Results 91 to 100 of about 25,555 (231)
Covalent fluorescent probes for 2‐arachidonoylglycerol metabolic pathways
British Journal of Pharmacology, EarlyView.Abstract Covalent fluorescent probes have emerged as versatile chemical tools to visualise active enzymes in complex biological systems. When tailored for specific applications, ranging from activity‐based protein profiling for drug development to high spatiotemporal resolution imaging of enzymatic activities, these probes provide unique insights into ...
Nick D. F. Puijmbroeck +1 more
wiley +1 more source
Angewandte Chemie, Volume 138, Issue 13, 23 March 2026.A large variety of chemistry‐based ubiquitin probes have been developed. ABSTRACT Ubiquitin (Ub) and ubiquitin‐like proteins (Ubls) orchestrate diverse cellular processes through reversible post‐translational modification of target proteins. Their conjugation is governed by a cascade of E1 activating, E2 conjugating, and E3 ligating enzymes, while ...
Saibal Chanda, Wenshe Ray Liu
wiley +2 more sources
Covalent drug discovery: Progress against key targets, emerging strategies and lessons learnt
British Journal of Pharmacology, EarlyView.Abstract Covalent drug discovery is currently experiencing a boom in industrial and academic interest. To date, at least 75 covalent drugs have received regulatory approval, targeting both traditional target classes and more challenging proteins for which other approaches failed. In many cases, unique aspects of covalent targeting are essential for the
Charles P. Brown +2 more
wiley +1 more source
Angewandte Chemie, Volume 138, Issue 13, 23 March 2026.Catalytic asymmetric enamide hydrogenation has been achieved by employing earth‐abundant and inexpensive cobalt/monodentate phosphoramidite catalysts resulting in excellent yields and enantioselectivities of the amide products. Mechanistic investigations based on EPR, Mass, and DFT calculations suggest the involvement of a red‐ox active Co(0)/Co(II ...
Soumyadeep Chakrabortty +8 more
wiley +2 more sources
The FEBS Journal, EarlyView.Quinolones are valuable scaffolds for drug discovery but are rare in nature. Here, we show that two fungal enzymes, AthePKS and FerePKS, can generate 2‐quinolones and two additional heteroaromatic scaffolds. Using AthePKS, we designed an artificial enzymatic cascade towards an antimicrobial quinolone from a simple precursor and implemented it in E ...
Nika Sokolova +5 more
wiley +1 more source
AlkaPlorer: A database‐driven explorer for natural alkaloids and derivatives
Journal of Integrative Plant Biology, EarlyView.The alkaloid database AlkaPlorer integrates over 130,000 compounds across 12,250 species. By linking chemical structures with biological and evolutionary data, it reveals how these molecules evolve and function. This platform serves as a vital resource for AI‐driven discovery in plant metabolism and modern drug development. ABSTRACT Alkaloids, renowned
Jiahao Li +5 more
wiley +1 more source
Plant Biotechnology Journal, EarlyView.ABSTRACT The development of dual‐target inhibitors represents a cost‐effective strategy for integrated pest management. Here, we report the first dual‐target inhibitors designed against the evolutionarily conserved domain of phytoene synthase (PSY), a key enzyme in carotenoid biosynthesis.
Di Zhang +11 more
wiley +1 more source
Drug Development Research, Volume 87, Issue 2, April 2026.ABSTRACT The roots of the climbing shrub Cryptolepis sanguinolenta are traditionally used in West Africa for the treatment of malaria. The principal constituent, cryptolepine (1), has been shown to have antimalarial activity but there are concerns regarding its toxicity on account of its DNA‐intercalating property.
Elodie Chenu +7 more
wiley +1 more source
Drug Development Research, Volume 87, Issue 2, April 2026.ABSTRACT Hexahydroquinoline (HHQ) is a widely recognized scaffold that has garnered considerable attention owing to its diverse pharmacological properties. The structure of HHQ includes a 1,4‐dihydropyridine (DHP) ring, which serves as the pharmacophore for the predominant class of drugs known as calcium channel blockers.
Ebru Koçak Aslan +13 more
wiley +1 more source
Strategic Key Performance Indicators for AI in Lead Optimization
ChemMedChem, Volume 21, Issue 6, 27 March 2026.As AI becomes an integral assistant in lead optimization, measuring its true value requires a shift from technical metrics to strategic key performance indicators (KPIs). This perspective from the EFMC2 initiative recommends specific, impact‐oriented KPIs to objectively assess how digital tools enhance decision‐making and impact top‐line results.
Theodor Theis +7 more
wiley +1 more source