Identification of a novel PHGDH covalent inhibitor by chemical proteomics and phenotypic profiling

• Main Authors: Chen Chen (Author), Tianyu Zhu (Author), Xiaoqin Liu (Author), Dongrong Zhu (Author), Yi Zhang (Author), Sifang Wu (Author), Chao Han (Author), Hao Zhang (Author), Jianguang Luo (Author), Lingyi Kong (Author)
• Format: Book
• Published: Elsevier, 2022-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

The first rate-limiting enzyme of the serine synthesis pathway (SSP), phosphoglycerate dehydrogenase (PHGDH), is hyperactive in multiple tumors, which leads to the activation of SSP and promotes tumorigenesis. However, only a few inhibitors of PHGDH have been discovered to date, especially the coval...