Future challenges with DNA-encoded chemical libraries in the drug discovery domain

G Zhao, Y Huang, Y Zhou, Y Li, X Li - Expert Opinion on Drug …, 2019 - Taylor & Francis
Introduction: DNA-encoded chemical libraries (DELs) have come of age and emerged to
become a powerful technology platform for ligand discovery in biomedical research and …

Open-air alkylation reactions in photoredox-catalyzed DNA-encoded library synthesis

JP Phelan, SB Lang, J Sim, S Berritt… - Journal of the …, 2019 - ACS Publications
DNA-encoded library (DEL) technology is a powerful tool commonly used by the
pharmaceutical industry for the identification of compounds with affinity to biomolecular …

Applications of reactive cysteine profiling

KM Backus - Activity-Based Protein Profiling, 2019 - Springer
Cysteine thiols are involved in a diverse set of biological transformations, including
nucleophilic and redox catalysis, metal coordination and formation of both dynamic and …

Chemical epigenetics: the impact of chemical and chemical biology techniques on bromodomain target validation

M Schiedel, M Moroglu, DMH Ascough… - Angewandte Chemie …, 2019 - Wiley Online Library
Epigenetics is currently the focus of intense research interest across a broad range of
disciplines due to its importance in a multitude of biological processes and disease states …

Development of a selection method for discovering irreversible (covalent) binders from a DNA-encoded library

Z Zhu, LSC Grady, Y Ding, KE Lind… - … the Science of Drug …, 2019 - journals.sagepub.com
DNA-encoded libraries (DELs) have been broadly applied to identify chemical probes for
target validation and lead discovery. To date, the main application of the DEL platform has …

An Activity‐Based Probe Targeting Non‐Catalytic, Highly Conserved Amino Acid Residues within Bromodomains

M D'Ascenzio, KM Pugh, R Konietzny… - Angewandte …, 2019 - Wiley Online Library
Bromodomain‐containing proteins are epigenetic modulators involved in a wide range of
cellular processes, from recruitment of transcription factors to pathological disruption of gene …

Small-molecule modulators of the ATPase VCP/p97 affect specific p97 cellular functions

A Figuerola-Conchas, J Saarbach… - ACS chemical …, 2019 - ACS Publications
VCP/p97 belongs to the AAA+ ATPase family and has an essential role in several cellular
processes ranging from cell division to protein homeostasis. Compounds targeting p97 …

Opportunities and challenges for the development of covalent chemical immunomodulators

KM Backus, J Cao, SM Maddox - Bioorganic & Medicinal Chemistry, 2019 - Elsevier
Compounds that react irreversibly with cysteines have reemerged as potent and selective
tools for altering protein function, serving as chemical probes and even clinically approved …

Chemische Epigenetik: der Einfluss chemischer und chemo‐biologischer Techniken auf die Zielstruktur‐Validierung von Bromodomänen

M Schiedel, M Moroglu, DMH Ascough… - Angewandte …, 2019 - Wiley Online Library
Viele Disziplinen befassen sich gegenwärtig mit Epigenetik, da diese von Bedeutung für
viele biologische Vorgänge und pathologische Zustände ist. Auf molekularer Ebene fußen …

DNA-Encoded Compound Libraries: An Emerging Paradigm in Drug Hit Discovery

RM Franzini - Drug Discovery and Development, Third Edition, 2019 - taylorfrancis.com
The development of new therapeutic agents critically depends on the availability of
technologies that enable their effective development. A typical drug discovery workflow …