Structure-Based Design of “Head-to-Tail” Macrocyclic PROTACs
C Li, Y Chen, W Huang, Y Qiu, S Huang, Y Zhou… - JACS Au, 2024 - ACS Publications
Macrocyclization is a compelling strategy for conventional drug design for improving
biological activity, target specificity, and metabolic stability, but it was rarely applied to the …
biological activity, target specificity, and metabolic stability, but it was rarely applied to the …
CRBN‐PROTACs in Cancer Therapy: From Mechanistic Insights to Clinical Applications
Cereblon (CRBN), a member of the E3 ubiquitin ligase complex, has gained significant
attention as a therapeutic target in cancer. CRBN regulates the degradation of various …
attention as a therapeutic target in cancer. CRBN regulates the degradation of various …
Discovery of SMD-3236: A Potent, Highly Selective and Efficacious SMARCA2 Degrader for the Treatment of SMARC4-Deficient Human Cancers
SMARCA2 is an attractive synthetic lethal target in human cancers with mutated, inactivated
SMARCA4. We report herein the discovery of highly potent and selective SMARCA2 …
SMARCA4. We report herein the discovery of highly potent and selective SMARCA2 …
Use of ionic liquids in amidation reactions for proteolysis targeting chimera synthesis
M Eleuteri, J Desantis, G Cruciani, R Germani… - Organic & …, 2024 - pubs.rsc.org
Selective degradation of disease-causing proteins using proteolysis targeting chimeras
(PROTACs) has gained great attention, thanks to its several advantages over traditional …
(PROTACs) has gained great attention, thanks to its several advantages over traditional …