Fluorine and fluorinated motifs in the design and application of bioisosteres for drug design

NA Meanwell - Journal of medicinal chemistry, 2018 - ACS Publications
The electronic properties and relatively small size of fluorine endow it with considerable
versatility as a bioisostere and it has found application as a substitute for lone pairs of …

Pharmacogenomics of drug metabolizing enzymes and transporters: relevance to precision medicine

S Ahmed, Z Zhou, J Zhou… - Genomics, proteomics and …, 2016 - academic.oup.com
The interindividual genetic variations in drug metabolizing enzymes and transporters
influence the efficacy and toxicity of numerous drugs. As a fundamental element in precision …

Disposition of nirmatrelvir, an orally bioavailable inhibitor of SARS-CoV-2 3C-like protease, across animals and humans

H Eng, AL Dantonio, EP Kadar, RS Obach, L Di… - Drug Metabolism and …, 2022 - ASPET
The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3C-like protease
inhibitor PF-07321332 (nirmatrelvir), in combination with ritonavir (Paxlovid), was recently …

Deuterodehalogenation Under Net Reductive or Redox‐Neutral Conditions Enabled by Paired Electrolysis

D Wood, S Lin - Angewandte Chemie, 2023 - Wiley Online Library
Interest in deuterated active pharmaceutical ingredients (APIs) is increasing as deuteration
holds promise for kinetic isotope effect (KIE) regulated fine‐tuning of API performance …

The concise guide to PHARMACOLOGY 2013/14: enzymes

SPH Alexander, HE Benson… - British Journal of …, 2013 - Wiley Online Library
Abstract The Concise Guide to PHARMACOLOGY 2013/14 provides concise overviews of
the key properties of over 2000 human drug targets with their pharmacology, plus links to an …

Discovery of pemigatinib: a potent and selective fibroblast growth factor receptor (FGFR) inhibitor

L Wu, C Zhang, C He, D Qian, L Lu, Y Sun… - Journal of Medicinal …, 2021 - ACS Publications
Aberrant activation of FGFR has been linked to the pathogenesis of many tumor types.
Selective inhibition of FGFR has emerged as a promising approach for cancer treatment …

Metabolic activation of the toxic natural products from herbal and dietary supplements leading to toxicities

YK Wang, WQ Li, S Xia, L Guo, Y Miao… - Frontiers in …, 2021 - frontiersin.org
Currently, herbal and dietary supplements have been widely applied to prevent and treat
various diseases. However, the potential toxicities and adverse reactions of herbal and …

G protein-coupled receptors (GPCRs): advances in structures, mechanisms, and drug discovery

M Zhang, T Chen, X Lu, X Lan, Z Chen… - Signal Transduction and …, 2024 - nature.com
G protein-coupled receptors (GPCRs), the largest family of human membrane proteins and
an important class of drug targets, play a role in maintaining numerous physiological …

Discovery of orally bioavailable SOS1 inhibitors for suppressing KRAS-driven carcinoma

H He, Y Zhang, J Xu, Y Li, H Fang, Y Liu… - Journal of Medicinal …, 2022 - ACS Publications
The interaction between son of sevenless 1 (SOS1) gene and Kirsten rat sarcoma viral
oncogene (KRAS) is crucial for activating signals of proliferation and survival in a range of …

Pan Assay Interference Compounds (PAINS) and other promiscuous compounds in antifungal research: Miniperspective

M Pouliot, S Jeanmart - Journal of medicinal chemistry, 2016 - ACS Publications
Every week, articles disclosing new antifungal leads reported as promising starting points for
optimization projects are published. In many cases, the mechanism that accounts for their …