[HTML][HTML] Design and synthesis of analogues of natural products

ME Maier - Organic & Biomolecular Chemistry, 2015 - pubs.rsc.org
In this article strategies for the design and synthesis of natural product analogues are
summarized and illustrated with some selected examples. Proven strategies include …

Following the lead from nature with covalent inhibitors

R Lagoutte, N Winssinger - Chimia, 2017 - ojs.chimia.ch
Covalent inhibitors are re-emerging as pharmacologically interesting entities with several
candidates having received recent approval for therapeutic intervention. Nature has …

Targeting drug resistance in EGFR with covalent inhibitors: a structure-based design approach

J Engel, A Richters, M Getlik, S Tomassi… - Journal of medicinal …, 2015 - ACS Publications
Receptor tyrosine kinases represent one of the prime targets in cancer therapy, as the
dysregulation of these elementary transducers of extracellular signals, like the epidermal …

Development of selective covalent Janus kinase 3 inhibitors

L Tan, K Akahane, R McNally… - Journal of medicinal …, 2015 - ACS Publications
The Janus kinases (JAKs) and their downstream effectors, signal transducer and activator of
transcription proteins (STATs), form a critical immune cell signaling circuit, which is of …

Screening for covalent inhibitors using DNA-display of small molecule libraries functionalized with cysteine reactive moieties

C Zambaldo, JP Daguer, J Saarbach, S Barluenga… - …, 2016 - pubs.rsc.org
DNA-encoded chemical libraries are increasingly used to identify leads for drug discovery or
chemical biology. Despite the resurging interest in covalent inhibitors, libraries are typically …

A highly selective and sensitive near-infrared fluorescence probe for arylamine N-acetyltransferase 2 in vitro and in vivo

X Wang, L Cui, N Zhou, W Zhu, R Wang, X Qian… - Chemical …, 2013 - pubs.rsc.org
We developed a near-infrared fluorescence probe for the highly selective and sensitive
detection of NAT2 activity. An arylamine was designed as the substrate part for NATs, as …

Sense-and-release logic-gated molecular network responding to dimeric cell surface proteins

S Angerani, N Winssinger - Journal of the American Chemical …, 2020 - ACS Publications
Dimeric proteins are prominent in biology, and receptor dimerization (homo-or
heterodimerization) is central to signal transduction. Herein, we report a network that …

Site-Specific Glycoconjugation of Protein via Bioorthogonal Tetrazine Cycloaddition with a Genetically Encoded trans-Cyclooctene or Bicyclononyne

T Machida, K Lang, L Xue, JW Chin… - Bioconjugate …, 2015 - ACS Publications
Efficient access to proteins modified site-specifically with glycans is important in
glycobiology and for therapeutic applications. Herein, we report a biocompatible protein …

Luciferase‐Induced Photouncaging: Bioluminolysis

D Chang, E Lindberg, S Feng, S Angerani… - Angewandte …, 2019 - Wiley Online Library
Bioluminescence resonance energy transfer (BRET) has been widely used for studying
dynamic processes in biological systems such as protein–protein interactions and other …

Recent advances in JAK3 inhibition: Isoform selectivity by covalent cysteine targeting

M Forster, M Gehringer, SA Laufer - Bioorganic & medicinal chemistry …, 2017 - Elsevier
Janus kinases (JAKs) are a family of four cytosolic protein kinases with a high degree of
structural similarity. Due to its very restricted role in immune regulation, JAK3 was promoted …