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Year Number of Results
2005 2
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2011 1
2012 3
2013 2
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2020 1
2021 1
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19 results

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Page 1
Structurally Diverse Histone Deacetylase Photoreactive Probes: Design, Synthesis, and Photolabeling Studies in Live Cells and Tissue.
Aboukhatwa SM, Hanigan TW, Taha TY, Neerasa J, Ranjan R, El-Bastawissy EE, Elkersh MA, El-Moselhy TF, Frasor J, Mahmud N, McLachlan A, Petukhov PA. Aboukhatwa SM, et al. Among authors: petukhov pa. ChemMedChem. 2019 Jun 5;14(11):1096-1107. doi: 10.1002/cmdc.201900114. Epub 2019 Apr 10. ChemMedChem. 2019. PMID: 30921497 Free PMC article.
Histone deacetylase (HDAC) activity is modulated in vivo by post-translational modifications and formation of multiprotein complexes. Novel chemical tools to study how these factors affect engagement of HDAC isoforms by HDAC inhibitors (HDACi) in cells …
Histone deacetylase (HDAC) activity is modulated in vivo by post-translational modifications and formation of multiprotein com …
Scaffold dependent histone deacetylase (HDAC) inhibitor induced re-equilibration of the subcellular localization and post-translational modification state of class I HDACs.
Hanigan TW, Taha TY, Aboukhatwa SM, Frasor J, Petukhov PA. Hanigan TW, et al. Among authors: petukhov pa. PLoS One. 2017 Oct 18;12(10):e0186620. doi: 10.1371/journal.pone.0186620. eCollection 2017. PLoS One. 2017. PMID: 29045501 Free PMC article.
The mechanism of action of histone deacetylase inhibitors (HDACi) is mainly attributed to the inhibition of the deacetylase catalytic activity for their histone substrates. ...The subcellular re-equilibration of HDAC1 was subsequent to the accumulation of acetylated …
The mechanism of action of histone deacetylase inhibitors (HDACi) is mainly attributed to the inhibition of the deacetylase catalytic …
Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.
Taha TY, Aboukhatwa SM, Knopp RC, Ikegaki N, Abdelkarim H, Neerasa J, Lu Y, Neelarapu R, Hanigan TW, Thatcher GRJ, Petukhov PA. Taha TY, et al. Among authors: petukhov pa. ACS Med Chem Lett. 2017 Aug 1;8(8):824-829. doi: 10.1021/acsmedchemlett.7b00126. eCollection 2017 Aug 10. ACS Med Chem Lett. 2017. PMID: 28835796 Free PMC article.
Histone deacetylase 8 (HDAC8) is a promising drug target for multiple therapeutic applications. ...The selectivity of 3g and 3n was confirmed in SH-SY5Y cells as both did not increase the acetylation of histone H3 and alpha-tubulin. Discovery of the novel TIQ chemot …
Histone deacetylase 8 (HDAC8) is a promising drug target for multiple therapeutic applications. ...The selectivity of 3g and 3n was c …
Novel HDAC inhibitors with radiosensitizing properties.
Jung M, Velena A, Chen B, Petukhov PA, Kozikowski AP, Dritschilo A. Jung M, et al. Among authors: petukhov pa. Radiat Res. 2005 May;163(5):488-93. doi: 10.1667/rr3345. Radiat Res. 2005. PMID: 15850409
The members of the histone deacetylase (HDAC) family play important roles in various cellular processes, including transcriptional regulation, cell proliferation, differentiation and apoptosis. Inhibitors of histone deacetylases are emerging as an important n …
The members of the histone deacetylase (HDAC) family play important roles in various cellular processes, including transcripti …
Design, Synthesis, Molecular Modeling, and Biological Evaluation of Novel Amine-based Histone Deacetylase Inhibitors.
Abdelkarim H, Neelarapu R, Madriaga A, Vaidya AS, Kastrati I, Karumudi B, Wang YT, Taha TY, Thatcher GRJ, Frasor J, Petukhov PA. Abdelkarim H, et al. Among authors: petukhov pa. ChemMedChem. 2017 Dec 19;12(24):2030-2043. doi: 10.1002/cmdc.201700449. Epub 2017 Nov 30. ChemMedChem. 2017. PMID: 29080240 Free PMC article.
Histone deacetylases (HDACs) are promising drug targets for a variety of therapeutic applications. Herein we describe the design, synthesis, biological evaluation in cellular models of cancer, and preliminary drug metabolism and pharmacokinetic studies (DMPK) of a series o …
Histone deacetylases (HDACs) are promising drug targets for a variety of therapeutic applications. Herein we describe the design, syn …
Histone deacetylase inhibitor-based chromatin precipitation for identification of targeted genomic loci.
Hanigan TW, Danes JM, Taha TY, Frasor J, Petukhov PA. Hanigan TW, et al. Among authors: petukhov pa. J Biol Methods. 2018;5(1):e88. doi: 10.14440/jbm.2018.216. J Biol Methods. 2018. PMID: 29682593 Free PMC article.
Histone deacetylase (HDAC) catalyzes the removal of acetyl marks from histones, effectively regulating gene expression. Genome wide chromatin immunoprecipitation (ChIP) studies have shown HDACs are present on numerous active and repressed genes. However, H …
Histone deacetylase (HDAC) catalyzes the removal of acetyl marks from histones, effectively regulating gene expression. …
Neuronal complexity is attenuated in preclinical models of migraine and restored by HDAC6 inhibition.
Bertels Z, Singh H, Dripps I, Siegersma K, Tipton AF, Witkowski WD, Sheets Z, Shah P, Conway C, Mangutov E, Ao M, Petukhova V, Karumudi B, Petukhov PA, Baca SM, Rasenick MM, Pradhan AA. Bertels Z, et al. Among authors: petukhov pa. Elife. 2021 Apr 15;10:e63076. doi: 10.7554/eLife.63076. Elife. 2021. PMID: 33856345 Free PMC article.
Cytoskeletal flexibility is fundamental to neuronal-plasticity and is dependent on dynamic microtubules. Histone-deacetylase-6 (HDAC6) decreases microtubule dynamics by deacetylating its primary substrate, alpha-tubulin. ...
Cytoskeletal flexibility is fundamental to neuronal-plasticity and is dependent on dynamic microtubules. Histone-deacetylase-6 (HDAC6 …
Divergent JNK Phosphorylation of HDAC3 in Triple-Negative Breast Cancer Cells Determines HDAC Inhibitor Binding and Selectivity.
Hanigan TW, Aboukhatwa SM, Taha TY, Frasor J, Petukhov PA. Hanigan TW, et al. Among authors: petukhov pa. Cell Chem Biol. 2017 Nov 16;24(11):1356-1367.e8. doi: 10.1016/j.chembiol.2017.08.015. Epub 2017 Sep 21. Cell Chem Biol. 2017. PMID: 28943357 Free PMC article.
Histone deacetylase (HDAC) catalytic activity is regulated by formation of co-regulator complexes and post-translational modification. ...This study points to HDAC3 and the JNK axes as targets in TNBC, highlights how HDAC phosphorylation affects HDACi binding …
Histone deacetylase (HDAC) catalytic activity is regulated by formation of co-regulator complexes and post-translational modif …
A chimeric SERM-histone deacetylase inhibitor approach to breast cancer therapy.
Patel HK, Siklos MI, Abdelkarim H, Mendonca EL, Vaidya A, Petukhov PA, Thatcher GR. Patel HK, et al. Among authors: petukhov pa. ChemMedChem. 2014 Mar;9(3):602-13. doi: 10.1002/cmdc.201300270. Epub 2013 Aug 16. ChemMedChem. 2014. PMID: 23956109 Free PMC article.
Breast cancer remains a significant cause of death in women, and few therapeutic options exist for estrogen receptor negative (ER (-)) cancers. Epigenetic reactivation of target genes using histone deacetylase (HDAC) inhibitors has been proposed in ER (-) cancers to …
Breast cancer remains a significant cause of death in women, and few therapeutic options exist for estrogen receptor negative (ER (-)) cance …
19 results