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   Articles with "mtap" as a keyword



Integrative Clinical and Genomic Characterization of MTAP-deficient Metastatic Urothelial Cancer.

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recommendations! Published in 2021 at "European urology oncology"

DOI: 10.1016/j.euo.2021.10.006

Abstract: Deficiency of MTAP (MTAPdef) mainly occurs because of homozygous loss of chromosome 9p21, which is the most common copy-number loss in metastatic urothelial cancer (mUC). We characterized the clinical and genomic features of MTAPdef mUC… read more here.

Keywords: urothelial cancer; mtap; biology; cancer ... See more keywords
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Expression and localisation of methylthioadenosine phosphorylase (MTAP) in oral squamous cell carcinoma and their significance in epithelial-to-mesenchymal transition.

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recommendations! Published in 2021 at "Pathology"

DOI: 10.1016/j.pathol.2021.05.101

Abstract: Methylthioadenosine phosphorylase (MTAP) is a rate-limiting enzyme in the methionine salvage pathway, which recycles one carbon unit that is lost during polyamine synthesis back into the methionine cycle. Although MTAP deficiency has been reported in… read more here.

Keywords: methylthioadenosine phosphorylase; oral squamous; expression mtap; expression ... See more keywords

Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers.

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recommendations! Published in 2024 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c00133

Abstract: It has been shown that PRMT5 inhibition by small molecules can selectively kill cancer cells with homozygous deletion of the MTAP gene if the inhibitors can leverage the consequence of MTAP deletion, namely, accumulation of… read more here.

Keywords: brain; discovery tng908; mtap deleted; mta ... See more keywords

From DNA-Encoded Library Screening to AM-9747: An MTA-Cooperative PRMT5 Inhibitor with Potent Oral In Vivo Efficacy

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recommendations! Published in 2025 at "Journal of Medicinal Chemistry"

DOI: 10.1021/acs.jmedchem.4c03101

Abstract: Inhibition of the methyltransferase enzyme PRMT5 by MTA accumulation is a vulnerability of MTAP-deleted cancers. Herein, we report the discovery and optimization of a quinolin-2-amine DEL hit that cooperatively binds PRMT5:MEP50 and MTA to generate… read more here.

Keywords: library screening; mta; dna encoded; prmt5 ... See more keywords

Discovery of AMG 193, an MTA-Cooperative PRMT5 Inhibitor for the Treatment of MTAP-Deleted Cancers.

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recommendations! Published in 2025 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.4c03121

Abstract: MTAP deletion occurs in 10-15% of all human cancers due to its proximity to the tumor suppressor gene CDKN2A. The loss of MTAP leads to accumulation of methylthioadenosine (MTA), which shares structural similarity to S-adenosyl… read more here.

Keywords: amg 193; mtap deleted; cooperative prmt5; mta cooperative ... See more keywords

PRMT5: A Promising Synthetical Lethal Target for MTAP-Deleted Cancers.

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recommendations! Published in 2025 at "Journal of medicinal chemistry"

DOI: 10.1021/acs.jmedchem.5c01895

Abstract: PRMT5 is a promising target for cancer therapy. However, the first-generation PRMT5 inhibitors failed in the clinical trials due to the dose-limiting hematological toxicities, which could be attributed to the indiscriminate blockade of PRMT5 and… read more here.

Keywords: prmt5 promising; lethal; promising synthetical; target ... See more keywords
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MTAP-deficiency could predict better treatment response in advanced lung adenocarcinoma patients initially treated with pemetrexed-platinum chemotherapy and bevacizumab

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recommendations! Published in 2020 at "Scientific Reports"

DOI: 10.1038/s41598-020-57812-2

Abstract: To investigate the predictive value of methylthioadenosine phosphorylase (MTAP) on treatment response and survival in advanced lung adenocarcinoma. MTAP expression was detected by immunohistochemistry. Treatment response and survival were compared according to MTAP expression level.… read more here.

Keywords: lung adenocarcinoma; advanced lung; treatment response; response ... See more keywords

Transition state analogue of MTAP extends lifespan of APCMin/+ mice

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recommendations! Published in 2021 at "Scientific Reports"

DOI: 10.1038/s41598-021-87734-6

Abstract: A mouse model of human Familial Adenomatous Polyposis responds favorably to pharmacological inhibition of 5′-methylthioadenosine phosphorylase (MTAP). Methylthio-DADMe-Immucillin-A (MTDIA) is an orally available, transition state analogue inhibitor of MTAP. 5′-Methylthioadenosine (MTA), the substrate for MTAP,… read more here.

Keywords: mtdia; apcmin mice; mice; state analogue ... See more keywords

DDDR-10. TNG456 is a next-generation, brain-penetrant, MTA-cooperative PRMT5 inhibitor for the treatment of solid tumors, including glioblastoma, with MTAP loss

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recommendations! Published in 2025 at "Neuro-Oncology"

DOI: 10.1093/neuonc/noaf201.0647

Abstract: MTAP deletions occur in 10-15% of all human cancers, providing one of the largest precision oncology patient populations. MTA-cooperative PRMT5 inhibitors leverage the well-characterized synthetic lethal relationship between PRMT5 inhibition and MTAP loss. TNG908, TNG462,… read more here.

Keywords: mtap null; brain; solid tumors; cooperative prmt5 ... See more keywords
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Correlation of methylthioadenosine phosphorylase (MTAP) protein expression with MTAP and CDKN2A copy number in malignant pleural mesothelioma

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recommendations! Published in 2021 at "Histopathology"

DOI: 10.1111/his.14324

Abstract: Methylthioadenosine phosphorylase (MTAP) immunohistochemical expression is a specific marker of CDKN2A deletion in malignant mesothelioma. However, the relationship of MTAP expression with MTAP copy number remains unexplored. read more here.

Keywords: copy number; methylthioadenosine phosphorylase; expression mtap; expression ... See more keywords

Nutrient availability shapes methionine metabolism in p16/MTAP-deleted cells

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recommendations! Published in 2019 at "Science Advances"

DOI: 10.1126/sciadv.aav7769

Abstract: Nutrient availability is found to determine methionine metabolism. Codeletions of gene loci containing tumor suppressors and neighboring metabolic enzymes present an attractive synthetic dependency in cancers. However, the impact that these genetic events have on… read more here.

Keywords: metabolism; p16; nutrient availability; methionine metabolism ... See more keywords