Bioorthogonal chemistry
SL Scinto, DA Bilodeau, R Hincapie, W Lee… - Nature Reviews …, 2021 - nature.com
Bioorthogonal chemistry represents a class of high-yielding chemical reactions that proceed
rapidly and selectively in biological environments without side reactions towards …
rapidly and selectively in biological environments without side reactions towards …
The medicinal chemist's toolbox for late stage functionalization of drug-like molecules
T Cernak, KD Dykstra, S Tyagarajan… - Chemical Society …, 2016 - pubs.rsc.org
The advent of modern C–H functionalization chemistries has enabled medicinal chemists to
consider a synthetic strategy, late stage functionalization (LSF), which utilizes the C–H …
consider a synthetic strategy, late stage functionalization (LSF), which utilizes the C–H …
Modern advances in heterocyclic chemistry in drug discovery
AP Taylor, RP Robinson, YM Fobian… - Organic & …, 2016 - pubs.rsc.org
New advances in synthetic methodologies that allow rapid access to a wide variety of
functionalized heterocyclic compounds are of critical importance to the medicinal chemist as …
functionalized heterocyclic compounds are of critical importance to the medicinal chemist as …
The promise and peril of chemical probes
CH Arrowsmith, JE Audia, C Austin, J Baell… - Nature chemical …, 2015 - nature.com
Chemical probes are powerful reagents with increasing impacts on biomedical research.
However, probes of poor quality or that are used incorrectly generate misleading results. To …
However, probes of poor quality or that are used incorrectly generate misleading results. To …
Expanding chemical probe space: quality criteria for covalent and degrader probes
IV Hartung, J Rudolph, MM Mader… - Journal of Medicinal …, 2023 - ACS Publications
Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …
Improving target assessment in biomedical research: the GOT-IT recommendations
CH Emmerich, LM Gamboa, MCJ Hofmann… - Nature reviews Drug …, 2021 - nature.com
Academic research plays a key role in identifying new drug targets, including understanding
target biology and links between targets and disease states. To lead to new drugs, however …
target biology and links between targets and disease states. To lead to new drugs, however …
Sulfonyl fluorides as privileged warheads in chemical biology
A Narayanan, LH Jones - Chemical science, 2015 - pubs.rsc.org
Sulfonyl fluoride electrophiles have found significant utility as reactive probes in chemical
biology and molecular pharmacology. As warheads they possess the right balance of …
biology and molecular pharmacology. As warheads they possess the right balance of …
Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine
Over the past decade, remarkable advances have been witnessed in the development of
small-molecule probes. These molecular tools have been widely applied for interrogating …
small-molecule probes. These molecular tools have been widely applied for interrogating …
WD40 repeat domain proteins: a novel target class?
M Schapira, M Tyers, M Torrent… - Nature reviews Drug …, 2017 - nature.com
Antagonism of protein–protein interactions (PPIs) with small molecules is becoming more
feasible as a therapeutic approach. Successful PPI inhibitors tend to target proteins …
feasible as a therapeutic approach. Successful PPI inhibitors tend to target proteins …
[HTML][HTML] Chemical probes and drug leads from advances in synthetic planning and methodology
CJ Gerry, SL Schreiber - Nature Reviews Drug Discovery, 2018 - nature.com
Screening of small-molecule libraries is a productive method for identifying both chemical
probes of disease-related targets and potential starting points for drug discovery. In this …
probes of disease-related targets and potential starting points for drug discovery. In this …