Targeting KMT2A: A Potential Approach To Cancer Therapies (G4297)

Target Name: KMT2A

NCBI ID: G4297

KMT2A

Targeting KMT2A: A Potential Approach To Cancer Therapies

KMT2A, also known as MLL cleavage product C180, is a protein that is expressed in various tissues throughout the body. It is a key player in the DNA replication process and has been linked to the development and progression of various diseases, including leukemia.

Research has shown that KMT2A can be targeted as a drug or biomarker in cancer therapies. One approach to targeting KMT2A is through the use of small molecules that can inhibit its activity. One such small molecule is called KO-184, which is a compound that was synthesized by researchers at the University of California, San Diego.

KO-184 works by inhibiting the activity of KMT2A, preventing it from cleaving DNA and leading to the accumulation of mutations in the genome. This can lead to the development of cancer. In preclinical studies, KO-184 has been shown to be an effective inhibitor of KMT2A and has the potential to be a useful drug or biomarker in cancer therapies.

Another approach to targeting KMT2A is through the use of antibodies that recognize and target specific regions of the protein. One such antibody is called KM2, which was developed by researchers at the University of California, Davis.

KM2 is designed to recognize a specific epitope (a region of the protein that is unique to one species) on the KMT2A protein. It is able to bind to this epitope and can inhibit KMT2A's activity, leading to the accumulation of mutations in the genome. This can lead to the development of cancer. In preclinical studies, KM2 has been shown to be an effective inhibitor of KMT2A and has the potential to be a useful drug or biomarker in cancer therapies.

In addition to its potential use as a drug or biomarker, KMT2A is also of interest as a target for diagnostic tests. The MLL cleavage product gene is located on the X chromosome and is expressed in various tissues throughout the body, including the brain, spleen, and testes. This makes it a potential target for diagnostic tests that detect abnormalities in the X chromosome.

Research has shown that KMT2A is often expressed in various types of cancer, including leukemia, and that it is associated with poor prognosis. This suggests that KMT2A may be a useful biomarker for the diagnosis and prognosis of cancer.

In conclusion, KMT2A is a protein that is of interest as a drug or biomarker in cancer therapies due to its role in the DNA replication process and its association with the development and progression of various diseases, including leukemia. The small molecules KO-184 and KM2 have been shown to be effective inhibitors of KMT2A and have the potential to be useful drugs or biomarkers in cancer therapies. Additionally, KMT2A is also a potential target for diagnostic tests that detect abnormalities in the X chromosome. Further research is needed to fully understand the potential of KMT2A as a drug or biomarker and to develop safe and effective therapies for the treatment of cancer.

Protein Name: Lysine Methyltransferase 2A

Functions: Histone methyltransferase that plays an essential role in early development and hematopoiesis (PubMed:15960975, PubMed:12453419, PubMed:15960975, PubMed:19556245, PubMed:19187761, PubMed:20677832, PubMed:21220120, PubMed:26886794). Catalytic subunit of the MLL1/MLL complex, a multiprotein complex that mediates both methylation of 'Lys-4' of histone H3 (H3K4me) complex and acetylation of 'Lys-16' of histone H4 (H4K16ac) (PubMed:15960975, PubMed:12453419, PubMed:15960975, PubMed:19556245, PubMed:24235145, PubMed:19187761, PubMed:20677832, PubMed:21220120, PubMed:26886794). Catalyzes methyl group transfer from S-adenosyl-L-methionine to the epsilon-amino group of 'Lys-4' of histone H3 (H3K4) via a non-processive mechanism. Part of chromatin remodeling machinery predominantly forms H3K4me1 and H3K4me2 methylation marks at active chromatin sites where transcription and DNA repair take place (PubMed:25561738, PubMed:15960975, PubMed:12453419, PubMed:15960975, PubMed:19556245, PubMed:19187761, PubMed:20677832, PubMed:21220120, PubMed:26886794). Has weak methyltransferase activity by itself, and requires other component of the MLL1/MLL complex to obtain full methyltransferase activity (PubMed:19187761, PubMed:26886794). Has no activity toward histone H3 phosphorylated on 'Thr-3', less activity toward H3 dimethylated on 'Arg-8' or 'Lys-9', while it has higher activity toward H3 acetylated on 'Lys-9' (PubMed:19187761). Binds to unmethylated CpG elements in the promoter of target genes and helps maintain them in the nonmethylated state (PubMed:20010842). Required for transcriptional activation of HOXA9 (PubMed:12453419, PubMed:20677832, PubMed:20010842). Promotes PPP1R15A-induced apoptosis (PubMed:10490642). Plays a critical role in the control of circadian gene expression and is essential for the transcriptional activation mediated by the CLOCK-BMAL1 heterodimer (By similarity). Establishes a permissive chromatin state for circadian transcription by mediating a rhythmic methylation of 'Lys-4' of histone H3 (H3K4me) and this histone modification directs the circadian acetylation at H3K9 and H3K14 allowing the recruitment of CLOCK-BMAL1 to chromatin (By similarity). Also has auto-methylation activity on Cys-3882 in absence of histone H3 substrate (PubMed:24235145)

The "KMT2A Target / Biomarker Review Report" is a customizable review of hundreds up to thousends of related scientific research literature by AI technology, covering specific information about KMT2A comprehensively, including but not limited to:
•   general information;
•   protein structure and compound binding;
•   protein biological mechanisms;
•   its importance;
•   the target screening and validation;
•   expression level;
•   disease relevance;
•   drug resistance;
•   related combination drugs;
•   pharmacochemistry experiments;
•   related patent analysis;
•   advantages and risks of development, etc.
The report is helpful for project application, drug molecule design, research progress updates, publication of research papers, patent applications, etc. If you are interested to get a full version of this report, please feel free to contact us at BD@silexon.ai

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