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Pharmacological inhibition of KDM5A for cancer treatment.
Yang GJ, Wu J, Miao L, Zhu MH, Zhou QJ, Lu XJ, Lu JF, Leung CH, Ma DL, Chen J. Yang GJ, et al. Eur J Med Chem. 2021 Dec 15;226:113855. doi: 10.1016/j.ejmech.2021.113855. Epub 2021 Sep 15. Eur J Med Chem. 2021. PMID: 34555614 Review.
It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cell metastasis and invasiveness, drug resistance, and is associated with poor prognosis. ...This review will present the structural aspects of …
It is aberrantly expressed in many cancers, where it impedes differentiation and contributes to cancer cell proliferation, cel …
The emerging role of KDM5A in human cancer.
Yang GJ, Zhu MH, Lu XJ, Liu YJ, Lu JF, Leung CH, Ma DL, Chen J. Yang GJ, et al. J Hematol Oncol. 2021 Feb 17;14(1):30. doi: 10.1186/s13045-021-01041-1. J Hematol Oncol. 2021. PMID: 33596982 Free PMC article. Review.
Emerging studies indicate that KDM5A is responsible for driving multiple human diseases, particularly cancers. In this review, we summarize the roles of KDM5A in human cancers, survey the field of KDM5A inhibitors including their anticancer acti …
Emerging studies indicate that KDM5A is responsible for driving multiple human diseases, particularly cancers. In this review, …
A chromatin-mediated reversible drug-tolerant state in cancer cell subpopulations.
Sharma SV, Lee DY, Li B, Quinlan MP, Takahashi F, Maheswaran S, McDermott U, Azizian N, Zou L, Fischbach MA, Wong KK, Brandstetter K, Wittner B, Ramaswamy S, Classon M, Settleman J. Sharma SV, et al. Cell. 2010 Apr 2;141(1):69-80. doi: 10.1016/j.cell.2010.02.027. Cell. 2010. PMID: 20371346 Free PMC article.
Accumulating evidence implicates heterogeneity within cancer cell populations in the response to stressful exposures, including drug treatments. ...These cells demonstrate >100-fold reduced drug sensitivity and maintain viability via engagement of IGF-1 receptor signali …
Accumulating evidence implicates heterogeneity within cancer cell populations in the response to stressful exposures, including drug …
KDM5A promotes proliferation and EMT in ovarian cancer and closely correlates with PTX resistance.
Feng T, Wang Y, Lang Y, Zhang Y. Feng T, et al. Mol Med Rep. 2017 Sep;16(3):3573-3580. doi: 10.3892/mmr.2017.6960. Epub 2017 Jul 12. Mol Med Rep. 2017. PMID: 28714030
In brief, KDM5A is a crucial oncogene that is significantly upregulated in ovarian cancer. Its expression is closely correlated with cancer cell proliferation, EMT and metastasis. KDM5A suppresses ovarian cancer cell apoptosis under PTX treatmen …
In brief, KDM5A is a crucial oncogene that is significantly upregulated in ovarian cancer. Its expression is closely correlate …
Targeting of KDM5A by miR-421 in Human Ovarian Cancer Suppresses the Progression of Ovarian Cancer Cells.
Ren F, Shrestha C, Shi H, Sun F, Zhang M, Cao Y, Li G. Ren F, et al. Onco Targets Ther. 2020 Sep 23;13:9419-9428. doi: 10.2147/OTT.S266211. eCollection 2020. Onco Targets Ther. 2020. PMID: 33061428 Free PMC article. Retracted.
PURPOSE: The retinoblastoma binding protein RBP2 (KDM5A) is a histone demethylase that promotes cell growth in many human cancers. ...MATERIALS AND METHODS: Public microarray databases were analyzed to assess KDM5A and miR-421 expression in ovarian cancer …
PURPOSE: The retinoblastoma binding protein RBP2 (KDM5A) is a histone demethylase that promotes cell growth in many human cancers …
The KDM5A/RBP2 histone demethylase represses NOTCH signaling to sustain neuroendocrine differentiation and promote small cell lung cancer tumorigenesis.
Oser MG, Sabet AH, Gao W, Chakraborty AA, Schinzel AC, Jennings RB, Fonseca R, Bonal DM, Booker MA, Flaifel A, Novak JS, Christensen CL, Zhang H, Herbert ZT, Tolstorukov MY, Buss EJ, Wong KK, Bronson RT, Nguyen QD, Signoretti S, Kaelin WG Jr. Oser MG, et al. Genes Dev. 2019 Dec 1;33(23-24):1718-1738. doi: 10.1101/gad.328336.119. Epub 2019 Nov 14. Genes Dev. 2019. PMID: 31727771 Free PMC article.
More than 90% of small cell lung cancers (SCLCs) harbor loss-of-function mutations in the tumor suppressor gene RB1 The canonical function of the RB1 gene product, pRB, is to repress the E2F transcription factor family, but pRB also functions to regulate cellular different …
More than 90% of small cell lung cancers (SCLCs) harbor loss-of-function mutations in the tumor suppressor gene RB1 The canonical fun …
Drawing a line between histone demethylase KDM5A and KDM5B: their roles in development and tumorigenesis.
Yoo J, Kim GW, Jeon YH, Kim JY, Lee SW, Kwon SH. Yoo J, et al. Exp Mol Med. 2022 Dec;54(12):2107-2117. doi: 10.1038/s12276-022-00902-0. Epub 2022 Dec 12. Exp Mol Med. 2022. PMID: 36509829 Free PMC article. Review.
Notably, the KDM5 subfamily of histone lysine-specific demethylases plays essential roles in the proper development and differentiation of tissues, and aberrant regulation of KDM5 proteins during development can lead to chronic developmental defects and even cancer. In thi …
Notably, the KDM5 subfamily of histone lysine-specific demethylases plays essential roles in the proper development and differentiation of t …
Activation of the KDM5A/miRNA-495/YTHDF2/m6A-MOB3B axis facilitates prostate cancer progression.
Du C, Lv C, Feng Y, Yu S. Du C, et al. J Exp Clin Cancer Res. 2020 Oct 21;39(1):223. doi: 10.1186/s13046-020-01735-3. J Exp Clin Cancer Res. 2020. PMID: 33087165 Free PMC article.
This study was performed to elucidate the potential effects of KDM5A on prostate cancer (PCa) progression via the miR-495/YTHDF2/m6A-MOB3B axis. ...CONCLUSION: In summary, our study highlights the potential of histone demethylase KDM5A activity in enhancing P …
This study was performed to elucidate the potential effects of KDM5A on prostate cancer (PCa) progression via the miR-495/YTHD …
Histone H3 proline 16 hydroxylation regulates mammalian gene expression.
Liu X, Wang J, Boyer JA, Gong W, Zhao S, Xie L, Wu Q, Zhang C, Jain K, Guo Y, Rodriguez J, Li M, Uryu H, Liao C, Hu L, Zhou J, Shi X, Tsai YH, Yan Q, Luo W, Chen X, Strahl BD, von Kriegsheim A, Zhang Q, Wang GG, Baldwin AS, Zhang Q. Liu X, et al. Nat Genet. 2022 Nov;54(11):1721-1735. doi: 10.1038/s41588-022-01212-x. Epub 2022 Nov 8. Nat Genet. 2022. PMID: 36347944 Free PMC article.
Here, we report the existence of a histone PTM in mammalian cells, namely histone H3 with hydroxylation of proline at residue 16 (H3P16oh), which is catalyzed by the proline hydroxylase EGLN2. We show that H3P16oh enhances direct binding of KDM5A to its substrate, histone …
Here, we report the existence of a histone PTM in mammalian cells, namely histone H3 with hydroxylation of proline at residue 16 (H3P16oh), …
Domain architecture and protein-protein interactions regulate KDM5A recruitment to the chromatin.
Kataria A, Tyagi S. Kataria A, et al. Epigenetics. 2023 Dec;18(1):2268813. doi: 10.1080/15592294.2023.2268813. Epub 2023 Oct 15. Epigenetics. 2023. PMID: 37838974 Free PMC article. Review.
Its link to various diseases, including cancer, makes KDM5A an important target for drug development. However, despite several studies outlining its significance in various pathways, our lack of understanding of its recruitment and function at the target sites on th …
Its link to various diseases, including cancer, makes KDM5A an important target for drug development. However, despite several …
185 results