article thumbnail

Structure-Based Optimization of Covalent, Small-Molecule Stabilizers of the 14-3-3?/ER? Protein–Protein Interaction from Nonselective Fragments

Covalent Modifiers

Arkin Journal of the American Chemical Society 2023 DOI: 10.1021/jacs.3c05161 Orthogonal biophysical assays, including mass spectrometry and fluorescence anisotropy, were used to establish structure–activity relationships. Visser, Edmee Vandenboorn, Sheng Chen, Priyadarshini Jaishankar, Maurits Overmans, Shubhankar Dutta, R.

article thumbnail

Advancements in hit identification for membrane protein drug discovery

Drug Target Review

The development of PoLiPa technology marks a new era in membrane protein drug discovery, rendering otherwise difficult targets accessible to structural biology, biophysical assays and other screening technologies. 2023) Biochemistry, G protein coupled receptors , StatPearls [Internet]. Jones EM, et al. doi:10.7554/elife.54895.

article thumbnail

Obstacles and innovations of macrocyclic drug development

Drug Target Review

Phase III trials for MK-0616 commenced in the second half of 2023. Their combined efforts have spanned both the academic research environment at UCSF and the applied field at BioPharmics LLC, which later became the BioPharmics Division of Optibrium in 2023. Journal of Computer-Aided Molecular Design , 37(11): 519535, 2023.