: A Potential Therapeutic approach for Alzheimer’s Disease Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-13 Shrishti Singh, Lokesh Kumar Bhatt
Although Amyloid beta plaque and neurofibrillary tangles are considered the two main hallmarks of Alzheimer’s disease (AD), the mechanism by which they contribute is not clearly understood. Cellular senescence (CS) has been demonstrated to be a key characteristic of AD. Recent research suggests that persistent buildup of senescent cells over time results in protracted activation of inflammatory stress
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Pathophysiology, Current Therapeutic Options, Vaccine Candidates, and Drug Targets for Human Brucellosis Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-07-13 Manisha Pritam, Rajnish Kumar
Brucellosis is an infectious disease caused by different species of Brucella bacteria. It is also known as Malta fever, one of the neglected diseases that can cause infection in both animals and humans. Although human-to-human infection is rare, it can spread through the inhalation of airborne agents, and if left untreated, it can lead to serious health complications. In this review, we aim to highlight
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A Network Medical Framework based on Inflammatory Genes to Identify Drug Candidates for Abdominal Aortic Aneurysms Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-06-06 Xiaoyang Niu, Bing Wang
Background: Clinically, abdominal aortic aneurysms (AAA) can be treated with surgical intervention, but there is currently no effective drug for the disease. Methods: This study analyzed the biomedical data of single-cell RNA sequencing (scRNA-seq), RNA-seq and the network medical data of drug-target interaction as well as protein-protein interaction to identify key targets and potential drug compounds
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Mammalian Target of Rapamycin (mTOR) Signalling Pathway-A Potential Target for Cancer Intervention: A Short Overview Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-05-25 Rajesh Basnet, Buddha Bahadur Basnet, Radheshyam Gupta, TilBahadur Basnet, Sandhya Khadka, Md Shan Alam
Background: The mammalian role of the rapamycin (mTOR) pathway is the practical nutrient-sensitive regulation of animal growth and plays a central role in physiology, metabolism, and common diseases. The mTOR is activated in response to nutrients, growth factors, and cellular energy. The mTOR pathway activates in various cellular processes and human cancer diseases. Dysfunction of mTOR signal transduction
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A Detailed Review of Molecular Pathways and Mechanisms Responsible for the Development and Aggravation of Neuropathy and Nephropathy in Diabetes Curr. Mol. Pharmacol. (IF 2.7) Pub Date : 2023-05-12 Phool Chandra, Neetu Sachan, Nikita Saraswat, Niraj Vyawahare
Background: Diabetic mellitus is responsible for triggering many conditions, such as neuropathy, nephropathy, and retinopathy. Hyperglycemia leads to the development of oxidative stress conditions, activation of pathways, and generation of metabolites, leading to complications like neuropathy and nephropathy. Objective: This paper aims to discuss the mechanism of actions, pathways, and metabolites