Impact of cross-coupling reactions in drug discovery and development
MJ Buskes, MJ Blanco - Molecules, 2020 - mdpi.com
Cross-coupling reactions have played a critical role enabling the rapid expansion of
structure–activity relationships (SAR) during the drug discovery phase to identify a clinical …
structure–activity relationships (SAR) during the drug discovery phase to identify a clinical …
E3 ligase ligands in successful PROTACs: an overview of syntheses and linker attachment points
Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new
and exciting class of therapeutic agents that promise to significantly impact drug discovery …
and exciting class of therapeutic agents that promise to significantly impact drug discovery …
Antibody-mediated delivery of chimeric BRD4 degraders. Part 1: exploration of antibody linker, payload loading, and payload molecular properties
PS Dragovich, TH Pillow, RA Blake… - Journal of Medicinal …, 2021 - ACS Publications
The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …
related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin …
Rapid synthesis of pomalidomide-conjugates for the development of protein degrader libraries
DK Brownsey, BC Rowley, E Gorobets, BS Gelfand… - Chemical …, 2021 - pubs.rsc.org
Current methods for the preparation of heterobifunctional pomalidomide-conjugates rely on
methods that are often low yielding and produce intractable byproducts. Herein we describe …
methods that are often low yielding and produce intractable byproducts. Herein we describe …
Design and characterization of PROTAC degraders specific to protein N-terminal methyltransferase 1
Protein N-terminal methylation catalyzed by N-terminal methyltransferase 1 (NTMT1) is an
emerging methylation present in eukaryotes, playing important regulatory roles in various …
emerging methylation present in eukaryotes, playing important regulatory roles in various …
Expanding the Structural Diversity at the Phenylene Core of Ligands for the von Hippel–Lindau E3 Ubiquitin Ligase: Development of Highly Potent Hypoxia-Inducible …
LP Vu, CJ Diehl, R Casement, AG Bond… - Journal of Medicinal …, 2023 - ACS Publications
Hypoxia-inducible factor-1α (HIF-1α) constitutes the principal mediator of cellular adaptation
to hypoxia in humans. The HIF-1α protein level and activity are tightly regulated by the …
to hypoxia in humans. The HIF-1α protein level and activity are tightly regulated by the …
Discovery of highly potent and selective IRAK1 degraders to probe scaffolding functions of IRAK1 in ABC DLBCL
L Fu, J Zhang, B Shen, L Kong, Y Liu… - Journal of Medicinal …, 2021 - ACS Publications
MyD88 gene mutation has been identified as one of the most prevalent driver mutations in
the activated B-cell-like diffuse large B-cell lymphoma (ABC DLBCL). The published …
the activated B-cell-like diffuse large B-cell lymphoma (ABC DLBCL). The published …
Feasible column chromatography-free, multi-gram scale synthetic process of VH032 amine, which could enable rapid PROTAC library construction
PROTACs represent a promising modality that has gained significant attention for the
treatment of cancer, Alzheimer's disease, and so forth. Due to limited structural information of …
treatment of cancer, Alzheimer's disease, and so forth. Due to limited structural information of …
Efficient, multi-hundred-gram scale access to E3 ubiquitin ligase ligands for degrader development
MS Cooper, MC Norley, S Armitage… - Organic & …, 2023 - pubs.rsc.org
Small molecule heterobifunctional degraders (commonly also known as PROTACs) offer
tremendous potential to deliver new therapeutics in areas of unmet medical need. To deliver …
tremendous potential to deliver new therapeutics in areas of unmet medical need. To deliver …
Identification of non-conventional small molecule degraders and stabilizers of squalene synthase
JGF Hoock, C Rossetti, M Bilgin, L Depta… - Chemical …, 2023 - pubs.rsc.org
Squalene synthase (SQS) is an essential enzyme in the mevalonate pathway, which
controls cholesterol biosynthesis and homeostasis. Although catalytic inhibitors of SQS have …
controls cholesterol biosynthesis and homeostasis. Although catalytic inhibitors of SQS have …