MedChemCases

In response to Novartis’ publication of TNO155, the Institute for Applied Cancer Science (IACS) at the University of Texas MD Anderson Cancer Center made a significant scientific contribution by unveiling their SHP2 inhibitor, designated as IACS-15414. By employing in silico screening techniques, they utilized the crystal structure of the SHP2 mutant T468 protein (4OHL) as […]

The first clinical-stage SHP2 (Src homology-2 domain-containing protein tyrosine phosphatase-2) inhibitor TNO155 was discovered by Novartis. The intriguing details of this discovery were documented in two consecutive papers, namely J. Med. Chem. 2016, 59, 7773−7782 and J. Med. Chem. 2020, 63, 13578−13594. During a high-throughput screening process, a known ion channel inhibitor SHP836 was identified