{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Guo Z"],"funding":["Flight Attendant Medical Research Institute","Damon Runyon Cancer Research Fund","National Cancer Institute","NCI NIH HHS"],"pagination":["17158-17162"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC6861656"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["58(48)"],"pubmed_abstract":["Glucose transporters play an essential role in cancer cell proliferation and survival and have been pursued as promising cancer drug targets. Using microarrays of a library of new macrocycles known as rapafucins, which were inspired by the natural product rapamycin, we screened for new inhibitors of GLUT1. We identified multiple hits from the rapafucin 3D microarray and confirmed one hit as a bona fide GLUT1 ligand, which we named rapaglutin A (RgA). We demonstrate that RgA is a potent inhibitor of GLUT1 as well as GLUT3 and GLUT4, with an IC<sub>50</sub> value of low nanomolar for GLUT1. RgA was found to inhibit glucose uptake, leading to a decrease in cellular ATP synthesis, activation of AMP-dependent kinase, inhibition of mTOR signaling, and induction of cell-cycle arrest and apoptosis"],"journal":["Angewandte Chemie (International ed. in English)"],"pubmed_title":["Discovery of a Potent GLUT Inhibitor from a Library of Rapafucins by Using 3D Microarrays."],"pmcid":["PMC6861656"],"funding_grant_id":["DP1 CA174428","P30 CA006973","P30CA006973"],"pubmed_authors":["Liu JO","Liberti MV","Guo Z","Li RJ","Xie Y","Zhu H","Sukumar S","Wang J","Rao AVS","Hong SY","Cheng Z","Liu W","Peng H","Li Y","Schiene-Fischer C","Korangath P","Ying X","Wang Y","Locasale JW","Fischer G"],"additional_accession":[]},"is_claimable":false,"name":"Discovery of a Potent GLUT Inhibitor from a Library of Rapafucins by Using 3D Microarrays.","description":"Glucose transporters play an essential role in cancer cell proliferation and survival and have been pursued as promising cancer drug targets. Using microarrays of a library of new macrocycles known as rapafucins, which were inspired by the natural product rapamycin, we screened for new inhibitors of GLUT1. We identified multiple hits from the rapafucin 3D microarray and confirmed one hit as a bona fide GLUT1 ligand, which we named rapaglutin A (RgA). We demonstrate that RgA is a potent inhibitor of GLUT1 as well as GLUT3 and GLUT4, with an IC<sub>50</sub> value of low nanomolar for GLUT1. RgA was found to inhibit glucose uptake, leading to a decrease in cellular ATP synthesis, activation of AMP-dependent kinase, inhibition of mTOR signaling, and induction of cell-cycle arrest and apoptosis","dates":{"release":"2019-01-01T00:00:00Z","publication":"2019 Nov","modification":"2025-05-18T13:17:10.479Z","creation":"2025-05-18T13:17:10.479Z"},"accession":"S-EPMC6861656","cross_references":{"pubmed":["31591797"],"doi":["10.1002/anie.201905578"]}}