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 …

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 …

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 …

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 …

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 …

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 …

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 …

Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

S Pan, A Ding, Y Li, Y Sun, Y Zhan, Z Ye… - Chemical Society …, 2023 - pubs.rsc.org
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 …

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 …

[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 …