Category: 1448190-10-0

Buckley, Dennis L. published the artcileHaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins, Formula: C11H8N2OS, the publication is ACS Chemical Biology (2015), 10(8), 1831-1837, database is CAplus and MEDLINE.

Small mol.-induced protein degradation is an attractive strategy for the development of chem. probes. One method for inducing targeted protein degradation involves the use of PROTACs, heterobifunctional mols. that can recruit specific E3 ligases to a desired protein of interest. PROTACs have been successfully used to degrade numerous proteins in cells, but the peptidic E3 ligase ligands used in previous PROTACs have hindered their development into more mature chem. probes or therapeutics. The authors report the design of a novel class of PROTACs that incorporate small mol. VHL ligands to successfully degrade HaloTag7 fusion proteins. These HaloPROTACs will inspire the development of future PROTACs with more drug-like properties. Addnl., these HaloPROTACs are useful chem. genetic tools, due to their ability to chem. knock down widely used HaloTag7 fusion proteins in a general fashion.

ACS Chemical Biology published new progress about 1448190-10-0. 1448190-10-0 belongs to thiazole, auxiliary class Thiazoles, name is 2-Hydroxy-4-(4-methylthiazol-5-yl)benzonitrile, and the molecular formula is C11H8N2OS, Formula: C11H8N2OS.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica

Farnaby, William published the artcileBAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design, Safety of 2-Hydroxy-4-(4-methylthiazol-5-yl)benzonitrile, the publication is Nature Chemical Biology (2019), 15(7), 672-680, database is CAplus and MEDLINE.

Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 and SMARCA4 using a bromodomain ligand and recruitment of the E3 ubiquitin ligase VHL. High-resolution ternary complex crystal structures and biophys. investigation guided rational and efficient optimization toward ACBI1(I), a potent and cooperative degrader of SMARCA2, SMARCA4 and PBRM1. I induced anti-proliferative effects and cell death caused by SMARCA2 depletion in SMARCA4 mutant cancer cells, and in acute myeloid leukemia cells dependent on SMARCA4 ATPase activity. These findings exemplify a successful biophysics- and structure-based PROTAC design approach to degrade high profile drug targets, and pave the way toward new therapeutics for the treatment of tumors sensitive to the loss of BAF complex ATPases.

Nature Chemical Biology published new progress about 1448190-10-0. 1448190-10-0 belongs to thiazole, auxiliary class Thiazoles, name is 2-Hydroxy-4-(4-methylthiazol-5-yl)benzonitrile, and the molecular formula is C11H8N2OS, Safety of 2-Hydroxy-4-(4-methylthiazol-5-yl)benzonitrile.

Referemce:
https://pubchem.ncbi.nlm.nih.gov/compound/thiazole,
Thiazole | chemical compound | Britannica