Discovery of an Orally Bioavailable and Selective PKMYT1 Inhibitor, RP-6306.
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DOI: 10.1021/acs.jmedchem.2c00552
Abstract: PKMYT1 is a regulator of CDK1 phosphorylation and is a compelling therapeutic target for the treatment of certain types of DNA damage response cancers due to its established synthetic lethal relationship with CCNE1 amplification. To… read more here.
Keywords: pkmyt1 inhibitor; pkmyt1; discovery orally; orally bioavailable ... See more keywords
Targeting Protein Kinase, Membrane-Associated Tyrosine/Threonine 1 (PKMYT1) for Precision Cancer Therapy: From Discovery to Clinical Trial.
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DOI: 10.1021/acs.jmedchem.4c01619
Abstract: \Protein kinase membrane-associated tyrosine/threonine 1 (PKMYT1), an overlooked member of the WEE family responsible for regulating cell cycle transition, has recently emerged as a compelling therapeutic target for precision cancer therapy due to its established… read more here.
Keywords: membrane associated; protein kinase; therapy; precision ... See more keywords
Targeting CCNE1 amplified ovarian and endometrial cancers by combined inhibition of PKMYT1 and ATR
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DOI: 10.1038/s41467-025-58183-w
Abstract: Ovarian cancers (OVCAs) and endometrial cancers (EMCAs) with CCNE1-amplification are often resistant to standard treatment and represent an unmet clinical need. Synthetic-lethal screening identified loss of the CDK1 regulator, PKMYT1, as synthetically lethal with CCNE1-amplification.… read more here.
Keywords: ccne1; ovarian endometrial; pkmyt1; endometrial cancers ... See more keywords
c-Myb-mediated inhibition of miR-601 in facilitating malignance of osteosarcoma via augmentation of PKMYT1
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DOI: 10.1038/s41598-022-10684-0
Abstract: The crosstalk between osteosarcoma (OS) development and abnormally expressed microRNA (miR)-601 is not explored explicitly. Here, we identified the downregulated miR-601 in osteosarcoma (OS) through a comprehensive bioinformatics analysis of GEO Datasets. The results indicated… read more here.
Keywords: pkmyt1; mir 601; osteosarcoma; mir ... See more keywords
Abstract 1735: The discovery of PKMYT1 inhibitors to exploit synthetic lethality caused by replication stress
Sign Up to like & getrecommendations! Published in 2025 at "Cancer Research"
DOI: 10.1158/1538-7445.am2025-1735
Abstract: Replication stress is a feature of the hyper-proliferation experienced by many cancers, leading to genome instability and accumulation of potentially lethal DNA damage. During their evolution, many cancer cells inactivate specific DNA-damage response pathways, placing… read more here.
Keywords: replication stress; pkmyt1 inhibitors; pkmyt1; dna ... See more keywords
Abstract 1742: Discovery and preclinical profiling of a novel PKMYT1 inhibitor, EVT-0003023, with high efficacy in late-stage, post-treatment non-small cell lung cancer models
Sign Up to like & getrecommendations! Published in 2025 at "Cancer Research"
DOI: 10.1158/1538-7445.am2025-1742
Abstract: Protein kinase membrane-associated tyrosine/threonine 1 (PKMYT1) is a negative regulator of CDK1 activity and has been identified as a putative synthetic lethal target in cancers which up-regulate cyclin E (CCNE1) or harbor mutations in genes… read more here.
Keywords: cancer; non small; evt 0003023; pkmyt1 ... See more keywords
Abstract LB436: VRN16: A novel PKMYT1 kinase selective inhibitor with wide therapeutic window
Sign Up to like & getrecommendations! Published in 2025 at "Cancer Research"
DOI: 10.1158/1538-7445.am2025-lb436
Abstract: PKMYT1, a serine/threonine kinase, selectively regulates CDK1 during the G2/M phase transition to prevent mitotic entry in the presence of DNA damage, whereas WEE1 kinase regulates both CDK1 and CDK2. Inhibition of PKMYT1 forces cancer… read more here.
Keywords: cancer; vrn16 novel; pkmyt1; inhibitor ... See more keywords
Demethylase ALKBH5 suppresses invasion of gastric cancer via PKMYT1 m6A modification
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DOI: 10.1186/s12943-022-01522-y
Abstract: Background Gastric cancer (GC) is one of the most pernicious tumors that seriously harm human healthcare. GC metastasis is one of the prime cause of failed cancer treatment, but correlation between N6-methyladenosine (m6A) and GC… read more here.
Keywords: cancer; alkbh5; metastasis; m6a ... See more keywords
Overexpressed PKMYT1 promotes tumor progression and associates with poor survival in esophageal squamous cell carcinoma
Sign Up to like & getrecommendations! Published in 2019 at "Cancer Management and Research"
DOI: 10.2147/cmar.s214243
Abstract: Background Esophageal squamous cell carcinoma (ESCC) is one of the most common malignant tumors worldwide and the 5-year overall survival rate remains poor. Protein kinase, membrane associated tyrosine/threonine (PKMYT1) is overexpressed in several cancers and… read more here.
Keywords: pkmyt1; progression; pkmyt1 escc; esophageal squamous ... See more keywords
High expression of PKMYT1 predicts poor prognosis and aggravates the progression of osteosarcoma via the NF κB pathway in MG63 cells.
Sign Up to like & getrecommendations! Published in 2023 at "Current cancer drug targets"
DOI: 10.2174/1568009623666230206154944
Abstract: BACKGROUND Protein kinase, membrane associated tyrosine/threonine 1 (PKMYT1) contributes to the proliferative, migratory, invasive and colony forming capabilities of oncocytes. Dysregulated expression of PKMYT1 is associated with numerous malignancies. However, at present, the functional role… read more here.
Keywords: osteosarcoma; pkmyt1; expression; mg63 cells ... See more keywords
Protein kinase, membrane‑associated tyrosine/threonine 1 is associated with the progression of colorectal cancer.
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DOI: 10.3892/or.2018.6371
Abstract: The protein kinase, membrane‑associated tyrosine/threonine 1 (PKMYT1) is known to inhibit precocious entry into mitosis by phosphorylating CDK1 at Thr14 and Tyr15 residues. However, the functional importance of PKMYT1 in colorectal cancer (CRC) remains unknown. Thus,… read more here.
Keywords: pkmyt1; associated tyrosine; membrane associated; protein kinase ... See more keywords