{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Wen CL"],"funding":["Science and Technology Commission of Shanghai Municipality","Shanghai Municipal Education Commission","Shanghai Eastern Youth Scholar Program","National Natural Science Foundation of China"],"pagination":["23264-23273"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6859357"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["116(46)"],"pubmed_abstract":["Glycolytic enzyme phosphoglycerate mutase 1 (PGAM1) plays a critical role in cancer metabolism by coordinating glycolysis and biosynthesis. A well-validated PGAM1 inhibitor, however, has not been reported for treating pancreatic ductal adenocarcinoma (PDAC), which is one of the deadliest malignancies worldwide. By uncovering the elevated PGAM1 expressions were statistically related to worse prognosis of PDAC in a cohort of 50 patients, we developed a series of allosteric PGAM1 inhibitors by structure-guided optimization. The compound KH3 significantly suppressed proliferation of various PDAC cells by down-regulating the levels of glycolysis and mitochondrial respiration in correlation with PGAM1 expression. Similar to PGAM1 depletion, KH3 dramatically hampered the canonic pathways highly i"],"journal":["Proceedings of the National Academy of Sciences of the United States of America"],"pubmed_title":["An allosteric PGAM1 inhibitor effectively suppresses pancreatic ductal adenocarcinoma."],"pmcid":["PMC6859357"],"funding_grant_id":["21472026","81871906","21877014","DQ2015010","81672325","14ZZ103","81502695","81802358","15JC1402800","91853206"],"pubmed_authors":["Tang XM","Lu W","Shen BY","Xiang XQ","Huang K","Wang XJ","Huang JY","Wang PH","Wang Q","Chen Z","Zhan Q","Ye DY","Dai YT","Lai LH","Shi MM","Zhou L","Chen J","Wang LW","Sun X","Jiang LL","Li HW","Li M","Wang QB","Li HT","Fang Y","Chen SJ","Lu XX","Zhang XD","Wen CL","Peng CH","Ruan XX","Xu YH"],"additional_accession":[]},"is_claimable":false,"name":"An allosteric PGAM1 inhibitor effectively suppresses pancreatic ductal adenocarcinoma.","description":"Glycolytic enzyme phosphoglycerate mutase 1 (PGAM1) plays a critical role in cancer metabolism by coordinating glycolysis and biosynthesis. A well-validated PGAM1 inhibitor, however, has not been reported for treating pancreatic ductal adenocarcinoma (PDAC), which is one of the deadliest malignancies worldwide. By uncovering the elevated PGAM1 expressions were statistically related to worse prognosis of PDAC in a cohort of 50 patients, we developed a series of allosteric PGAM1 inhibitors by structure-guided optimization. The compound KH3 significantly suppressed proliferation of various PDAC cells by down-regulating the levels of glycolysis and mitochondrial respiration in correlation with PGAM1 expression. Similar to PGAM1 depletion, KH3 dramatically hampered the canonic pathways highly i","dates":{"release":"2019-01-01T00:00:00Z","publication":"2019 Nov","modification":"2026-05-03T02:46:59.701Z","creation":"2025-04-04T22:45:04.099Z"},"accession":"S-EPMC6859357","cross_references":{"pubmed":["31662475"],"doi":["10.1073/pnas.1914557116"]}}