journal
https://read.qxmd.com/read/38697854/mdm2-inhibitors-for-cancer-therapy-the-past-present-and-future
#21
REVIEW
Wei Wang, Najah Albadari, Yi Du, Josef F Fowler, Hannah T Sang, Wa Xian, Frank McKeon, Wei Li, Jia Zhou, Ruiwen Zhang
Since its discovery over 35 years ago, MDM2 has emerged as an attractive target for the development of cancer therapy. MDM2's activities extend from carcinogenesis to immunity to the response to various cancer therapies. Since the report of the first MDM2 inhibitor more than 30 years ago, various approaches to inhibit MDM2 have been attempted, with hundreds of small-molecule inhibitors evaluated in preclinical studies and numerous molecules tested in clinical trials. Although many MDM2 inhibitors and degraders have been evaluated in clinical trials, there is currently no Food and Drug Administration (FDA)-approved MDM2 inhibitor on the market...
May 2, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38697853/a-chance-to-grow-and-excel-as-an-associate-editor-of-pharmacological-reviews-editorial
#22
EDITORIAL
Ali H Eid
No abstract text is available yet for this article.
May 2, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38622001/precision-medicine-in-rheumatic-diseases-unlocking-the-potential-of-antibody-drug-conjugates
#23
JOURNAL ARTICLE
Zhiwen Huang, Zachary Braunstein, Jun Chen, Yingying Wei, Xiaoquan Rao, Lingli Dong, Jixin Zhong
In the era of precision medicine, Antibody-Drug Conjugates (ADCs) have emerged as a cutting-edge therapeutic strategy. These innovative compounds combine the precision of monoclonal antibodies with the potent cell-killing or immune-modulating abilities of attached drug payloads. This unique strategy not only reduces off-target toxicity but also enhances the therapeutic effectiveness of drugs. Beyond their well-established role in oncology, ADCs are now showing promising potential in addressing the unmet needs in the therapeutics of rheumatic diseases...
April 15, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38351075/emergence-of-extracellular-vesicles-as-liquid-biopsy-for-neurological-disorders-boom-or-bust
#24
REVIEW
Ashish Kumar, Michael A Nader, Gagan Deep
Extracellular vesicles (EVs) have emerged as an attractive liquid biopsy approach in the diagnosis and prognosis of multiple diseases and disorders. The feasibility of enriching specific subpopulations of EVs from biofluids based on their unique surface markers has opened novel opportunities to gain molecular insight from various tissues and organs, including the brain. Over the past decade, EVs in bodily fluids have been extensively studied for biomarkers associated with various neurological disorders, such as Alzheimer's disease, Parkinson's disease, schizophrenia, bipolar disorder, major depressive disorders, substance use disorders, human immunodeficiency virus-associated neurocognitive disorder, and cancer/treatment-induced neurodegeneration...
February 13, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38351074/the-arylamine-n-acetyltransferases-as-therapeutic-targets-in-metabolic-diseases-associated-with-mitochondrial-dysfunction
#25
REVIEW
Chandra Choudhury, Melinder K Gill, Courtney E McAleese, Neville J Butcher, Shyuan T Ngo, Frederik J Steyn, Rodney F Minchin
In humans, there are two arylamine N-acetyltransferase genes that encode functional enzymes ( NAT1 and NAT2 ) as well as one pseudogene, all of which are located together on chromosome 8. Although they were first identified by their role in the acetylation of drugs and other xenobiotics, recent studies have shown strong associations for both enzymes in a variety of diseases, including cancer, cardiovascular disease, and diabetes. There is growing evidence that this association may be causal. Consistently, NAT1 and NAT2 are shown to be required for healthy mitochondria...
February 13, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38351073/a-25-year-journey-as-author-and-associate-editor-of-pharmacological-reviews-editorial
#26
EDITORIAL
Martin C Michel
No abstract text is available yet for this article.
February 13, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38351072/protecting-human-and-animal-health-the-road-from-animal-models-to-new-approach-methods
#27
REVIEW
Barbara L F Kaplan, Alan M Hoberman, William Slikker, Mary Alice Smith, Emanuela Corsini, Thomas B Knudsen, M Sue Marty, Sonya K Sobrian, Suzanne C Fitzpatrick, Marcia H Ratner, Donna L Mendrick
Animals and animal models have been invaluable for our current understanding of human and animal biology, including physiology, pharmacology, biochemistry, and disease pathology. However, there are increasing concerns with continued use of animals in basic biomedical, pharmacological, and regulatory research to provide safety assessments for drugs and chemicals. There are concerns that animals do not provide sufficient information on toxicity and/or efficacy to protect the target population, so scientists are utilizing the principles of replacement, reduction, and refinement (the 3Rs) and increasing the development and application of new approach methods (NAMs)...
February 13, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38351071/the-role-of-g-protein-coupled-receptors-and-receptor-kinases-in-pancreatic-%C3%AE-cell-function-and-diabetes
#28
REVIEW
Matthew J Varney, Jeffrey L Benovic
Type 2 diabetes (T2D) mellitus has emerged as a major global health concern that has accelerated in recent years due to poor diet and lifestyle. Afflicted individuals have high blood glucose levels that stem from the inability of the pancreas to make enough insulin to meet demand. Although medication can help to maintain normal blood glucose levels in individuals with chronic disease, many of these medicines are outdated, have severe side effects, and often become less efficacious over time, necessitating the need for insulin therapy...
February 13, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38351070/leveraging-lymphatic-system-targeting-in-systemic-lupus-erythematosus-for-improved-clinical-outcomes
#29
REVIEW
K T Babalola, M Arora, R Ganugula, S K Agarwal, C Mohan, M N V Ravi Kumar
The role of advanced drug delivery strategies in drug repositioning and minimizing drug attrition rates, when applied early in drug discovery, is poised to increase the translational impact of various therapeutic strategies in disease prevention and treatment. In this context, drug delivery to the lymphatic system is gaining prominence not only to improve the systemic bioavailability of various pharmaceutical drugs but also to target certain specific diseases associated with the lymphatic system. Although the role of the lymphatic system in lupus is known, very little is done to target drugs to yield improved clinical benefits...
February 13, 2024: Pharmacological Reviews
https://read.qxmd.com/read/38101936/correction-to-goods-and-bads-of-the-endocannabinoid-system-as-a-therapeutic-target-lessons-learned-after-30-years
#30
JOURNAL ARTICLE
(no author information available yet)
No abstract text is available yet for this article.
December 15, 2023: Pharmacological Reviews
https://read.qxmd.com/read/38101935/correction-to-oxycodone-a-current-perspective-on-its-pharmacology-abuse-and-pharmacotherapeutic-developments
#31
JOURNAL ARTICLE
(no author information available yet)
No abstract text is available yet for this article.
December 15, 2023: Pharmacological Reviews
https://read.qxmd.com/read/38101934/nonhormonal-male-contraceptive-development-strategies-for-progress
#32
REVIEW
Logan Nickels, Wei Yan
Despite the widely demonstrated public health benefits of contraception, limited contraceptive options are available for men, placing both the contraceptive burden and opportunity solely on women. This review outlines the need for an increased focus on male contraceptive development and highlights several related topics, including the perspectives of women and men on male contraceptives, historical challenges, and reasons behind the persistent delays in male contraceptive development. It also discusses the importance of serendipitous observations in drug discovery and the limitations of depleting sperm or spermatogenic cells as a contraceptive approach...
December 15, 2023: Pharmacological Reviews
https://read.qxmd.com/read/38101933/-pharmacological-reviews-75th-year-anniversary-past-and-future-editorial
#33
EDITORIAL
Lynette C Daws
No abstract text is available yet for this article.
December 15, 2023: Pharmacological Reviews
https://read.qxmd.com/read/37940347/the-slc6a15-slc6a20-neutral-amino-acid-transporter-subfamily-functions-diseases-and-their-therapeutic-relevance
#34
JOURNAL ARTICLE
Jędrzej Kukułowicz, Krzysztof Pietrzak-Lichwa, Klaudia Klimończyk, Nathalie Idlin, Marek Bajda
The neutral amino acid transporter subfamily that consists of six members; consecutively SLC6A15-SLC620, also called orphan transporters, represents membrane, sodium-dependent symporter proteins that belong to the family of solute carrier 6 (SLC6). Primarily, they mediate the transport of neutral amino acids from the extracellular milieu toward cell or storage vesicles utilizing an electric membrane potential as the driving force. Orphan transporters are widely distributed throughout the body, covering many systems; for instance, the central nervous, renal, or intestinal system, supplying cells into molecules utilized in biochemical, signaling, and building pathways afterward...
November 8, 2023: Pharmacological Reviews
https://read.qxmd.com/read/37339882/targeting-epidermal-growth-factor-receptor-for-cancer-treatment-abolishing-both-kinase-dependent-and-kinase-independent-functions-of-the-receptor
#35
REVIEW
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 are aimed at inhibiting the activation or the activity of EGFR tyrosine kinase. However, these agents have shown efficacy in only a few types of cancers...
November 2023: Pharmacological Reviews
https://read.qxmd.com/read/37321860/oxycodone-a-current-perspective-on-its-pharmacology-abuse-and-pharmacotherapeutic-developments
#36
REVIEW
James E Barrett, Aryan Shekarabi, Saadet Inan
Oxycodone, a semisynthetic derivative of naturally occurring thebaine, an opioid alkaloid, has been available for more than 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 of oxycodone, it was not until the 1990s that clinical studies began to explore its analgesic efficacy. These studies were followed by the pursuit of several preclinical studies to examine the analgesic effects and abuse liability of oxycodone in laboratory animals and the subjective effects in human volunteers...
November 2023: Pharmacological Reviews
https://read.qxmd.com/read/37863655/-regulation-of-pain-perception-by-microbiota-in-parkinson-s-disease
#37
JOURNAL ARTICLE
Zulmary Manjarres, Margarita Calvo, Rodrigo Pacheco
Pain perception involves current stimulation in peripheral nociceptive nerves and the subsequent stimulation of postsynaptic excitatory neurons in the spinal cord. Importantly, in chronic pain, the neural activity of both peripheral nociceptors and postsynaptic neurons in the central nervous system is influenced by several inflammatory mediators produced by the immune system. Growing evidence has indicated that the commensal microbiota plays an active role in regulating pain perception by either acting directly on nociceptors or indirectly through the modulation of the inflammatory activity on immune cells...
October 20, 2023: Pharmacological Reviews
https://read.qxmd.com/read/37845080/-halogenated-antimicrobial-agents-to-combat-drug-resistant-pathogens
#38
JOURNAL ARTICLE
Olajide Sunday Faleye, Bharath Reddy Boya, Jin Hyung Lee, Inho Choi, Jintae Lee
Antimicrobial resistance presents us with a potential global crisis as it undermines the abilities of conventional antibiotics to combat pathogenic microbes. The history of antimicrobial agents is replete with examples of scaffolds containing halogens. In this review, we discuss the impacts of halogen atoms in various antibiotic types and antimicrobial scaffolds and their modes of action, structure-activity relationships, and the contributions of halogen atoms in antimicrobial activity and drug resistance. Other halogenated molecules, including carbohydrates, peptides, lipids, and polymeric complexes, are also reviewed, and the effects of halogenated scaffolds on pharmacokinetics, pharmacodynamics, and factors affecting antimicrobial and antivirulence activities are presented...
October 16, 2023: Pharmacological Reviews
https://read.qxmd.com/read/37696583/-targeting-the-liver-with-nucleic-acid-therapeutics-for-the-treatment-of-systemic-diseases-of-liver-origin
#39
JOURNAL ARTICLE
Anagha Gogate, Jordyn Belcourt, Milan Shah, Alicia Zongxun Wang, Alexis Frankel, Holly Kolmel, Matthew Chalon, Prajith Stephen, Aarush Kolli, Sherouk M Tawfik, Jing Jin, Raman Bahal, Theodore P Rasmussen, Jose E Manautou, Xiao-Bo Zhong
Systemic diseases of liver origin (SDLO) are complex diseases in multiple organ systems, such as cardiovascular, musculoskeletal, endocrine, renal, respiratory, and sensory organ systems, caused by irregular liver metabolism and production of functional factors. Examples of such diseases discussed in this article include primary hyperoxaluria, familial hypercholesterolemia, acute hepatic porphyria, hereditary transthyretin amyloidosis, hemophilia, atherosclerotic cardiovascular diseases, alpha-1 antitrypsin deficiency-associated liver disease, and complement-mediated diseases...
September 11, 2023: Pharmacological Reviews
https://read.qxmd.com/read/37684054/-therapeutic-potential-of-targeting-prokineticin-receptors-in-diseases
#40
JOURNAL ARTICLE
Martina Vincenzi, Amin Kremic, Appoline Jouve, Roberta Lattanzi, Rossella Miele, Mohamed Benharouga, Nadia Alfaidy-Benharouga, Stephanie Migrenne-Li, Anumantha G Kanthasamy, Marimelia Porcionatto, Napoleone Ferrara, Igor V Tetko, Laurent Désaubry, Canan G Nebigil
The prokineticins (PKs) were discovered approximately 20 years ago as small peptides inducing gut contractility. Today, they are established as angiogenic, anorectic and proinflammatory cytokines, chemokines, hormones and neuropeptides involved in variety of physiological and pathophysiological pathways. Their altered expression or mutations implicated in several diseases make them a potential biomarker. Their G-protein coupled receptors (GPCRs), PKR1 and PKR2 have divergent roles that can be therapeutic target for treatment of cardiovascular, metabolic, and neural diseases as well as pain and cancer...
September 8, 2023: Pharmacological Reviews
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