Discovery of 2(1H)-Quinoxalinone Derivatives as Potent and Selective MAT2A Inhibitors for the Treatment of MTAP-Deficient Cancers.
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DOI: 10.1021/acs.jmedchem.4c01635
Abstract: Methionine adenosyltransferase 2A (MAT2A) has emerged as a synthetic lethal drug target in cancers bearing homozygous methylthioadenosine phosphorylase (MTAP) gene deletion. Despite the remarkable progress in the discovery and development of MAT2A inhibitors, current understanding… read more here.
Keywords: mat2a; selective mat2a; mat2a inhibitors; mtap deficient ... See more keywords
Abstract 1746: FGFR3 inhibition is a highly effective therapy in MTAP-deficient, FGFR3 altered urothelial carcinoma
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DOI: 10.1158/1538-7445.am2025-1746
Abstract: FGFR3 alterations are observed in more than 15% of metastatic urothelial cancers. In 2019, erdafitinib was the first FGFR inhibitor approved by the FDA for treatment of FGFR3-altered metastatic urothelial cancer with an objective response… read more here.
Keywords: mtap deficient; fgfr inhibitors; fgfr3 altered;
Abstract 6862: Preclinical evaluation of drugs for the treatment of MTAP-deficient cancers
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DOI: 10.1158/1538-7445.am2025-6862
Abstract: 5-Methylthioadenosine phosphorylase (MTAP), a key enzyme in the methionine salvage pathway that plays a vital role in cell apoptosis, proliferation, differentiation and inflammatory response, is frequently deleted in human cancers, approximately 15% of total tumors,… read more here.
Keywords: treatment; mtap deficient; deficient cancers; prmt5 ... See more keywords
Reduced symmetric dimethylation stabilizes vimentin and promotes metastasis in MTAP‐deficient lung cancer
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DOI: 10.15252/embr.202154265
Abstract: The aggressive nature and poor prognosis of lung cancer led us to explore the mechanisms driving disease progression. Utilizing our invasive cell‐based model, we identified methylthioadenosine phosphorylase (MTAP) and confirmed its suppressive effects on tumorigenesis… read more here.
Keywords: lung cancer; mtap deficient;
Immune suppression in MTAP-deficient cancers via glutamate metabolism and CXCL10 downregulation
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DOI: 10.3389/fimmu.2025.1634342
Abstract: Background Immune checkpoint inhibitors (ICIs) have transformed cancer therapy; however, their efficacy remains limited in certain tumor subtypes, including those deficient in methylthioadenosine phosphorylase (MTAP). MTAP-deficient cancers are characterized by immunosuppressive tumor microenvironments (TMEs) and… read more here.
Keywords: mtap deficient; glutamate metabolism; deficient;