Bromodomains: a new target class for drug development

AG Cochran, AR Conery, RJ Sims III - Nature Reviews Drug Discovery, 2019 - nature.com
Less than a decade ago, it was shown that bromodomains, acetyl lysine 'reader'modules
found in proteins with varied functions, were highly tractable small-molecule targets. This is …

Small-molecule discovery through DNA-encoded libraries

AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …

DNA-encoded library screening as core platform technology in drug discovery: its synthetic method development and applications in DEL synthesis

M Song, GT Hwang - Journal of medicinal chemistry, 2020 - ACS Publications
DNA-encoded library technology (DELT) was introduced to our medicinal chemistry society
more than 20 years ago. The application of DELT in the development of clinical candidates …

High-power screening (HPS) empowered by DNA-encoded libraries

YK Sunkari, VK Siripuram, TL Nguyen… - Trends in …, 2022 - cell.com
The world is totally dependent on medications. As science progresses, new, better, and
cheaper drugs are needed more than ever. The pharmaceutical industry has been …

A chemical toolbox for the study of bromodomains and epigenetic signaling

Q Wu, D Heidenreich, S Zhou, S Ackloo… - Nature …, 2019 - nature.com
Bromodomains (BRDs) are conserved protein interaction modules which recognize (read)
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …

Bromodomain inhibitors and therapeutic applications

BK Gajjela, MM Zhou - Current opinion in chemical biology, 2023 - Elsevier
The bromodomain acts to recognize acetylated lysine in histones and transcription proteins
and plays a fundamental role in chromatin-based cellular processes including gene …

Bromodomain drug discovery–the past, the present, and the future

M Pervaiz, P Mishra, S Günther - The Chemical Record, 2018 - Wiley Online Library
With the bromodomain (BRD) inhibitor JQ1, a remarkable success story of BRD4 as a novel
drug target has been set off that yielded many anti‐cancer drugs that are now in clinical …

Bispecific estrogen receptor α degraders incorporating novel binders identified using DNA-encoded chemical library screening

JS Disch, JM Duffy, ECY Lee, D Gikunju… - Journal of Medicinal …, 2021 - ACS Publications
Bispecific degraders (PROTACs) of ERα are expected to be advantageous over current
inhibitors of ERα signaling (aromatase inhibitors/SERMs/SERDs) used to treat ER+ breast …

Reversible covalent headpiece enables interconversion between double‐and single‐stranded DNA‐encoded chemical libraries

G Zhao, S Zhong, G Zhang, Y Li… - Angewandte Chemie …, 2022 - Wiley Online Library
The use of a proper encoding methodology is one of the most important aspects when
practicing DEL technology. A “headpiece”‐based double‐stranded DEL encoding method is …

DNA-encoded library-derived DDR1 inhibitor prevents fibrosis and renal function loss in a genetic mouse model of Alport syndrome

H Richter, AL Satz, M Bedoucha… - ACS chemical …, 2018 - ACS Publications
The importance of Discoidin Domain Receptor 1 (DDR1) in renal fibrosis has been shown
via gene knockout and use of antisense oligonucleotides; however, these techniques act via …