COA of Formula: C8H7BrO2In 2017 ,《Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1》 appeared in Journal of Medicinal Chemistry. The author of the article were Guzik, Katarzyna; Zak, Krzysztof M.; Grudnik, Przemyslaw; Magiera, Katarzyna; Musielak, Bogdan; Torner, Ricarda; Skalniak, Lukasz; Domling, Alexander; Dubin, Grzegorz; Holak, Tad A.. The article conveys some information:
Blockade of the PD-1/PD-L1 immune checkpoint pathway with monoclonal antibodies has provided significant advances in cancer treatment. The antibody-based immunotherapies carry a number of disadvantages such as the high cost of the antibodies, their limited half-life, and immunogenicity. Development of small-mol. PD-1/PD-L1 inhibitors that could overcome these drawbacks is slow because of the incomplete structural information for this pathway. The first chem. PD-1/PD-L1 inhibitors have been recently disclosed by Bristol-Myers Squibb. Here we present NMR and X-ray characterization for the two classes of these inhibitors. The X-ray structures of the PD-L1/inhibitor complexes reveal one inhibitor mol. located at the center of the PD-L1 homodimer, filling a deep hydrophobic channel-like pocket between two PD-L1 mols. Derivatives of (2-methyl-3-biphenylyl)methanol exhibit the structures capped on one side of the channel, whereas the compounds based on [3-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-methylphenyl]methanol induce an enlarged interaction interface that results in the open “”face-back”” tunnel through the PD-L1 dimer. In the experiment, the researchers used 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2COA of Formula: C8H7BrO2)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products. COA of Formula: C8H7BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary