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Extracellular Vesicle Heterogeneity and Its Impact for Regenerative Medicine Applications Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 van de Wakker, S. I., Meijers, F. M., Sluijter, J. P. G., Vader, P.
Extracellular vesicles (EVs) are cell-derived membrane-enclosed particles that are involved in physiologic and pathologic processes. EVs are increasingly being studied for therapeutic applications in the field of regenerative medicine. Therapeutic application of stem cell–derived EVs has shown great potential to stimulate tissue repair. However, the exact mechanisms through which they induce this effect
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Hepatic Bile Formation: Developing a New Paradigm Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 Javitt, N. B.
In 1959, Ivar Sperber contrasted bile formation with that of urine and proposed that water flow into the canalicular conduit is in response to an osmotic, not a hydrostatic, gradient. Early attempts to support the hypothesis using a bile acid, sodium taurocholate, and the hormone secretin to stimulate bile flow led to conflicting data and a moratorium on attempts to further develop the initial proposal
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The Myc Family and the Metastasis Suppressor NDRG1: Targeting Key Molecular Interactions with Innovative Therapeutics Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 Deng, Z., Richardson, D. R.
Cancer is a leading cause of death worldwide, resulting in ~10 million deaths in 2020. Major oncogenic effectors are the Myc proto-oncogene family, which consists of three members including c-Myc, N-Myc, and L-Myc. As a pertinent example of the role of the Myc family in tumorigenesis, amplification of MYCN in childhood neuroblastoma strongly correlates with poor patient prognosis. Complexes between
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Paradoxes of Cellular SUMOylation Regulation: A Role of Biomolecular Condensates? Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 Cheng, X., Yang, W., Lin, W., Mei, F.
Protein SUMOylation is a major post-translational modification essential for maintaining cellular homeostasis. SUMOylation has long been associated with stress responses as a diverse array of cellular stress signals are known to trigger rapid alternations in global protein SUMOylation. In addition, while there are large families of ubiquitination enzymes, all small ubiquitin-like modifiers (SUMOs)
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Pharmacological Regulation of Endoplasmic Reticulum Structure and Calcium Dynamics: Importance for Neurodegenerative Diseases Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 Parkkinen, I., Their, A., Asghar, M. Y., Sree, S., Jokitalo, E., Airavaara, M.
The endoplasmic reticulum (ER) is the largest organelle of the cell, composed of a continuous network of sheets and tubules, and is involved in protein, calcium (Ca2+), and lipid homeostasis. In neurons, the ER extends throughout the cell, both somal and axodendritic compartments, and is highly important for neuronal functions. A third of the proteome of a cell, secreted and membrane-bound proteins
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Goods and Bads of the Endocannabinoid System as a Therapeutic Target: Lessons Learned after 30 Years Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 Maccarrone, M., Di Marzo, V., Gertsch, J., Grether, U., Howlett, A. C., Hua, T., Makriyannis, A., Piomelli, D., Ueda, N., van der Stelt, M.
The cannabis derivative marijuana is the most widely used recreational drug in the Western world and is consumed by an estimated 83 million individuals (~3% of the world population). In recent years, there has been a marked transformation in society regarding the risk perception of cannabis, driven by its legalization and medical use in many states in the United States and worldwide. Compelling research
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{beta}-Arrestins: Structure, Function, Physiology, and Pharmacological Perspectives Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 Wess, J., Oteng, A.-B., Rivera-Gonzalez, O., Gurevich, E. V., Gurevich, V. V.
The two β-arrestins, β-arrestin-1 and -2 (systematic names: arrestin-2 and -3, respectively), are multifunctional intracellular proteins that regulate the activity of a very large number of cellular signaling pathways and physiologic functions. The two proteins were discovered for their ability to disrupt signaling via G protein-coupled receptors (GPCRs) via binding to the activated receptors. However
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ABCB1 and ABCG2 Regulation at the Blood-Brain Barrier: Potential New Targets to Improve Brain Drug Delivery Pharmacol. Rev. (IF 21.1) Pub Date : 2023-08-14 Schulz, J. A., Hartz, A. M. S., Bauer, B.
The drug efflux transporters ABCB1 and ABCG2 at the blood-brain barrier limit the delivery of drugs into the brain. Strategies to overcome ABCB1/ABCG2 have been largely unsuccessful, which poses a tremendous clinical problem to successfully treat central nervous system (CNS) diseases. Understanding basic transporter biology, including intracellular regulation mechanisms that control these transporters
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Optical approaches for investigating neuromodulation and G Protein-Coupled Receptor signaling. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-07-10 David J Marcus,Michael R Bruchas
Despite that fact roughly 40% of all FDA approved pharmacological therapeutics target G Protein-Coupled Receptors (GPCRs), there remains a noted gap in our understanding of the physiological and functional role of these receptors at the systems level. While heterologous expression systems and in vitro assays have revealed a tremendous amount about GPCR signaling cascades, how these cascades interact
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Targeting Epidermal Growth Factor Receptor for Cancer Treatment: Abolishing both Kinase-Dependent and Kinase-Independent Functions of the Receptor. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-06-20 Yuesheng Zhang
Epidermal growth factor receptor (EGFR), a receptor tyrosine kinase, is activated by ligand binding, overexpression, or mutation. It is well known for its tyrosine kinase-dependent oncogenic activities in a variety of human cancers. A large number of EGFR inhibitors have been developed for cancer treatment, including monoclonal antibodies, tyrosine kinase inhibitors, and a vaccine. The EGFR inhibitors
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Effects of medications on heat loss capacity in chronic disease patients: health implications amidst global warming. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-06-16 Jericho Wee,Xiang Ren Tan,Samuel H Gunther,Mohammed Ihsan,Melvin Khee Shing Leow,Doreen Su-Yin Tan,Johan G Eriksson,Jason Kai Wei Lee
Pharmacological agents used to treat or manage diseases can modify the level of heat strain experienced by chronically ill and elderly patients via different mechanistic pathways. Human thermoregulation is a crucial homeostatic process that maintains body temperature within a narrow range during heat stress through dry (i.e., increasing skin blood flow) and evaporative (i.e., sweating) heat loss, as
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Oxycodone: A Current Perspective on its Pharmacology, Abuse and Pharmacotherapeutic Developments. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-06-15 James E Barrett,Aryan Shekarabi,Saadet Inan
ABSTRACT Oxycodone, a semi-synthetic derivative of naturally occurring thebaine, an opioid alkaloid, has been available for over 100 years. Although thebaine cannot be used therapeutically due to the occurrence of convulsions at higher doses, it has been converted to a number of other widely used compounds that include naloxone, naltrexone, buprenorphine, and oxycodone. Despite the early identification
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Pharmacogenomics: Driving Personalized Medicine Pharmacol. Rev. (IF 21.1) Pub Date : 2023-07-01 Wolfgang Sadee, Danxin Wang, Katherine Hartmann, Amanda Ewart Toland, Hyunyoung Jeong
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Potassium Channels in Parkinson’s Disease: Potential Roles in Its Pathogenesis and Innovative Molecular Targets for Treatment Pharmacol. Rev. (IF 21.1) Pub Date : 2023-07-01 Xiaoyi Chen, Yunjiang Feng, Ronald J. Quinn, Dean L. Pountney, Des R. Richardson, George D. Mellick, Linlin Ma, Habibeh Khoshbouei
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Advances in Nanozymes as a Paradigm for Viral Diagnostics and Therapy Pharmacol. Rev. (IF 21.1) Pub Date : 2023-07-01 Garima Sharma, Srijan Chatterjee, Chiranjib Chakraborty, Jin-Chul Kim, Martin Michel
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Review of Natural Language Processing in Pharmacology Pharmacol. Rev. (IF 21.1) Pub Date : 2023-07-01 Dimitar Trajanov, Vangel Trajkovski, Makedonka Dimitrieva, Jovana Dobreva, Milos Jovanovik, Matej Klemen, Aleš Žagar, Marko Robnik-Šikonja, Habibeh Khoshbouei
Natural language processing (NLP) is an area of artificial intelligence that applies information technologies to process the human language, understand it to a certain degree, and use it in various applications. This area has rapidly developed in the past few years and now employs modern variants of deep neural networks to extract relevant patterns from large text corpora. The main objective of this
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Cellular Senescence: From Mechanisms to Current Biomarkers and Senotherapies Pharmacol. Rev. (IF 21.1) Pub Date : 2023-07-01 Vasco Lucas, Cláudia Cavadas, Célia Alexandra Aveleira, Vivian Hook
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Current and Emerging Pharmacological Targets and Treatments of Urinary Incontinence and Related Disorders Pharmacol. Rev. (IF 21.1) Pub Date : 2023-07-01 Martin C. Michel, Linda Cardozo, Christopher J. Chermansky, Francisco Cruz, Yasuhiko Igawa, Kyu-Sung Lee, Arun Sahai, Alan J. Wein, Karl-Erik Andersson, Lynette Daws
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Lymphocyte depleting and modulating therapies for chronic lung allograft dysfunction. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-06-09 Saskia Bos,Pauline Pradère,Hanne Beeckmans,Andrea Zajacova,Bart M Vanaudenaerde,Andrew J Fisher,Robin Vos
Chronic lung rejection, also called chronic lung allograft dysfunction (CLAD), remains the major hurdle limiting long-term survival after lung transplantation and limited therapeutic options are available to slow the progressive decline in lung function. Most interventions are only temporarily effective in stabilising the loss of or modestly improving lung function, with disease progression resuming
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Extracellular vesicle heterogeneity and its impact for regenerative medicine applications. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-06-06 Simonides Immanuel van de Wakker,Fleur Michelle Meijers,Joost Petrus Gerardus Sluijter,Pieter Vader
Extracellular vesicles (EVs) are cell-derived membrane enclosed particles that are involved in physiological and pathological processes. EVs are increasingly being studied for therapeutic applications in the field of regenerative medicine. Therapeutic application of stem cell-derived EVs has shown great potential to stimulate tissue repair. However, the exact mechanisms through which they induce this
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The Myc Family and the Metastasis Suppressor NDRG1: Targeting Key Molecular Interactions with Innovative Therapeutics. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-06-06 Zhao Deng,Des R Richardson
Cancer is a leading cause of death worldwide resulting in ~10 million deaths in 2020. Major oncogenic effectors are the Myc proto-oncogene family that consists of three members including c-Myc, N-Myc, and L-Myc. As a pertinent example of the role of the Myc family in tumorigenesis, amplification of MYCN in childhood neuroblastoma strongly correlates with poor patient prognosis. Complexes between Myc
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Paradoxes of cellular SUMOylation regulation: a role of biomolecular condensates? Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-03 Xiaodong Cheng,Wenli Yang,Wei Lin,Fang Mei
Protein SUMOylation is a major post-translational modification important for maintaining cellular homeostasis. SUMOylation has long been associated with stress responses as a diverse array of cellular stress signals are known to trigger rapid alternations in global protein SUMOylation. In addition, while there are large families of ubiquitination enzymes, all SUMOs are conjugated by a set of enzymatic
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Pharmacological regulation of endoplasmic reticulum structure and calcium dynamics: importance for neurodegenerative diseases. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-01 Ilmari Parkkinen,Anna Their,Muhammad Yasir Asghar,Sreesha Sree,Eija Jokitalo,Mikko Airavaara
The endoplasmic reticulum (ER) is the largest organelle of the cell, composed of a continuous network of sheets and tubules, and is involved in protein, calcium (Ca2+) and lipid homeostasis. In neurons, the ER extends throughout the cell, both somal and axodendritic compartments, and is highly important for neuronal functions. A third of the proteome of a cell, secreted and membrane-bound proteins
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Understanding the Neural Mechanisms of General Anesthesia from Interaction with Sleep–Wake State: A Decade of Discovery Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-01 Wei-Wei Bao, Shan Jiang, Wei-Min Qu, Wen-Xian Li, Chang-Hong Miao, Zhi-Li Huang, Lynette Daws
The development of cutting-edge techniques to study specific brain regions and neural circuits that regulate sleep–wake brain states and general anesthesia (GA), has increased our understanding of these states that exhibit similar neurophysiologic traits. This review summarizes current knowledge focusing on cell subtypes and neural circuits that control wakefulness, rapid eye movement (REM) sleep,
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Sulfotransferase 2B1b, Sterol Sulfonation, and Disease Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-01 Ian Cook, Thomas S. Leyh, Stephen Alexander
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Pharmacological Inhibition of the NLRP3 Inflammasome: Structure, Molecular Activation, and Inhibitor-NLRP3 Interaction Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-01 Qiang Ma, John Schuetz
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Time to Change: A Systems Pharmacology Approach to Disentangle Mechanisms of Drug-Induced Mitochondrial Toxicity Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-01 Charlotte A. Hoogstraten, Jonathan J. Lyon, Jan A.M. Smeitink, Frans G.M. Russel, Tom J.J. Schirris, John Schuetz
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Turn On, Tune In, Turnover! Target Biology Impacts In Vivo Potency, Efficacy, and Clearance Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-01 Johan Gabrielsson, Stephan Hjorth, Paul Insel
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G Protein-Coupled Receptor Pharmacology—Insights from Mass Spectrometry Pharmacol. Rev. (IF 21.1) Pub Date : 2023-05-01 Hsin-Yung Yen, Ali Jazayeri, Carol V. Robinson, Gunnar Schulte
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β- Arrestins: Structure, Function, Physiology, and Pharmacological Perspectives. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-04-07 Jürgen Wess,Antwi-Boasiako Oteng,Osvaldo Rivera-Gonzalez,Eugenia V Gurevich,Vsevolod V Gurevich
The two beta-arrestins, beta-arrestin-1 and -2 (systematic names: arrestin-2 and -3, respectively), are multifunctional intracellular proteins that regulate the activity of a very large number of cellular signaling pathways and physiological functions. The two proteins were discovered for their ability to disrupt signaling via G protein-coupled receptors (GPCRs) via binding to the activated receptors
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ABCB1 and ABCG2 Regulation at the Blood-Brain Barrier: Potential New Targets to Improve Brain Drug Delivery. Pharmacol. Rev. (IF 21.1) Pub Date : 2023-03-27 Julia A Schulz,Anika M S Hartz,Björn Bauer
The drug efflux transporters ABCB1 and ABCG2 at the blood-brain barrier limit the delivery of drugs into the brain. Strategies to overcome ABCB1/ABCG2 have been largely unsuccessful, which poses a tremendous clinical problem to successfully treat CNS diseases. Understanding basic transporter biology, including intracellular regulation mechanisms that control these transporters, is critical to solve
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Pharmacology of Heparin and Related Drugs: An Update Pharmacol. Rev. (IF 21.1) Pub Date : 2023-03-01 John Hogwood, Barbara Mulloy, Rebeca Lever, Elaine Gray, Clive P. Page, Lynette Daws
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Targeting Persistent Changes in Neuroimmune and Epigenetic Signaling in Adolescent Drinking to Treat Alcohol Use Disorder in Adulthood Pharmacol. Rev. (IF 21.1) Pub Date : 2023-03-01 Fulton T. Crews, Leon G. Coleman, Victoria A. Macht, Ryan P. Vetreno, Robert Dantzer
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Newly Developed Targeted Therapies Against the Androgen Receptor in Triple-Negative Breast Cancer: A Review Pharmacol. Rev. (IF 21.1) Pub Date : 2023-03-01 Edris Choupani, Mohammad Mahmoudi Gomari, Saeed Zanganeh, Sherko Nasseri, Kaveh Haji-allahverdipoor, Neda Rostami, Yaeren Hernandez, Safa Najafi, Neda Saraygord-Afshari, Arshad Hosseini, Michael Gottesman
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Molecular Tweezers: Supramolecular Hosts with Broad-Spectrum Biological Applications Pharmacol. Rev. (IF 21.1) Pub Date : 2023-03-01 Hedieh Shahpasand-Kroner, Ibrar Siddique, Ravinder Malik, Gabriel R. Linares, Magdalena I. Ivanova, Justin Ichida, Tatjana Weil, Jan Münch, Elsa Sanchez-Garcia, Frank-Gerrit Klärner, Thomas Schrader, Gal Bitan, Habibeh Khoshbouei
Lysine-selective molecular tweezers (MTs) are supramolecular host molecules displaying a remarkably broad spectrum of biologic activities. MTs act as inhibitors of the self-assembly and toxicity of amyloidogenic proteins using a unique mechanism. They destroy viral membranes and inhibit infection by enveloped viruses, such as HIV-1 and SARS-CoV-2, by mechanisms unrelated to their action on protein
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Pharmacological Targeting of Mitochondria in Diabetic Kidney Disease Pharmacol. Rev. (IF 21.1) Pub Date : 2023-02-13 Cleveland, K. H., Schnellmann, R. G.
Diabetic kidney disease (DKD) is the leading cause of end-stage renal disease (ESRD) in the United States and many other countries. DKD occurs through a variety of pathogenic processes that are in part driven by hyperglycemia and glomerular hypertension, leading to gradual loss of kidney function and eventually progressing to ESRD. In type 2 diabetes, chronic hyperglycemia and glomerular hyperfiltration
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Sex/Gender Differences in the Time-Course for the Development of Substance Use Disorder: A Focus on the Telescoping Effect Pharmacol. Rev. (IF 21.1) Pub Date : 2023-03-01 Eleanor Blair Towers, Ivy L. Williams, Emaan I. Qillawala, Emilie F. Rissman, Wendy J. Lynch, Michael Nader
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Interaction of Cardiovascular Nonmodifiable Risk Factors, Comorbidities and Comedications With Ischemia/Reperfusion Injury and Cardioprotection by Pharmacological Treatments and Ischemic Conditioning Pharmacol. Rev. (IF 21.1) Pub Date : 2023-01-01 Péter Ferdinandy, Ioanna Andreadou, Gary F. Baxter, Hans Erik Bøtker, Sean M. Davidson, Dobromir Dobrev, Bernard J. Gersh, Gerd Heusch, Sandrine Lecour, Marisol Ruiz-Meana, Coert J. Zuurbier, Derek J. Hausenloy, Rainer Schulz, Finn Olav Levy
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Dopamine, Immunity, and Disease Pharmacol. Rev. (IF 21.1) Pub Date : 2023-01-01 Breana Channer, Stephanie M. Matt, Emily A. Nickoloff-Bybel, Vasiliki Pappa, Yash Agarwal, Jason Wickman, Peter J. Gaskill, Habibeh Khoshbouei
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Pharmacological Modulation of the Crosstalk between Aberrant Janus Kinase Signaling and Epigenetic Modifiers of the Histone Deacetylase Family to Treat Cancer Pharmacol. Rev. (IF 21.1) Pub Date : 2023-01-01 Al-Hassan M. Mustafa, Oliver H. Krämer, Lynette Daws
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Elucidating the Interactome of G Protein-Coupled Receptors and Receptor Activity-Modifying Proteins Pharmacol. Rev. (IF 21.1) Pub Date : 2023-01-01 Ilana B. Kotliar, Emily Lorenzen, Jochen M. Schwenk, Debbie L. Hay, Thomas P. Sakmar, Gunnar Schulte
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Pharmacological Reviews Announces Inaugural Social Media Ambassadors. Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Lynette C Daws
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Animal Behavior in Psychedelic Research Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Anna U. Odland, Jesper L. Kristensen, Jesper T. Andreasen, Lynette Daws
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Opportunities for Nitric Oxide in Potentiating Cancer Immunotherapy Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Jihoon Kim, Susan N. Thomas, Martin Michel
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Looking Under the Lamppost: The Search for New Cancer Targets in the Human Kinome Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Mireia Sueca-Comes, Elena Cristina Rusu, Anna M. Grabowska, David O. Bates, Stephen Alexander
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The Angiotensin AT2Receptor: From a Binding Site to a Novel Therapeutic Target Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 U. Muscha Steckelings, Robert E. Widdop, Edward D. Sturrock, Lizelle Lubbe, Tahir Hussain, Elena Kaschina, Thomas Unger, Anders Hallberg, Robert M. Carey, Colin Sumners, Rhian Touyz
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Therapeutic Potential of Targeting Regulated Intramembrane Proteolysis Mechanisms of Voltage-Gated Ion Channel Subunits and Cell Adhesion Molecules Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Samantha L. Hodges, Alexandra A. Bouza, Lori L. Isom, Lynette Daws
Several integral membrane proteins undergo regulated intramembrane proteolysis (RIP), a tightly controlled process through which cells transmit information across and between intracellular compartments. RIP generates biologically active peptides by a series of proteolytic cleavage events carried out by two primary groups of enzymes: sheddases and intramembrane-cleaving proteases (iCLiPs). Following
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Self-Entropic Broadening Theory: Toward a New Understanding of Self and Behavior Change Informed by Psychedelics and Psychosis Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Haley Maria Dourron, Camilla Strauss, Peter S. Hendricks, Eric Barker
The extremes of human experiences, such as those occasioned by classic psychedelics and psychosis, provide a rich contrast for understanding how components of these experiences impact well-being. In recent years, research has suggested that classic psychedelics display the potential to promote positive enduring psychologic and behavioral changes in clinical and nonclinical populations. Paradoxically
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Exploring Intestinal Surface Receptors in Oral Nanoinsulin Delivery Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Carlynne Choy, Lee Yong Lim, Lai Wah Chan, Zhixiang Cui, Shirui Mao, Tin Wui Wong, Clive Page
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Positive Allosteric Modulators of Glycine Receptors and Their Potential Use in Pain Therapies Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Casey I. Gallagher, Damien A. Ha, Robert J. Harvey, Robert J. Vandenberg, Lynette Daws
Glycine receptors are ligand-gated ion channels that mediate synaptic inhibition throughout the mammalian spinal cord, brainstem, and higher brain regions. They have recently emerged as promising targets for novel pain therapies due to their ability to produce antinociception by inhibiting nociceptive signals within the dorsal horn of the spinal cord. This has greatly enhanced the interest in developing
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Changing Cerebral Blood Flow, Glucose Metabolism, and Dopamine Binding Through Transcranial Magnetic Stimulation: A Systematic Review of Transcranial Magnetic Stimulation-Positron Emission Tomography Literature Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Kaitlin R. Kinney, Colleen A. Hanlon, Michael Nader
Transcranial magnetic stimulation (TMS) is a noninvasive neuromodulation tool currently used as a treatment in multiple psychiatric and neurologic disorders. Despite its widespread use, we have an incomplete understanding of the way in which acute and chronic sessions of TMS affect various neural and vascular systems. This systematic review summarizes the state of our knowledge regarding the effects
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Neural Mechanisms and Psychology of Psychedelic Ego Dissolution Pharmacol. Rev. (IF 21.1) Pub Date : 2022-10-01 Devon Stoliker, Gary F. Egan, Karl J. Friston, Adeel Razi, Eric Barker
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Carbon Monoxide Signaling: Examining Its Engagement with Various Molecular Targets in the Context of Binding Affinity, Concentration, and Biologic Response Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Zhengnan Yuan, Ladie Kimberly De La Cruz, Xiaoxiao Yang, Binghe Wang, Qiang Ma
Carbon monoxide (CO) has been firmly established as an endogenous signaling molecule with a variety of pathophysiological and pharmacological functions, including immunomodulation, organ protection, and circadian clock regulation, among many others. In terms of its molecular mechanism(s) of action, CO is known to bind to a large number of hemoproteins with at least 25 identified targets, including
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ATP and Adenosine Metabolism in Cancer: Exploitation for Therapeutic Gain Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Gennady G. Yegutkin, Detlev Boison, Stephen Alexander
Adenosine is an evolutionary ancient metabolic regulator linking energy state to physiologic processes, including immunomodulation and cell proliferation. Tumors create an adenosine-rich immunosuppressive microenvironment through the increased release of ATP from dying and stressed cells and its ectoenzymatic conversion into adenosine. Therefore, the adenosine pathway becomes an important therapeutic
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Quantitative Proteomics in Translational Absorption, Distribution, Metabolism, and Excretion and Precision Medicine Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Deepak Ahire, Laken Kruger, Sheena Sharma, Vijaya Saradhi Mettu, Abdul Basit, Bhagwat Prasad, Charles France
A reliable translation of in vitro and preclinical data on drug absorption, distribution, metabolism, and excretion (ADME) to humans is important for safe and effective drug development. Precision medicine that is expected to provide the right clinical dose for the right patient at the right time requires a comprehensive understanding of population factors affecting drug disposition and response. Characterization
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Matrix Metalloproteinases: From Molecular Mechanisms to Physiology, Pathophysiology, and Pharmacology Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Luiz G.N. de Almeida, Hayley Thode, Yekta Eslambolchi, Sameeksha Chopra, Daniel Young, Sean Gill, Laurent Devel, Antoine Dufour, Gunnar Schulte
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New Technologies Bloom Together for Bettering Cancer Drug Conjugates Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Yiming Jin, Shahab Edalatian Zakeri, Raman Bahal, Andrew J. Wiemer, Eric Barker
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Mass Spectrometry Approaches Empowering Neuropeptide Discovery and Therapeutics Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Krishna D. B. Anapindi, Elena V. Romanova, James W. Checco, Jonathan V. Sweedler, Vivian Hook
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Allosteric Modulators of Metabotropic Glutamate Receptors as Novel Therapeutics for Neuropsychiatric Disease Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Deborah J. Luessen, P. Jeffrey Conn, Lynette Daws
Metabotropic glutamate (mGlu) receptors, a family of G-protein-coupled receptors, have been identified as novel therapeutic targets based on extensive research supporting their diverse contributions to cell signaling and physiology throughout the nervous system and important roles in regulating complex behaviors, such as cognition, reward, and movement. Thus, targeting mGlu receptors may be a promising
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Cathepsin B Gene Knockout Improves Behavioral Deficits and Reduces Pathology in Models of Neurologic Disorders Pharmacol. Rev. (IF 21.1) Pub Date : 2022-07-01 Gregory Hook, Thomas Reinheckel, Junjun Ni, Zhou Wu, Mark Kindy, Christoph Peters, Vivian Hook, Eric Barker