THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors

British Journal of Pharmacology, Journal Year: 2019, Volume and Issue: 176(S1)

Published: Nov. 11, 2019

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. provides concise overviews key properties nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links open access knowledgebase source and their ligands (www.guidetopharmacology.org), which more detailed views target ligand properties. Although represents approximately 400 pages, material presented substantially reduced compared information website. It a permanent, citable, point-in-time record that will survive database updates. full contents section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14748. G protein-coupled receptors are one six major pharmacological into divided, others being: ion channels, nuclear hormone receptors, catalytic enzymes transporters. These nomenclature guidance summary best available tools, alongside references suggestions for further reading. landscape format designed facilitate comparison related from contemporary mid-2019, supersedes data 2017/18, 2015/16 2013/14 Guides previous Receptors Channels. produced close conjunction International Union Basic Clinical Pharmacology Committee Receptor Nomenclature Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification targets, where appropriate.

Language: Английский

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Amide Bond Bioisosteres: Strategies, Synthesis, and Successes

Journal of Medicinal Chemistry, Journal Year: 2020, Volume and Issue: 63(21), P. 12290 - 12358

Published: July 20, 2020

The amide functional group plays a key role in the composition of biomolecules, including many clinically approved drugs. Bioisosterism is widely employed rational modification lead compounds, being used to increase potency, enhance selectivity, improve pharmacokinetic properties, eliminate toxicity, and acquire novel chemical space secure intellectual property. introduction bioisostere leads structural changes molecular size, shape, electronic distribution, polarity, pKa, dipole or polarizability, which can be either favorable detrimental biological activity. This approach has opened up new avenues drug design development resulting more efficient candidates introduced onto market as well clinical pipeline. Herein, we review strategic decisions selecting an (the why), synthetic routes each how), success stories implementation) provide comprehensive overview this important toolbox for medicinal chemists.

Language: Английский

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The circadian regulation of food intake

Nature Reviews Endocrinology, Journal Year: 2019, Volume and Issue: 15(7), P. 393 - 405

Published: May 9, 2019

Language: Английский

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Importance of Melatonin in Assisted Reproductive Technology and Ovarian Aging

International Journal of Molecular Sciences, Journal Year: 2020, Volume and Issue: 21(3), P. 1135 - 1135

Published: Feb. 8, 2020

Melatonin is probably produced in all cells but only secreted by the pineal gland. The secretion of melatonin determined light–dark cycle, and it released at night. regulates biological rhythms via its receptors located suprachiasmatic nuclei hypothalamus. also has strong antioxidant activities to scavenge free radicals such as reactive oxygen species (ROS). direct radical scavenging actions are receptor independent. ROS play an important role reproductive function including ovulatory process. However, excessive can have adverse effect on oocytes because oxidative stress, thereby causing infertility. It becoming clear that ovarian follicular fluid themselves, which protects these from damage well having other beneficial oocyte maturation, fertilization, embryo development. Trials humans investigated improvement outcomes assisted technology (ART), vitro fertilization transfer (IVF-ET), way administering patients suffering In addition, clinical research examined anti-aging molecule antioxidative actions, relationship with aging diseases, e.g., Alzheimer’s Parkinson’s disease, underway. may reduce aging, a major issue technology. This review explains between human function, applications expected improve IVF, while discussing possibilities for preventing aging.

Language: Английский

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Obesity and chronic kidney disease

AJP Endocrinology and Metabolism, Journal Year: 2022, Volume and Issue: 324(1), P. E24 - E41

Published: Nov. 16, 2022

The prevalence of obesity has increased dramatically during the past decades, which been a major health problem. Since 1975, number people with worldwide nearly tripled. An increasing studies find as driver chronic kidney disease (CKD) progression, and mechanisms are complex include hemodynamic changes, inflammation, oxidative stress, activation renin-angiotensin-aldosterone system (RAAS). Obesity-related is characterized by glomerulomegaly, often accompanied localized segmental glomerulosclerosis lesions. In these patients, early symptoms atypical, microproteinuria being main clinical manifestation nephrotic syndrome rare. Weight loss RAAS blockers have protective effect on obesity-related CKD, but even so, significant proportion patients eventually progress to end-stage renal despite treatment. Thus, it critical comprehend underlying CKD create new tactics for slowing or stopping progression. this review, we summarize current knowledge disease, its pathological future perspectives

Language: Английский

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Melatonin Effects on Glucose Metabolism: Time To Unlock the Controversy

Trends in Endocrinology and Metabolism, Journal Year: 2020, Volume and Issue: 31(3), P. 192 - 204

Published: Jan. 1, 2020

Language: Английский

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Genetics of circadian rhythms and sleep in human health and disease

Nature Reviews Genetics, Journal Year: 2022, Volume and Issue: 24(1), P. 4 - 20

Published: Aug. 26, 2022

Language: Английский

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Melatonin potentials against viral infections including COVID-19: Current evidence and new findings

Virus Research, Journal Year: 2020, Volume and Issue: 287, P. 198108 - 198108

Published: Aug. 5, 2020

Language: Английский

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Ionizing Radiation as a Source of Oxidative Stress—The Protective Role of Melatonin and Vitamin D

International Journal of Molecular Sciences, Journal Year: 2020, Volume and Issue: 21(16), P. 5804 - 5804

Published: Aug. 13, 2020

Ionizing radiation (IR) has found widespread application in modern medicine, including medical imaging and radiotherapy. As a result, both patients healthcare professionals are exposed to various IR doses. To minimize the negative side effects of associated with oxidative imbalance, antioxidant therapy been considered. In this review, studies on melatonin vitamin D radiation-induced stress discussed. According research data, substances meet conditions for use as agents that protect humans against IR-induced tissue damage. Numerous have confirmed melatonin, hydro- lipophilic hormone strong properties, can potentially be used radioprotectant humans. Less is known about radioprotective D, but results date promising. Deficiencies common societies may contribute severity adverse exposure. Hence, supporting supplementation seems first importance. Interestingly, selectively radiosensitise cancer cells, which makes them promising adjuvants More needed area, especially

Language: Английский

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Transcriptional Control of Circadian Rhythms and Metabolism: A Matter of Time and Space

Endocrine Reviews, Journal Year: 2020, Volume and Issue: 41(5), P. 707 - 732

Published: May 11, 2020

All biological processes, living organisms, and ecosystems have evolved with the Sun that confers a 24-hour periodicity to life on Earth. Circadian rhythms arose from evolutionary needs maximize daily organismal fitness by enabling organisms mount anticipatory adaptive responses recurrent light-dark cycles associated environmental changes. The clock is conserved feature in nearly all forms of life, ranging prokaryotes virtually every cell multicellular eukaryotes. mammalian comprises transcription factors interlocked negative feedback loops, which generate circadian expression genes coordinate rhythmic physiology. In this review, we highlight previous recent studies advanced our understanding transcriptional architecture clock, specific focus epigenetic mechanisms, transcriptomics, 3-dimensional chromatin architecture. addition, discuss reciprocal ways metabolism regulate each other metabolic rhythms. We also implications biology human health, genetic environment disruptions novel therapeutic opportunities for medicine. Finally, explore remaining fundamental questions future challenges advancing field forward.

Language: Английский

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