bms-1001-hcl

Description: BMS-1001 HCl is anovel and potent small molecule inhibitor of the PD-1/PD-L1 proteinprotein interaction with IC50 value of 2.25 nM in cell free assays. Itwas first discovered by Bristol-Myers Squibb. Blockade of the PD-1/PD-L1immune checkpoint pathway with monoclonal antibodies has providedsignificant advances in cancer treatment. The antibody-basedimmunotherapies carry a number of disadvantages such as the high cost ofthe antibodies, their limited half-life, and immunogenicity.Development of small-molecule PD-1/PD-L1 inhibitors that could overcomethese drawbacks is slow because of the incomplete structural informationfor this pathway. The first chemical PD-1/PD-L1 inhibitors, BMS-1001and its analogs, have been recently disclosed by Bristol-Myers Squibb.

References: Skalniak L, Zak KM, Guzik K, Magiera K, Musielak B, Pachota M, Szelazek B, Kocik J, Grudnik P, Tomala M, Krzanik S, Pyrc K, Dömling A, Dubin G, Holak TA. Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells. Oncotarget. 2017 Aug 7; 8(42):72167-72181.