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Pharmacological characterization of allosteric modulators: A case for chemokine receptors Med. Res. Rev. (IF 13.3) Pub Date : 2024-04-18 Lisa S. den Hollander, Adriaan P. IJzerman, Laura H. Heitman
Chemokine receptors are relevant targets for a multitude of immunological diseases, but drug attrition for these receptors is remarkably high. While many drug discovery programs have been pursued, most prospective drugs failed in the follow‐up studies due to clinical inefficacy, and hence there is a clear need for alternative approaches. Allosteric modulators of receptor function represent an excellent
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1,2,4,5‐Tetraoxane derivatives/hybrids as potent antimalarial endoperoxides: Chronological advancements, structure−activity relationship (SAR) studies and future perspectives Med. Res. Rev. (IF 13.3) Pub Date : 2024-04-15 Abdul Rahaman T. A., Thakar Neha Rajendra, Kshirsagar Prasad Suhas, Sirish K. Ippagunta, Sandeep Chaudhary
Malaria is a life‐threatening disease that affects tropical and subtropical regions worldwide. Various drugs were used to treat malaria, including artemisinin and derivatives, antibiotics (tetracycline, doxycycline), quinolines (chloroquine, amodiaquine), and folate antagonists (sulfadoxine and pyrimethamine). Since the malarial parasites developed drug resistance, there is a need to develop new chemical
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Galectin‐8 inhibition and functions in immune response and tumor biology Med. Res. Rev. (IF 13.3) Pub Date : 2024-04-13 Edvin Purić, Ulf J. Nilsson, Marko Anderluh
Galectins are among organisms' most abundantly expressed lectins (carbohydrate‐binding proteins) that specifically bind β‐galactosides. They act not only outside the cell, where they bind to extracellular matrix glycans, but also inside the cell, where they have a significant impact on signaling pathways. Galectin‐8 is a galectin family protein encoded by the LGALS8 gene. Its role is evident in both
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A promising future of metal‐N‐heterocyclic carbene complexes in medicinal chemistry: The emerging bioorganometallic antitumor agents Med. Res. Rev. (IF 13.3) Pub Date : 2024-04-09 Qian Zhao, Bo Han, Cheng Peng, Nan Zhang, Wei Huang, Gu He, Jun‐Long Li
Metal complexes based on N‐heterocyclic carbene (NHC) ligands have emerged as promising broad‐spectrum antitumor agents in bioorganometallic medicinal chemistry. In recent decades, studies on cytotoxic metal–NHC complexes have yielded numerous compounds exhibiting superior cytotoxicity compared to cisplatin. Although the molecular mechanisms of these anticancer complexes are not fully understood, some
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The menace of severe adverse events and deaths associated with viral gene therapy and its potential solution Med. Res. Rev. (IF 13.3) Pub Date : 2024-03-29 Artyom Kachanov, Anastasiya Kostyusheva, Sergey Brezgin, Ivan Karandashov, Natalia Ponomareva, Andrey Tikhonov, Alexander Lukashev, Vadim Pokrovsky, Andrey A. Zamyatnin, Alessandro Parodi, Vladimir Chulanov, Dmitry Kostyushev
Over the past decade, in vivo gene replacement therapy has significantly advanced, resulting in market approval of numerous therapeutics predominantly relying on adeno‐associated viral vectors (AAV). While viral vectors have undeniably addressed several critical healthcare challenges, their clinical application has unveiled a range of limitations and safety concerns. This review highlights the emerging
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Benzopyrone, a privileged scaffold in drug discovery: An overview of FDA‐approved drugs and clinical candidates Med. Res. Rev. (IF 13.3) Pub Date : 2024-03-27 Venu Sharma, Ankita Sharma, Bhagyashri N. Wadje, Sandip B. Bharate
Natural products have always served as an important source of drugs for treating various diseases. Among various privileged natural product scaffolds, the benzopyrone class of compounds has a substantial presence among biologically active compounds. One of the pioneering anticoagulant drugs, warfarin approved in 1954 bears a benzo‐α‐pyrone (coumarin) nucleus. The widely investigated psoriasis drugs
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Elimination of the hepatitis B virus: A goal, a challenge Med. Res. Rev. (IF 13.3) Pub Date : 2024-03-26 Robério Amorim de Almeida Pondé, Guilherme de Sousa Pondé Amorim
The hepatitis B elimination is a goal proposed by the WHO to be achieved by 2030 through the adoption of synergistic measures for the prevention and chronic HBV infection treatment. Complete cure is characterized by the HBV elimination from the body and is the goal of the chronic hepatitis B treatment, which once achieved, will enable the hepatitis B elimination. This, today, has been a scientific
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Antineoplastics for treating Alzheimer's disease and dementia: Evidence from preclinical and observational studies Med. Res. Rev. (IF 13.3) Pub Date : 2024-03-26 Viswanath Das, John H. Miller, Charanraj Goud Alladi, Narendran Annadurai, Juan Bautista De Sanctis, Lenka Hrubá, Marián Hajdúch
As the world population ages, there will be an increasing need for effective therapies for aging‐associated neurodegenerative disorders, which remain untreatable. Dementia due to Alzheimer's disease (AD) is one of the leading neurological diseases in the aging population. Current therapeutic approaches to treat this disorder are solely symptomatic, making the need for new molecular entities acting
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Bioactive atropisomers: Unraveling design strategies and synthetic routes for drug discovery Med. Res. Rev. (IF 13.3) Pub Date : 2024-03-22 Shuai‐Jiang Liu, Qian Zhao, Xiao‐Chen Liu, Allan B. Gamble, Wei Huang, Qian‐Qian Yang, Bo Han
Atropisomerism, an expression of axial chirality caused by limited bond rotation, is a prominent aspect within the field of medicinal chemistry. It has been shown that atropisomers of a wide range of compounds, including established FDA‐approved drugs and experimental molecules, display markedly different biological activities. The time‐dependent reversal of chirality in atropisomers poses complexity
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Most recent advances and applications of extracellular vesicles in tackling neurological challenges Med. Res. Rev. (IF 13.3) Pub Date : 2024-03-19 Mandeep Kaur, Fusco Salvatore, Bram Van den Broek, Jaya Aseervatham, Abdolmohamad Rostami, Lorraine Iacovitti, Claudio Grassi, Barbara Lukomska, Amit K. Srivastava
Over the past few decades, there has been a notable increase in the global burden of central nervous system (CNS) diseases. Despite advances in technology and therapeutic options, neurological and neurodegenerative disorders persist as significant challenges in treatment and cure. Recently, there has been a remarkable surge of interest in extracellular vesicles (EVs) as pivotal mediators of intercellular
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Enhancing healthy aging with small molecules: A mitochondrial perspective Med. Res. Rev. (IF 13.3) Pub Date : 2024-03-14 Xiujiao Qin, Hongyuan Li, Huiying Zhao, Le Fang, Xiaohui Wang
The pursuit of enhanced health during aging has prompted the exploration of various strategies focused on reducing the decline associated with the aging process. A key area of this exploration is the management of mitochondrial dysfunction, a notable characteristic of aging. This review sheds light on the crucial role that small molecules play in augmenting healthy aging, particularly through influencing
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Emerging roles of nerve‐bone axis in modulating skeletal system Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-29 Jingya Li, Zhuoyuan Zhang, Jinru Tang, Zeyu Hou, Longjiang Li, Bo Li
Over the past decades, emerging evidence in the literature has demonstrated that the innervation of bone is a crucial modulator for skeletal physiology and pathophysiology. The nerve‐bone axis sparked extensive preclinical and clinical investigations aimed at elucidating the contribution of nerve‐bone crosstalks to skeleton metabolism, homeostasis, and injury repair through the perspective of skeletal
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Fluorescent imaging probes for in vivo ovarian cancer targeted detection and surgery Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-17 Roberta Solidoro, Antonella Centonze, Morena Miciaccia, Olga Maria Baldelli, Domenico Armenise, Savina Ferorelli, Maria Grazia Perrone, Antonio Scilimati
Ovarian cancer is the most lethal gynecological cancer, with a survival rate of approximately 40% at five years from the diagno. The first-line treatment consists of cytoreductive surgery combined with chemotherapy (platinum- and taxane-based drugs). To date, the main prognostic factor is related to the complete surgical resection of tumor lesions, including occult micrometastases. The presence of
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cGAS-STING pathway agonists are promising vaccine adjuvants Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-07 Xinyu Tian, Jiayuan Ai, Xiaohe Tian, Xiawei Wei
Adjuvants are of critical value in vaccine development as they act on enhancing immunogenicity of antigen and inducing long-lasting immunity. However, there are only a few adjuvants that have been approved for clinical use, which highlights the need for exploring and developing new adjuvants to meet the growing demand for vaccination. Recently, emerging evidence demonstrates that the cGAS-STING pathway
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Front Cover Image, Volume 44, Issue 2 Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-05 Kang Wang, Yuecan Zhang, Guangji Wang, Haiping Hao, Hong Wang
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Inside Front Cover Image, Volume 44, Issue 2 Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-05 Yu Zheng, Yuke Li, Mao Li, Rujing Wang, Yuhong Jiang, Mengnan Zhao, Jun Lu, Rui Li, Xiaofang Li, Sanjun Shi
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Development and therapeutic potential of GSPT1 molecular glue degraders: A medicinal chemistry perspective Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-05 Xiujin Chang, Fangui Qu, Chunxiao Li, Jingtian Zhang, Yanqing Zhang, Yuanyuan Xie, Zhongpeng Fan, Jinlei Bian, Jubo Wang, Zhiyu Li, Xi Xu
Unprecedented therapeutic targeting of previously undruggable proteins has now been achieved by molecular-glue-mediated proximity-induced degradation. As a small GTPase, G1 to S phase transition 1 (GSPT1) interacts with eRF1, the translation termination factor, to facilitate the process of translation termination. Studied demonstrated that GSPT1 plays a vital role in the acute myeloid leukemia (AML)
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Natural products as IL-6 inhibitors for inflammatory diseases: Synthetic and SAR perspective Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-02 Dipesh S. Harmalkar, Aneesh Sivaraman, Hossam Nada, Joohan Lee, Hyeseul Kang, Yongseok Choi, Kyeong Lee
Interleukin-6 (IL-6), a pleiotropic cytokine, plays a pivotal role in the pathophysiology of various diseases including diabetes, atherosclerosis, Alzheimer's disease, multiple myeloma, rheumatoid arthritis, and prostate cancer. The signaling pathways associated with IL-6 offer promising targets for therapeutic interventions in inflammatory diseases and IL-6-dependent tumors. Although certain anti-IL-6
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Nanotechnology and bioengineering approaches to improve the potency of mesenchymal stem cell as an off-the-shelf versatile tumor delivery vehicle Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-01 Mojtaba Taheri, Hossein Abdul Tehrani, Sadegh Dehghani, Mona Alibolandi, Ehsan Arefian, Mohammad Ramezani
Targeting actionable mutations in oncogene-driven cancers and the evolution of immuno-oncology are the two prominent revolutions that have influenced cancer treatment paradigms and caused the emergence of precision oncology. However, intertumoral and intratumoral heterogeneity are the main challenges in both fields of precision cancer treatment. In other words, finding a universal marker or pathway
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Cuproptosis: Mechanism, role, and advances in urological malignancies Med. Res. Rev. (IF 13.3) Pub Date : 2024-02-01 Jialong Wu, Jide He, Zenan Liu, Xuehua Zhu, Ziang Li, Anjing Chen, Jian Lu
Prostate, bladder, and kidney cancers are the most common malignancies of the urinary system. Chemotherapeutic drugs are generally used as adjuvant treatment in the middle, late, or recurrence stages after surgery for urologic cancers. However, traditional chemotherapy is plagued by problems such as poor efficacy, severe side effects, and complications. Copper-containing nanomedicines are promising
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Dissecting the pleiotropic roles of reactive oxygen species (ROS) in lung cancer: From carcinogenesis toward therapy Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-29 Ying Hou, Heng Wang, Jiarui Wu, Hongwei Guo, Xiuping Chen
Lung cancer is a major cause of morbidity and mortality. The specific pulmonary structure to directly connect with ambient air makes it more susceptible to damage from airborne toxins. External oxidative stimuli and endogenous reactive oxygen species (ROS) play a crucial role in promoting lung carcinogenesis and development. The biological properties of higher ROS levels in tumor cells than in normal
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Metal complexes bearing EGFR-inhibiting ligands as promising anticancer agents Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-27 Xiaoyan Ma, Zhaoran Wang, Yifei Li, Yawen Wang, Wukun Liu
Overexpression of the epidermal growth factor receptor (EGFR, erbB1) has been observed in a wide range of solid tumors and has frequently been associated with poor prognosis. As a result, EGFR inhibition has become an attractive anticancer drug design strategy, and a large number of small molecular inhibitors have been developed. Despite the widespread clinical use of EGFR tyrosine kinase inhibitors
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Recent advances in dietary androgen receptor inhibitors Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-27 Li Ren, Tiehua Zhang, Jie Zhang
As a nuclear transcription factor, the androgen receptor (AR) plays a crucial role not only in normal male sexual differentiation and growth of the prostate, but also in benign prostatic hyperplasia, prostatitis, and prostate cancer. Multiple population-based epidemiological studies demonstrated that prostate cancer risk was inversely associated with increased dietary intakes of green tea, soy products
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Emerging phosphodiesterase inhibitors for treatment of neurodegenerative diseases Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-27 Yu Xiang, Swapna Naik, Liyun Zhao, Jianyou Shi, Hengming Ke
Neurodegenerative diseases (NDs) cause progressive loss of neuron structure and ultimately lead to neuronal cell death. Since the available drugs show only limited symptomatic relief, NDs are currently considered as incurable. This review will illustrate the principal roles of the signaling systems of cyclic adenosine and guanosine 3′,5′-monophosphates (cAMP and cGMP) in the neuronal functions, and
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Recent advances in the adjunctive management of diabetic foot ulcer: Focus on noninvasive technologies Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-27 Fen Wang, Xiaoling Zhang, Jing Zhang, Qinqin Xu, Xuefeng Yu, Anhui Xu, Chengla Yi, Xuna Bian, Shiying Shao
Diabetic foot ulcer (DFU) is one of the most costly and serious complications of diabetes. Treatment of DFU is usually challenging and new approaches are required to improve the therapeutic efficiencies. This review aims to update new and upcoming adjunctive therapies with noninvasive characterization for DFU, focusing on bioactive dressings, bioengineered tissues, mesenchymal stem cell (MSC) based
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Preclinical evidence using synthetic compounds and natural products indicates that AMPK represents a potential pharmacological target for the therapy of pulmonary diseases Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-16 Chao Yang, Limor Rubin, Xiyong Yu, Philip Lazarovici, Wenhua Zheng
Adenosine 5′-monophosphate (AMP)-activated protein kinase (AMPK) is a highly conserved eukaryotic enzyme discovered as a key regulator of cellular energy homeostasis, with anti-inflammation, antioxidative stress, anticancer, and antifibrosis beneficial effects. AMPK is dysregulated in human pulmonary diseases such as acute lung injury, nonsmall cell lung cancer, pulmonary fibrosis, chronic obstructive
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The role of Toll-like receptors in neuropsychiatric disorders: Immunopathology, treatment, and management Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-16 Kiarash Saleki, Parsa Alijanizadeh, Nima Javanmehr, Nima Rezaei
Neuropsychiatric disorders denote a broad range of illnesses involving neurology and psychiatry. These disorders include depressive disorders, anxiety, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder, autism spectrum disorders, headaches, and epilepsy. In addition to their main neuropathology that lies in the central nervous system (CNS), lately, studies have highlighted the
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Insights into Ganoderma fungi meroterpenoids opening a new era of racemic natural products in mushrooms Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-10 Jiao-Jiao Zhang, Fu-Ying Qin, Yong-Xian Cheng
Ganoderma meroterpenoids (GMs) containing 688 structures to date were discovered to have multiple remarkable biological activities. 65.6% of meroterpenoids featuring stereogenic centers from Ganoderma species are racemates. Further, GMs from different Ganoderma species seem to have their own characteristics. In this review, a comprehensive summarization of GMs since 2000 is presented, including GM
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CXCR4/CXCL12 axis: “old” pathway as “novel” target for anti-inflammatory drug discovery Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-04 Liuxin Lu, Junjie Li, Xiaoying Jiang, Renren Bai
Inflammation is the body's defense response to exogenous or endogenous stimuli, involving complex regulatory mechanisms. Discovering anti-inflammatory drugs with both effectiveness and long-term use safety is still the direction of researchers' efforts. The inflammatory pathway was initially identified to be involved in tumor metastasis and HIV infection. However, research in recent years has proved
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The emergence of machine learning force fields in drug design Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-03 Mingan Chen, Xinyu Jiang, Lehan Zhang, Xiaoxu Chen, Yiming Wen, Zhiyong Gu, Xutong Li, Mingyue Zheng
In the field of molecular simulation for drug design, traditional molecular mechanic force fields and quantum chemical theories have been instrumental but limited in terms of scalability and computational efficiency. To overcome these limitations, machine learning force fields (MLFFs) have emerged as a powerful tool capable of balancing accuracy with efficiency. MLFFs rely on the relationship between
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H+-slip correlated to rotor free-wheeling as cause of F1FO-ATPase dysfunction in primary mitochondrial disorders Med. Res. Rev. (IF 13.3) Pub Date : 2024-01-03 Salvatore Nesci, Giovanni Romeo
Inborn errors of metabolism are related to mitochondrial disorders caused by dysfunction of the oxidative phosphorylation (OXPHOS) system. Congenital hypermetabolism in the infant is a rare disease belonging to Luft syndrome, nonthyroidal hypermetabolism, arising from a singular example of a defect in OXPHOS. The mitochondria lose coupling of mitochondrial substrates oxidation from the ADP phosphorylation
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Metabolomics at the tumor microenvironment interface: Decoding cellular conversations Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-26 Naomi Berrell, Habib Sadeghirad, Tony Blick, Charles Bidgood, Graham R. Leggatt, Ken O'Byrne, Arutha Kulasinghe
Cancer heterogeneity remains a significant challenge for effective cancer treatments. Altered energetics is one of the hallmarks of cancer and influences tumor growth and drug resistance. Studies have shown that heterogeneity exists within the metabolic profile of tumors, and personalized-combination therapy with relevant metabolic interventions could improve patient response. Metabolomic studies are
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Experimental structure based drug design (SBDD) applications for anti-leishmanial drugs: A paradigm shift? Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-24 Miguel Marín, Marta López, Laura Gallego-Yerga, Raquel Álvarez, Rafael Peláez
Leishmaniasis is a group of neglected tropical diseases caused by at least 20 species of Leishmania protozoa, which are spread by the bite of infected sandflies. There are three main forms of the disease: cutaneous leishmaniasis (CL, the most common), visceral leishmaniasis (VL, also known as kala-azar, the most serious), and mucocutaneous leishmaniasis. One billion people live in areas endemic to
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Glutathione-triggered prodrugs: Design strategies, potential applications, and perspectives Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-23 Jintao Zhao, Xinming Li, Tao Ma, Bingbing Chang, Baoxin Zhang, Jianguo Fang
The burgeoning prodrug strategy offers a promising avenue toward improving the efficacy and specificity of cytotoxic drugs. Elevated intracellular levels of glutathione (GSH) have been regarded as a hallmark of tumor cells and characteristic feature of the tumor microenvironment. Considering the pivotal involvement of elevated GSH in the tumorigenic process, a diverse repertoire of GSH-triggered prodrugs
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Advances in machine intelligence-driven virtual screening approaches for big-data Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-21 Neeraj Kumar, Vishal Acharya
Virtual screening (VS) is an integral and ever-evolving domain of drug discovery framework. The VS is traditionally classified into ligand-based (LB) and structure-based (SB) approaches. Machine intelligence or artificial intelligence has wide applications in the drug discovery domain to reduce time and resource consumption. In combination with machine intelligence algorithms, VS has emerged into revolutionarily
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Drugs/agents for the treatment of ischemic stroke: Advances and perspectives Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-21 Jian Jia, Weijie Jiao, Guan Wang, Jianbing Wu, Zhangjian Huang, Yihua Zhang
Ischemic stroke (IS) poses a significant threat to global human health and life. In recent decades, we have witnessed unprecedented progresses against IS, including thrombolysis, thrombectomy, and a few medicines that can assist in reopening the blocked brain vessels or serve as standalone treatments for patients who are not eligible for thrombolysis/thrombectomy therapies. However, the narrow time
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Translating mesenchymal stem cell and their exosome research into GMP compliant advanced therapy products: Promises, problems and prospects Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-14 Chui-Yan Ma, Yuqing Zhai, Chung Tony Li, Jie Liu, Xiang Xu, Hao Chen, Hung-Fat Tse, Qizhou Lian
Mesenchymal stem cells (MSCs) are one of the few stem cell types used in clinical practice as therapeutic agents for immunomodulation and ischemic tissue repair, due to their unique paracrine capacity, multiple differentiation potential, active components in exosomes, and effective mitochondria donation. At present, MSCs derived from tissues such as bone marrow and umbilical cord are widely applied
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Emerging potentials of Fe-based nanomaterials for chiral sensing and imaging Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-12 Njemuwa Nwaji, Juyong Gwak, My-Chi Nguyen, Huu-Quang Nguyen, Hyojin Kang, Youngeun Choi, Youngmi Kim, Hongxia Chen, Jaebeom Lee
Fe-based nanostructures have possessed promising properties that make it suitable for chiral sensing and imaging applications owing to their ultra-small size, non-toxicity, biocompatibility, excellent photostability, tunable fluorescence, and water solubility. This review summarizes the recent research progress in the field of Fe-based nanostructures and places special emphases on their applications
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Artemisinins: Promising drug candidates for the treatment of autoimmune diseases Med. Res. Rev. (IF 13.3) Pub Date : 2023-12-06 Xu Gao, Xian Lin, Qingwen Wang, Jian Chen
Autoimmune diseases are characterized by the immune system's attack on one's own tissues which are highly diverse and diseases differ in severity, causing damage in virtually all human systems including connective tissue (e.g., rheumatoid arthritis), neurological system (e.g., multiple sclerosis) and digestive system (e.g., inflammatory bowel disease). Historically, treatments normally include pain-killing
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LSD1 in drug discovery: From biological function to clinical application Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-28 Hui-Min Liu, Ying Zhou, He-Xiang Chen, Jiang-Wan Wu, Shi-Kun Ji, Liang Shen, Shao-Peng Wang, Hong-Min Liu, Ying Liu, Xing-Jie Dai, Yi-Chao Zheng
Lysine-specific demethylase 1 (LSD1) is a flavin adenine dinucleotide (FAD) dependent monoamine oxidase (MAO) that erases the mono-, and dimethylation of histone 3 lysine 4 (H3K4), resulting in the suppression of target gene transcriptions. Besides, it can also demethylate some nonhistone substrates to regulate their biological functions. As reported, LSD1 is widely upregulated and plays a key role
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Progress in RAS-targeted therapeutic strategies: From small molecule inhibitors to proteolysis targeting chimeras Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-27 Xinchen Lu, Jinmei Jin, Ye Wu, Xiaoxia Liu, Xiaohui Liang, Jiayi Lin, Qingyan Sun, Jiangjiang Qin, Weidong Zhang, Xin Luan
As a widely considerable target in chemical biology and pharmacological research, rat sarcoma (RAS) gene mutations play a critical driving factor in several fatal cancers. Despite the great progress of RAS subtype-specific inhibitors, rapid acquired drug resistance could limit their further clinical applications. Proteolysis targeting chimera (PROTAC) has emerged as a powerful tool to handle “undruggable”
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COVID-19 cooling: Nanostrategies targeting cytokine storm for controlling severe and critical symptoms Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-21 Yu Zheng, Yuke Li, Mao Li, Rujing Wang, Yuhong Jiang, Mengnan Zhao, Jun Lu, Rui Li, Xiaofang Li, Sanjun Shi
As severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) variants continue to wreak havoc worldwide, the “Cytokine Storm” (CS, also known as the inflammatory storm) or Cytokine Release Syndrome has reemerged in the public consciousness. CS is a significant contributor to the deterioration of infected individuals. Therefore, CS control is of great significance for the treatment of critically
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B-cell lymphoma-2 family proteins in the crosshairs: Small molecule inhibitors and activators for cancer therapy Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-20 Qineng Gong, Haojie Wang, Mi Zhou, Lu Zhou, Renxiao Wang, Yan Li
The B-cell lymphoma-2 (BCL-2) family of proteins plays a crucial role in the regulation of apoptosis, offering a dual mechanism for its control. Numerous studies have established a strong association between gene disorders of these proteins and the proliferation of diverse cancer cell types. Consequently, the identification and development of drugs targeting BCL-2 family proteins have emerged as a
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The new direction of drug development: Degradation of undruggable targets through targeting chimera technology Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-20 Xuewu Liang, Hairu Ren, Fengyang Han, Renwen Liang, Jiayan Zhao, Hong Liu
Imbalances in protein and noncoding RNA levels in vivo lead to the occurrence of many diseases. In addition to the use of small molecule inhibitors and agonists to restore these imbalances, recently emerged targeted degradation technologies provide a new direction for disease treatment. Targeted degradation technology directly degrades target proteins or RNA by utilizing the inherent degradation pathways
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Revisiting Aurora Kinase B: A promising therapeutic target for cancer therapy Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-20 Naga Rajiv Lakkaniga, Zhengyu Wang, Yao Xiao, Anupreet Kharbanda, Li Lan, Hong-yu Li
Cancer continues to be a major health concern globally, although the advent of targeted therapy has revolutionized treatment options. Aurora Kinase B is a serine-threonine kinase that has been explored as an oncology therapeutic target for more than two decades. Aurora Kinase B inhibitors show promising biological results in in-vitro and in-vivo experiments. However, there are no inhibitors approved
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Revolutionizing the battle against locally advanced breast cancer: A comprehensive insight into neoadjuvant radiotherapy Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-10 Xiangyi Kong, Jiarui Song, Peng Gao, Ran Gao, Lin Zhang, Yi Fang, Yipeng Wang, Jidong Gao, Jing Wang
Breast cancer (BC) constitutes one of the most pervasive malignancies affecting the female population. Despite progressive improvements in diagnostic and therapeutic technologies, leading to an increased detection of early stage BCs, locally advanced breast cancer (LABC) persists as a significant clinical challenge. Owing to its poor overall survival (OS) rate, elevated recurrence rate, and high potential
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Diverse biological functions of the renin-angiotensin system Med. Res. Rev. (IF 13.3) Pub Date : 2023-11-10 Adithi Rao, Shabir A. Bhat, Tomohiro Shibata, Jorge F. Giani, Florian Rader, Kenneth E. Bernstein, Zakir Khan
The renin-angiotensin system (RAS) has been widely known as a circulating endocrine system involved in the control of blood pressure. However, components of RAS have been found to be localized in rather unexpected sites in the body including the kidneys, brain, bone marrow, immune cells, and reproductive system. These discoveries have led to steady, growing evidence of the existence of independent
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FXR agonists for MASH therapy: Lessons and perspectives from obeticholic acid Med. Res. Rev. (IF 13.3) Pub Date : 2023-10-30 Kang Wang, Yuecan Zhang, Guangji Wang, Haiping Hao, Hong Wang
Nonalcoholic fatty liver disease, also called metabolic dysfunction-associated steatotic liver disease, is the most common liver disease worldwide and has no approved pharmacotherapy. Due to its beneficial effects on metabolic regulation, inflammation suppression, cell death prevention, and fibrogenesis inhibition, farnesoid X receptor (FXR) is widely accepted as a promising therapeutic target for
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Front Cover Image, Volume 43, Issue 6 Med. Res. Rev. (IF 13.3) Pub Date : 2023-10-03 Lijuan Xu, Chunlin Zhuang
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The triangular relationship between traditional Chinese medicines, intestinal flora, and colorectal cancer Med. Res. Rev. (IF 13.3) Pub Date : 2023-09-03 Yuqing Zou, Shuling Wang, Honghua Zhang, Yuxin Gu, Huijuan Chen, Zhihua Huang, Feifei Yang, Wenqi Li, Cheng Chen, Lianhui Men, Qingchang Tian, Tian Xie
Over the past decade, colorectal cancer has reported a higher incidence in younger adults and a lower mortality rate. Recently, the influence of the intestinal flora in the initiation, progression, and treatment of colorectal cancer has been extensively studied, as well as their positive therapeutic impact on inflammation and the cancer microenvironment. Historically, traditional Chinese medicine (TCM)
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Antioxidant peptides, the guardian of life from oxidative stress Med. Res. Rev. (IF 13.3) Pub Date : 2023-08-25 Yiyun Zhu, Kang Wang, Xinyi Jia, Caili Fu, Haining Yu, Yipeng Wang
Reactive oxygen species (ROS) are produced during oxidative metabolism in aerobic organisms. Under normal conditions, ROS production and elimination are in a relatively balanced state. However, under internal or external environmental stress, such as high glucose levels or UV radiation, ROS production can increase significantly, leading to oxidative stress. Excess ROS production not only damages biomolecules
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Rheumatoid arthritis molecular targets and their importance to flavonoid-based therapy Med. Res. Rev. (IF 13.3) Pub Date : 2023-08-21 Ana T. Rufino, Marisa Freitas, Carina Proença, José M. P. Ferreira de Oliveira, Eduarda Fernandes, Daniela Ribeiro
Rheumatoid arthritis (RA) is a progressive, chronic, autoimmune, inflammatory, and systemic condition that primarily affects the synovial joints and adjacent tissues, including bone, muscle, and tendons. The World Health Organization recognizes RA as one of the most prevalent chronic inflammatory diseases. In the last decade, there was an expansion on the available RA therapeutic options which aimed
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Limonoids from neem (Azadirachta indica A. Juss.) are potential anticancer drug candidates Med. Res. Rev. (IF 13.3) Pub Date : 2023-08-17 Siddavaram Nagini, Manikandan Palrasu, Anupam Bishayee
Neem (Azadirachta indica A. Juss.), a versatile evergreen tree recognized for its ethnopharmacological value, is a rich source of limonoids of the triterpenoid class, endowed with potent medicinal properties. Extracts of neem have been documented to display anticancer effects in diverse malignant cell lines as well as in preclinical animal models that has largely been attributed to the constituent
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Communal interaction of glycation and gut microbes in diabetes mellitus, Alzheimer's disease, and Parkinson's disease pathogenesis Med. Res. Rev. (IF 13.3) Pub Date : 2023-08-17 Rahul Shivaji Patil, Rashmi Santosh Tupe
Diabetes and its complications, Alzheimer's disease (AD), and Parkinson's disease (PD) are increasing gradually, reflecting a global threat vis-à-vis expressing the essentiality of a substantial paradigm shift in research and remedial actions. Protein glycation is influenced by several factors, like time, temperature, pH, metal ions, and the half-life of the protein. Surprisingly, most proteins associated
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The entrancing role of dietary polyphenols against the most frequent aging-associated diseases Med. Res. Rev. (IF 13.3) Pub Date : 2023-07-24 Muhammad Ajmal Shah, Hafiza Ishmal Faheem, Ayesha Hamid, Rimsha Yousaf, Muhammad Haris, Uzma Saleem, Ghulam Mujtaba Shah, Reem H. Alhasani, Norah A. Althobaiti, Ifat Alsharif, Ana Sanches Silva
Aging, a fundamental physiological process influenced by innumerable biological and genetic pathways, is an important driving factor for several aging-associated disorders like diabetes mellitus, osteoporosis, cancer, and neurodegenerative diseases including Alzheimer's and Parkinson's diseases. In the modern era, the several mechanisms associated with aging have been deeply studied. Treatment and
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Mechanism and application of β-adrenoceptor blockers in soft tissue wound healing Med. Res. Rev. (IF 13.3) Pub Date : 2023-07-20 Shasha Jia, Xueya Wang, Guowei Wang, Xiaojing Wang
Soft tissue damage stimulates sympathetic nerves to release large amounts of catecholamine hormones which bind to β-adrenergic receptors (β-ARs) on the cell membrane surface. It activates the downstream effector molecules and impairs soft tissue wound healing. β-blockers specifically inhibit β-ARs activation in acute/chronic skin lesions and ulcerative hemangiomas. They also accelerate soft tissue
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CYP1A inhibitors: Recent progress, current challenges, and future perspectives Med. Res. Rev. (IF 13.3) Pub Date : 2023-06-19 Ziru Dai, Yue Wu, Yuan Xiong, Jingjing Wu, Min Wang, Xiao Sun, Xinxin Ding, Ling Yang, Xiaobo Sun, Guangbo Ge
Mammalian cytochrome P450 1A (CYP1A) are key phase I xenobiotic-metabolizing enzymes that play a distinctive role in metabolic activation or metabolic clearance of a variety of procarcinogens, drugs, and endogenous substances. Human CYP1A subfamily contains two members (hCYP1A1 and hCYP1A2), which are known to catalyze the oxidative activation of some environmental procarcinogens into carcinogenic
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Microscopy based methods for characterization, drug delivery, and understanding the dynamics of nanoparticles Med. Res. Rev. (IF 13.3) Pub Date : 2023-06-09 Priyamvada Gupta, Nilesh Rai, Ashish Verma, Vibhav Gautam
Nanomedicine is an emerging field that exploits nanotechnology for the development of novel therapeutic and diagnostic modalities. Researches are been focussed in nanoimaging to develop noninvasive, highly sensitive, and reliable tools for diagnosis and visualization in nanomedical field. The application of nanomedicine in healthcare requires in-depth understanding of their structural, physical and
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Front Cover Image, Volume 43, Issue 4 Med. Res. Rev. (IF 13.3) Pub Date : 2023-06-05 Jessica Merjane, Roger Chung, Rickie Patani, Leszek Lisowski