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Total-body positron emission tomography imaging to accelerate radiotracer discovery pipelines. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-05-15 Andrew Sutherland,Marc R Dweck,David E Newby,Adriana A S Tavares
The development of the first total-body positron emission tomography (PET) clinical scanner is a transformational moment in nuclear medicine, reigniting the field by tackling 2 long-standing and critical barriers to the widespread clinical use of PET: radiation dose and patient throughput. Total-body PET also provides several other unique research and clinical opportunities, including potential to
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Pharmaceutical perspectives on oligonucleotide therapeutics and delivery systems. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-05-14 Dalton W Staller,Flobater I Gawargi,Sanjali S Panigrahi,Paras K Mishra,Ram I Mahato
Gene therapy has a pivotal role in treating new diseases. In addition to the recent mRNA-based COVID-19 vaccines produced by Pfizer-BioNTech and Moderna against severe acute respiratory syndrome corona virus 2, several new gene therapies have recently been approved as effective treatments for fatal genetic disorders such as Duchenne's muscular dystrophy, familial transthyretin amyloidosis, hemophilia
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International Union of Basic and Clinical Pharmacology. CXX. γ-Hydroxybutyrate protein targets in the mammalian brain-beyond classic receptors. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-05-05 Petrine Wellendorph,Stine Juul Gauger,Jens Velde Andersen,Birgitte Rahbek Kornum,Sara M O Solbak,Bente Frølund
γ-Hydroxybutyrate (GHB) is a multifaceted compound with an intriguing, yet undeciphered, pharmacology in the mammalian brain. As a metabolite of GABA it is tightly regulated in terms of synthesis and degradation, and is found in micromolar concentrations in the brain. When GHB is taken in high pharmacological doses, it causes euphoria, relaxation, hypothermia, and sedation, and regulates sleep. Through
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Immunomodulatory effects of calorie restriction and its mimetics: A new potential therapeutic approach for autoimmune diseases. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-04-29 Monokesh K Sen,Eileen Liao,Duan Ni,Anjie Ge,Laura Piccio
Calorie restriction (CR) is a well known intervention associated with multifaceted anti-aging and pro-longevity health benefits. It induces complex physiological cellular and molecular adaptations, resulting in the fine-tuning of metabolic and immune responses in both homeostatic and diseased states. It has thus been extensively studied both preclinically and clinically, uncovering its therapeutic
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Antipsychotics and dietary interventions: Pharmacodynamics, pharmacokinetics, and synergisms in therapy. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-04-29 Cristiana Perrotta,Carla Carnovale,Marco Pozzi,Clara De Palma,Davide Cervia,Maria Nobile,Emilio Clementi
Antipsychotic (AP) medications are the primary treatment for severe mental illnesses, including schizophrenia and severe mood disorders. APs are currently categorized into typical or first-generation APs and atypical or second-generation APs. Although both first-generation and second-generation APs are considered effective in treating psychotic symptoms in severe mental disorders, they differ in their
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Asthma therapeutics: Past, present, and future. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-04-28 Sarah L Rhoads,Lior Seluk,Michael E Wechsler
Asthma is a disease of airway inflammation and bronchial hyperresponsiveness affecting over 300 million individuals worldwide. Although described as early as 460 BC, the recognition of asthma as a disease, and the development and implementation of therapies to control it, emerged in the early 1900s. The subsequent century introduced the utilization of immunotherapy, inhaled medications, and anti-inflammatory
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Innovative therapeutics for renoprotection: Where we are. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-04-25 Monica Cortinovis,Norberto Perico,Giuseppe Remuzzi
Chronic kidney disease (CKD) has become highly prevalent worldwide, with major implications for public health, including increased risk of progression to kidney failure, cardiovascular events, and mortality. Up to a decade ago, renin-angiotensin system inhibitors, that is angiotensin-converting enzyme inhibitors and angiotensin II type 1 receptor blockers, were the only available pharmacological interventions
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5-HT2A receptors: Pharmacology and functional selectivity. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-04-23 Benjamin R Cummins,Gerald B Billac,David E Nichols,Charles D Nichols
Serotonin 5-HT2A receptors were one of the first serotonin receptors to be pharmacologically characterized. In mammals, they are expressed throughout the body in nearly every cell and tissue type, with the highest density in cortical layer V of the brain. They are involved in several aspects of normal physiological processes and behaviors and have been implicated in the etiology of neuropsychiatric
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Corrigendum to "International Union of Basic and Clinical Pharmacology. CXIX. Fundamental insights and clinical relevance regarding the carnitine palmitoyltransferase family of enzymes" [Pharmacological Reviews 77 (2025) 100051]. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-04-22 Rosalía Rodríguez-Rodríguez,Miguel Baena,Sebastián Zagmutt,West Kristian Paraiso,Ana Cristina Reguera,Rut Fadó,Núria Casals
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Cryoelectron microscopy as a tool for illuminating activation mechanisms of human class A orphan G protein-coupled receptors. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-04-02 Isabella C Russell,Dongju Lee,Denise Wootten,Patrick M Sexton,Fabian Bumbak
G protein-coupled receptors (GPCRs) are critically important medicinal targets, and the cryogenic electron microscopy (cryo-EM) revolution is providing novel high-resolution GPCR structures at a rapid pace. Orphan G protein-coupled receptors (oGPCRs) are a group of approximately 100 nonolfactory GPCRs for which endogenous ligands are unknown or not validated. The absence of modulating ligands adds
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Application of Kirchhoff's Laws to pharmacologic and pharmacokinetic analyses. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-03-21 Leslie Z Benet,Jasleen K Sodhi,Markus Ville Tiitto,Yue Xiang
Recently, we introduced a straightforward approach to derive clearance and rate constant equations, without relying on differential equations, utilizing Kirchhoff's Laws, a well known physics methodology used to describe rate-defining processes either in series or parallel. Manuscripts from our laboratory have re-examined published experimental data, demonstrating that the Kirchhoff's Laws methodology
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Activating autophagy to eliminate toxic protein aggregates with small molecules in neurodegenerative diseases. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-03-14 Yuqi Fu,Jin Zhang,Rui Qin,Yueting Ren,Tingting Zhou,Bo Han,Bo Liu
Neurodegenerative diseases (NDs), such as Alzheimer disease, Parkinson disease, Huntington disease, amyotrophic lateral sclerosis, and frontotemporal dementia, are well known to pose formidable challenges for their treatment due to their intricate pathogenesis and substantial variability among patients, including differences in environmental exposures and genetic predispositions. One of the defining
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The microcirculation, the blood-brain barrier, and the neurovascular unit in health and Alzheimer disease: The aberrant pericyte is a central player. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-03-13 Yasmin Amy Divecha,Sanketh Rampes,Sabine Tromp,Sevda T Boyanova,Alice Fleckney,Mehmet Fidanboylu,Sarah Ann Thomas
High fidelity neuronal signaling is enabled by a stable local microenvironment. A high degree of homeostatic regulation of the brain microenvironment, and its separation from the variable and potentially neurotoxic contents of the blood, is brought about by the central nervous system barriers. Evidence from clinical and preclinical studies implicates brain microcirculation, cerebral hypoperfusion,
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Corrigendum to "Toward a paradigm shift: Oral agents and injectable drugs in the future of obesity management" [Pharmacological Reviews 77 (2025) 100008]. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-03-07 Amirhossein Sahebkar,Ali H Eid
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Analyzing lognormal data: A nonmathematical practical guide. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-02-25 Harvey J Motulsky,Trajen Head,Paul B S Clarke
Lognormal distributions are pervasive in pharmacology and elsewhere in biomedical science, arising naturally when biological effects multiply rather than add. Despite their ubiquity in pharmacological parameters (eg, EC50, IC50, Kd, and Km), lognormal distributions are often overlooked or misunderstood, leading to flawed data analysis. This largely nonmathematical review explains why lognormal distributions
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International Union of Basic and Clinical Pharmacology. CXIX. Fundamental insights and clinical relevance regarding the carnitine palmitoyltransferase family of enzymes. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-02-25 Rosalía Rodríguez-Rodríguez,Miguel Baena,Sebastián Zagmutt,West Kristian Paraiso,Ana Cristina Reguera,Rut Fadó,Núria Casals
The carnitine palmitoyltransferases (CPTs) play a key role in controlling the oxidation of long-chain fatty acids and are potential therapeutic targets for diseases with a strong metabolic component, such as obesity, diabetes, and cancer. Four distinct proteins are CPT1A, CPT1B, CPT1C, and CPT2, differing in tissue expression and catalytic activity. CPT1s are finely regulated by malonyl-CoA, a metabolite
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Safety in treatment: Classical pharmacotherapeutics and new avenues for addressing maternal depression and anxiety during pregnancy. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-02-10 Merel Dagher,Catherine M Cahill,Anne M Andrews
We aimed to review clinical research on the safety profiles of antidepressant drugs and associations with maternal depression and neonatal outcomes. We focused on neuroendocrine changes during pregnancy and their effects on antidepressant pharmacokinetics. Pregnancy-induced alterations in drug disposition and metabolism impacting mothers and their fetuses are discussed. We considered evidence for the
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Heme-thiolate monooxygenase cytochrome P450 1B1, an old dog with many new tricks. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-02-05 Jong-Won Kim,Hung-Chun Tung,Bin Yang,Rajat Pant,Xiuchen Guan,Ye Feng,Wen Xie
Cytochrome P450 CYP1B1 is a heme-thiolate monooxygenase traditionally recognized for its xenobiotic functions and extrahepatic expressions. Recent studies have suggested that CYP1B1 is also expressed in hepatic stellate cells, immune cells, endothelial cells, and fibroblasts within the tumor microenvironment, as well as tumor cells themselves. CYP1B1 is responsible for the metabolism of a wide range
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The pharmacologic evolution of anticoagulants: From serendipity to precision therapy. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-01-28 Ali H Eid
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Pharmacotherapeutic opportunities within the Hippo signaling pathway. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-01-23 Ali H Eid
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Disease-modifying pharmacological treatments of type 1 diabetes: Molecular mechanisms, target checkpoints, and possible combinatorial treatments. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-01-23 Liudmila Kosheleva,Daniil Koshelev,Francisco Alejandro Lagunas-Rangel,Shmuel Levit,Alexander Rabinovitch,Helgi B Schiöth
After a century of extensive scientific investigations, there is still no curative or disease-modifying treatment available that can provide long-lasting remission for patients diagnosed with type 1 diabetes (T1D). Although T1D has historically been regarded as a classic autoimmune disorder targeting and destroying pancreatic islet β-cells, significant research has recently demonstrated that β-cells
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Cyclic nucleotide phosphodiesterases as drug targets. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-01-22 Michy P Kelly,Viacheslav O Nikolaev,Leila Gobejishvili,Claire Lugnier,Christian Hesslinger,Peter Nickolaus,David A Kass,Walma Pereira de Vasconcelos,Rodolphe Fischmeister,Stefan Brocke,Paul M Epstein,Gary A Piazza,Adam B Keeton,Gang Zhou,Mohammad Abdel-Halim,Ashraf H Abadi,George S Baillie,Mark A Giembycz,Graeme Bolger,Gretchen Snyder,Kjetil Tasken,Nathaniel E B Saidu,Martina Schmidt,Manuela Zaccolo
Cyclic nucleotides are synthesized by adenylyl and/or guanylyl cyclase, and downstream of this synthesis, the cyclic nucleotide phosphodiesterase families (PDEs) specifically hydrolyze cyclic nucleotides. PDEs control cyclic adenosine-3',5'monophosphate (cAMP) and cyclic guanosine-3',5'-monophosphate (cGMP) intracellular levels by mediating their quick return to the basal steady state levels. This
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Pharmacological strategies to bridge the gap between cancer and cardiovascular therapeutics. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-01-21 Ali H Eid
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From bone sentinel to immune savant: Vitamin D and its receptor's pharmacology. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-01-21 Ali H Eid
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Anticoagulants: From chance discovery to structure-based design. Pharmacol. Rev. (IF 19.3) Pub Date : 2025-01-07 Noel Chan,Stephanie Carlin,Jack Hirsh
Taking a historical perspective, we review the discovery, pharmacology, and clinical evaluation of the old and new anticoagulants that have been approved for clinical use. The drugs are discussed chronologically, starting in the 1880s, and progressing through to 2024. The innovations in technology used to develop novel anticoagulants came in fits and starts and reflected the advances in science and
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Reversing the odds: Advanced and emerging therapeutic strategies for male infertility. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-31 Ali H Eid
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Beyond the stomach stall: Current and emerging pharmacotherapeutics for gastroparesis. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-31 Ali H Eid
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Drugging dancing protein clouds: A close look at disorder-based drug design. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-27 Ali H Eid
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Carbonic anhydrase inhibitors: "Old" drugs with new potential in unexpected areas. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-27 Ali H Eid
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Toward a paradigm shift: Oral agents and injectable drugs in the future of obesity management. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-27 Amirhossein Sahebkar,Ali H Eid
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The Hippo pathway: Organ size control and beyond. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-25 Pengfei Guo,Sicheng Wan,Kun-Liang Guan
The Hippo signaling pathway is a highly conserved signaling network for controlling organ size, tissue homeostasis, and regeneration. It integrates a wide range of intracellular and extracellular signals, such as cellular energy status, cell density, hormonal signals, and mechanical cues, to modulate the activity of YAP/TAZ transcriptional coactivators. A key aspect of Hippo pathway regulation involves
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Vitamin D and its analogs in immune system regulation. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-24 Patricio Artusa,John H White
Vitamin D was discovered as the cure for nutritional rickets, a disease of bone growth arising from inadequate intestinal calcium absorption, and for much of the 20th century, it was studied for its critical role in calcium homeostasis. However, we now recognize that the vitamin D receptor and vitamin D metabolic enzymes are expressed in numerous tissues unrelated to calcium homeostasis. Notably, vitamin
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Shared molecular, cellular, and environmental hallmarks in cardiovascular disease and cancer: Any place for drug repurposing? Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-24 Elisa Avolio,Barbara Bassani,Marzia Campanile,Khaled Ak Mohammed,Paola Muti,Antonino Bruno,Gaia Spinetti,Paolo Madeddu
Cancer and cardiovascular disease (CVD) are the 2 biggest killers worldwide. Specific treatments have been developed for the 2 diseases. However, mutual therapeutic targets should be considered because of the overlap of cellular and molecular mechanisms. Cancer research has grown at a fast pace, leading to an increasing number of new mechanistic treatments. Some of these drugs could prove useful for
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Organic anion transporting polypeptides: Pharmacology, toxicology, structure, and transport mechanisms. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-12-09 Bruno Hagenbuch,Bruno Stieger,Kaspar P Locher
Organic anion transporting polypeptides (OATPs) are membrane proteins that mediate the uptake of a wide range of substrates across the plasma membrane of various cells and tissues. They are classified into 6 subfamilies, OATP1 through OATP6. Humans contain 12 OATPs encoded by 11 solute carrier of organic anion transporting polypeptide (SLCO) genes: OATP1A2, OATP1B1, OATP1B3, the splice variant OATP1B3-1B7
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Neurobiology of the incubation of drug craving: An update. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-29 Jonathan J Chow,Kayla M Pitts,Kenichiro Negishi,Rajtarun Madangopal,Yan Dong,Marina E Wolf,Yavin Shaham
Relapse to drug use is often preceded by drug craving. Clinical observations in the 1980s led clinical investigators to postulate that cue-induced cocaine craving may increase during abstinence. Over 2 decades ago, investigators identified an analogous phenomenon in rats of time-dependent increases in drug-seeking behavior during homecage abstinence and termed it incubation of cocaine craving. In 2011
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Pharmacological treatment for metabolic dysfunction-associated steatotic liver disease and related disorders: Current and emerging therapeutic options. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-22 Xiang Zhang,Harry Cheuk-Hay Lau,Jun Yu
Metabolic dysfunction-associated steatotic liver disease (MASLD; formerly known as nonalcoholic fatty liver disease) is a chronic liver disease affecting over a billion individuals worldwide. MASLD can gradually develop into more severe liver pathologies, including metabolic dysfunction-associated steatohepatitis (MASH), cirrhosis, and liver malignancy. Notably, although being a global health problem
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How to drug a cloud? Targeting intrinsically disordered proteins. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-10-21 Vladimir N Uversky
Biologically active proteins/regions without stable structure (i.e., intrinsically disordered proteins and regions (IDPs and IDRs)) are commonly found in all proteomes. They have a unique functional repertoire that complements the functionalities of ordered proteins and domains. IDPs/IDRs are multifunctional promiscuous binders capable of folding at interaction with specific binding partners on a template-
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Ironing Out the Mechanism of gp130 Signaling Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Essam Eldin A. Osman, Nouri Neamati, Des Richardson
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Intestinal Lymphatic Biology, Drug Delivery, and Therapeutics: Current Status and Future Directions Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Sanjeevini Babu Reddiar, Yining Xie, Mohammad Abdallah, Sifei Han, Luojuan Hu, Orlagh M. Feeney, Gracia Gracia, Abel Anshabo, Zijun Lu, Muhammad Asim Farooq, Ian K. Styles, Anthony R.J. Phillips, John A. Windsor, Christopher J.H. Porter, Enyuan Cao, Natalie L. Trevaskis, Rebecca Ritchie
Historically, the intestinal lymphatics were considered passive conduits for fluids, immune cells, dietary lipids, lipid soluble vitamins, and lipophilic drugs. Studies of intestinal lymphatic drug delivery in the late 20th century focused primarily on the drugs’ physicochemical properties, especially high lipophilicity, that resulted in intestinal lymphatic transport. More recent discoveries have
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Somatostatin: Linking Cognition and Alzheimer Disease to Therapeutic Targeting Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Karin E. Sandoval, Ken A. Witt, Kay Double
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Posttranslational Modifications ofα-Synuclein, Their Therapeutic Potential, and Crosstalk in Health and Neurodegenerative Diseases Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Kambiz Hassanzadeh, Jun Liu, Santhosh Maddila, M. Maral Mouradian, Kay Double
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Bile Acid Signaling in Metabolic and Inflammatory Diseases and Drug Development Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Tiangang Li, John Y.L. Chiang, Grace Guo
Bile acids are the end products of cholesterol catabolism. Hepatic bile acid synthesis accounts for a major fraction of daily cholesterol turnover in humans. Biliary secretion of bile acids generates bile flow and facilitates biliary secretion of lipids, endogenous metabolites, and xenobiotics. In intestine, bile acids facilitate the digestion and absorption of dietary lipids and fat-soluble vitamins
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Drug-Drug Interactions and Synergy: From Pharmacological Models to Clinical Application Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Luigino Calzetta, Clive Page, Maria Gabriella Matera, Mario Cazzola, Paola Rogliani, Martin Michel
This review explores the concept of synergy in pharmacology, emphasizing its importance in optimizing treatment outcomes through the combination of drugs with different mechanisms of action. Synergy, defined as an effect greater than the expected additive effect elicited by individual agents according to specific predictive models, offers a promising approach to enhance therapeutic efficacy while minimizing
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Glatiramer Acetate for the Treatment of Multiple Sclerosis: From First-Generation Therapy to Elucidation of Immunomodulation and Repair Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Rina Aharoni, Ron Milo, Ruth Arnon, Francesca Levi-Schaffer
Multiple sclerosis (MS) is a chronic inflammatory demyelinating and neurodegenerative disease of the central nervous system (CNS), with a putative autoimmune origin and complex pathogenesis. Modification of the natural history of MS by reducing relapses and slowing disability accumulation was first attained in the 1990 s with the development of the first-generation disease-modifying therapies. Glatiramer
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Roles of Individual Human Cytochrome P450 Enzymes in Drug Metabolism Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 F. Peter Guengerich, Ali Eid
Our knowledge of the roles of individual cytochrome P450 (P450) enzymes in drug metabolism has developed considerably in the past 30 years, and this base has been of considerable use in avoiding serious issues with drug interactions and issues due to variations. Some newer approaches are being considered for “phenotyping” metabolism reactions with new drug candidates. Endogenous biomarkers are being
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The 75-Year Anniversary of the Department of Physiology and Pharmacology at Karolinska Institutet—Examples of Recent Accomplishments and Future Perspectives Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Eddie Weitzberg, Magnus Ingelman-Sundberg, Jon O. Lundberg, Göran Engberg, Gunnar Schulte, Volker M. Lauschke, Lynette Daws
Karolinska Institutet is a medical university encompassing 21 departments distributed across three departmental or campus groups. Pharmacological research has a long and successful tradition at the institute with a multitude of seminal findings in the areas of neuronal control of vasodilatation, cardiovascular pharmacology, neuropsychopharmacology, receptor pharmacology, and pharmacogenomics that resulted
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Pharmacological Approaches to Hearing Loss Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Christopher R. Cederroth, Jonas Dyhrfjeld-Johnsen, Barbara Canlon, Gunnar Schulte
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Nitric Oxide Signaling and Regulation in the Cardiovascular System: Recent Advances Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Mattias Carlström, Eddie Weitzberg, Jon O. Lundberg, Gunnar Schulte
Nitric oxide (NO) from endothelial NO synthase importantly contributes to vascular homeostasis. Reduced NO production or increased scavenging during disease conditions with oxidative stress contribute to endothelial dysfunction and NO deficiency. In addition to the classical enzymatic NO synthases (NOS) system, NO can also be generated via the nitrate-nitrite-NO pathway. Dietary and pharmacological
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International Union of Basic and Clinical Pharmacology CXV: The Class F of G Protein-Coupled Receptors Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Gunnar Schulte, Eliot Ohlstein
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Neuroactive Kynurenines as Pharmacological Targets: New Experimental Tools and Exciting Therapeutic Opportunities Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-01 Ana Pocivavsek, Robert Schwarcz, Sophie Erhardt, Gunnar Schulte
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Summing Up Pharmacological Reviews' 75th Anniversary Year and a Look to the Future. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-10-16 Lynette C Daws
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Cytochrome P450 Enzymes: The Old Pandora's Box with an Ever-Growing Hope for Therapy Optimization and Drug Development-Editorial. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-10-16 Ahmed F El-Yazbi,Ali H Eid
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Seventy-Five Years of Interactions: The Department of Physiology and Pharmacology at Karolinska Institutet and Pharmacological Reviews. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-10-16 Gunnar Schulte
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Promising tools for future drug discovery and development in antiarrhythmic therapy. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-22 Gema Mondéjar-Parreño,Patricia Sánchez-Pérez,Francisco Miguel Cruz,José Jalife
Arrhythmia refers to irregularities in the rate and rhythm of the heart, with symptoms spanning from mild palpitations to life-threatening arrhythmias and sudden cardiac death. The complex molecular nature of arrhythmias complicates the selection of appropriate treatment. Current therapies involve the use of antiarrhythmic drugs (class I-IV) with limited efficacy and dangerous side effects and implantable
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Innovation in cancer pharmacotherapy through integrative consideration of germline and tumor genomes. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-22 Roman Tremmel,Daniel Hübschmann,Elke Schaeffeler,Sebastian Pirmann,Stefan Fröhling,Matthias Schwab
Precision cancer medicine is widely established, and numerous molecularly targeted drugs for various tumor entities are approved or are in development. Personalized pharmacotherapy in oncology has so far been based primarily on tumor characteristics, for example, somatic mutations. However, the response to drug treatment also depends on pharmacological processes summarized under the term ADME (absorption
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Biochemistry, pharmacology, and in vivo function of arginases. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-22 Sophia K Heuser,Junjie Li,Silke Pudewell,Anthea LoBue,Zhixin Li,Miriam M Cortese-Krott
The enzyme arginase catalyzes the hydrolysis of l-arginine into l-ornithine and urea. The 2 existing isoforms Arg1 and Arg2 exhibit different cellular localizations and metabolic functions. Arginase activity is crucial for nitrogen detoxification in the urea cycle, synthesis of polyamines, and control of l-arginine bioavailability and nitric oxide (NO) production. Despite significant progress in the
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International Union of Basic and Clinical Pharmacology. CXVIII. Update on the nomenclature for atypical chemokine receptors, including ACKR5. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-22 Andy Chevigné,Daniel F Legler,Antal Rot,Silvano Sozzani,Martyna Szpakowska,Marcus Thelen
Chemokines signal through classical G protein-coupled receptors to induce cell migration during development, immune homeostasis, and multiple diseases. Over the last decade, a subfamily of atypical chemokine receptors (ACKRs) was delineated from G protein-coupled receptors based on their inability to trigger conventional G protein signaling or mediate cell migration in response to chemokines. These
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Ferroptosis and pathogenesis of neuritic plaques in Alzheimer disease. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-22 Wolfgang J Streit,Leah Phan,Ingo Bechmann
Neuritic plaques are pathognomonic and terminal lesions of Alzheimer disease (AD). They embody AD pathogenesis because they harbor in one space critical pathologic features of the disease: amyloid deposits, neurofibrillary degeneration, neuroinflammation, and iron accumulation. Neuritic plaques are thought to arise from the conversion of diffuse extracellular deposits of amyloid-β protein (Aβ), and
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Therapeutic advantage of combinatorial chimeric antigen receptor T cell and chemotherapies. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-11-22 Meghan B Ward,Amber B Jones,Giedre Krenciute
Chimeric antigen receptor (CAR) T cell therapies have transformed outcomes for many patients with hematological malignancies. However, some patients do not respond to CAR T cell treatment, and adapting CAR T cells for treatment of solid and brain tumors has been met with many challenges, including a hostile tumor microenvironment and poor CAR T cell persistence. Thus, it is unlikely that CAR T cell
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Bioactives from marine resources as natural health products: A review. Pharmacol. Rev. (IF 19.3) Pub Date : 2024-10-07 Sarusha Santhiravel,Deepika Dave,Fereidoon Shahidi
The oceans are a rich source of a myriad of structurally different and unique natural products that are mainly found in invertebrates with potential applications in different disciplines. Microbial infection and cancer are the leading causes of death worldwide. Discovery of new sources of therapy for microbial infections is an urgent requirement due to the emergence of pathogenic microorganisms that