Drug intelligence / Profile preview

5MPN (Univ. of Louisville)

Development stage
Preclinical
Lead developer
University of Louisville
Modality
Small Molecules
01

Overview

5MPN (Univ. of Louisville): sourced facts only. name: "In order to target PFKFB4, we conducted a virtual screen of compounds that fit into the active site of PFKFB4 and discovered a first-in-class small molecule selective PFKFB4 inhibitor, termed 5MPN, that selectively inhibits recombinant PFKFB4 activity and decreases F26BP, glycolysis and proliferation in multiple NSCLC cell lines, with significantly higher anti-proliferative effects in Ras-driven cell lines." [DOI:10.1158/1538-7445.am2023-461]; target: "In order to target PFKFB4, we conducted a virtual screen of compounds that fit into the active site of PFKFB4 and discovered a first-in-class small molecule selective PFKFB4 inhibitor, termed 5MPN, that selectively inhibits recombinant PFKFB4 activity and decreases F26BP, glycolysis and proliferation in multiple NSCLC cell lines, with significantly higher anti-proliferative effects in Ras-driven cell lines." [DOI:10.1158/1538-7445.am2023-461]; developer: "1University of Louisville, Louisville, KY." [DOI:10.1158/1538-7445.am2023-461]; modality: "discovered a first-in-class small molecule selective PFKFB4 inhibitor, termed 5MPN, that selectively inhibits recombinant PFKFB4 activity and decreases F26BP, glycolysis and proliferation in multiple NSCLC cell lines, with significantly higher anti-proliferative effects in Ras-driven cell lines." [DOI:10.1158/1538-7445.am2023-461]; stage: "5MPN also caused marked suppression of growth in established NSCLC xenograft tumors, importantly without systemic toxicity." [DOI:10.1158/1538-7445.am2023-461]

02

Targets

PFKFB4 (6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 4)

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