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 …
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 …
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
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 …
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 …
cheaper drugs are needed more than ever. The pharmaceutical industry has been …
A chemical toolbox for the study of bromodomains and epigenetic signaling
Bromodomains (BRDs) are conserved protein interaction modules which recognize (read)
acetyl-lysine modifications, however their role (s) in regulating cellular states and their …
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 …
and plays a fundamental role in chromatin-based cellular processes including gene …
Bromodomain drug discovery–the past, the present, and the future
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 …
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 …
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 …
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 …
via gene knockout and use of antisense oligonucleotides; however, these techniques act via …