Advances in covalent drug discovery
L Boike, NJ Henning, DK Nomura - Nature Reviews Drug Discovery, 2022 - nature.com
Covalent drugs have been used to treat diseases for more than a century, but tools that
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …
facilitate the rational design of covalent drugs have emerged more recently. The purposeful …
Opportunities and challenges in phenotypic drug discovery: an industry perspective
Phenotypic drug discovery (PDD) approaches do not rely on knowledge of the identity of a
specific drug target or a hypothesis about its role in disease, in contrast to the target-based …
specific drug target or a hypothesis about its role in disease, in contrast to the target-based …
Enterococci enhance Clostridioides difficile pathogenesis
Enteric pathogens are exposed to a dynamic polymicrobial environment in the
gastrointestinal tract. This microbial community has been shown to be important during …
gastrointestinal tract. This microbial community has been shown to be important during …
Reimagining high-throughput profiling of reactive cysteines for cell-based screening of large electrophile libraries
Current methods used for measuring amino acid side-chain reactivity lack the throughput
needed to screen large chemical libraries for interactions across the proteome. Here we …
needed to screen large chemical libraries for interactions across the proteome. Here we …
Targeted protein degradation by electrophilic PROTACs that stereoselectively and site-specifically engage DCAF1
Targeted protein degradation induced by heterobifunctional compounds and molecular
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
glues presents an exciting avenue for chemical probe and drug discovery. To date, small …
Recent developments in PROTAC‐mediated protein degradation: from bench to clinic
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
Chemistry for covalent modification of endogenous/native proteins: from test tubes to complex biological systems
Chemical modification of proteins provides powerful tools to realize a broad range of
exciting biological applications, including the development of new classes of …
exciting biological applications, including the development of new classes of …
Recent advances in activity-based probes (ABPs) and affinity-based probes (A f BPs) for profiling of enzymes
Activity-based protein profiling (ABPP) is a technique that uses highly selective active-site
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …
targeted chemical probes to label and monitor the state of proteins. ABPP integrates the …
Recent advances in identifying protein targets in drug discovery
Phenotype-based screening has emerged as an alternative route for discovering new
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …
chemical entities toward first-in-class therapeutics. However, clarifying their mode of action …
Metabolites of microbiota response to tryptophan and intestinal mucosal immunity: A therapeutic target to control intestinal inflammation
J Zhang, S Zhu, N Ma, LJ Johnston… - Medicinal Research …, 2021 - Wiley Online Library
In a complex, diverse intestinal environment, commensal microbiota metabolizes excessive
dietary tryptophan to produce more bioactive metabolites connecting with kinds of diverse …
dietary tryptophan to produce more bioactive metabolites connecting with kinds of diverse …