Future challenges with DNA-encoded chemical libraries in the drug discovery domain
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 …
become a powerful technology platform for ligand discovery in biomedical research and …
Open-air alkylation reactions in photoredox-catalyzed DNA-encoded library synthesis
DNA-encoded library (DEL) technology is a powerful tool commonly used by the
pharmaceutical industry for the identification of compounds with affinity to biomolecular …
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 …
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 …
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 …
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 …
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 …
processes ranging from cell division to protein homeostasis. Compounds targeting p97 …
Opportunities and challenges for the development of covalent chemical immunomodulators
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 …
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 …
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 …
technologies that enable their effective development. A typical drug discovery workflow …