Proteomics

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Biophysical and biochemical properties of PHGDH revealed by studies on PHGDH inhibitors


ABSTRACT: Biophysical and biochemical properties of PHGDH revealed by studies on PHGDH inhibitors

ORGANISM(S): Homo Sapiens

SUBMITTER: Lunzhi Dai  

PROVIDER: PXD029445 | iProX | Fri Oct 29 00:00:00 BST 2021

REPOSITORIES: iProX

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Biophysical and biochemical properties of PHGDH revealed by studies on PHGDH inhibitors.

Tan Yuping Y   Zhou Xia X   Gong Yanqiu Y   Gou Kun K   Luo Youfu Y   Jia Da D   Dai Lunzhi L   Zhao Yinglan Y   Sun Qingxiang Q  

Cellular and molecular life sciences : CMLS 20211231 1


The rate-limiting serine biogenesis enzyme PHGDH is overexpressed in cancers. Both serine withdrawal and genetic/pharmacological inhibition of PHGDH have demonstrated promising tumor-suppressing activities. However, the enzyme properties of PHGDH are not well understood and the discovery of PHGDH inhibitors is still in its infancy. Here, oridonin was identified from a natural product library as a new PHGDH inhibitor. The crystal structure of PHGDH in complex with oridonin revealed a new alloster  ...[more]

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