4cbt

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'''Unreleased structure'''
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{{STRUCTURE_4cbt| PDB=4cbt | SCENE= }}
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===Design, synthesis, and biological evaluation of potent and selective Class IIa HDAC inhibitors as a potential therapy for Huntingtons disease===
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{{ABSTRACT_PUBMED_24261862}}
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The entry 4cbt is ON HOLD until Paper Publication
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==Disease==
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[[http://www.uniprot.org/uniprot/HDAC4_HUMAN HDAC4_HUMAN]] Defects in HDAC4 are the cause of brachydactyly-mental retardation syndrome (BDMR) [MIM:[http://omim.org/entry/600430 600430]]. A syndrome resembling the physical anomalies found in Albright hereditary osteodystrophy. Common features are mild facial dysmorphism, congenital heart defects, distinct brachydactyly type E, mental retardation, developmental delay, seizures, autism spectrum disorder, and stocky build. Soft tissue ossification is absent, and there are no abnormalities in parathyroid hormone or calcium metabolism.<ref>PMID:20691407</ref>
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Authors: Burli, R.W., Luckhurst, C.A., Aziz, O., Matthews, K.L., Yates, D., Lyons, K.A., Beconi, M., McAllister, G., Breccia, P., Stott, A.J., Penrose, S.D., Wall, M., Lamers, M., Leonard, P., Mueller, I., Richardson, C.M., Jarvis, R., Stones, L., Hughes, S., Wishart, G., Haughan, A.F., OConnell, C., Mead, T., McNeil, H., Vann, J., Mangette, J., Maillard, M., Beaumont, V., Munoz-Sanjuan, I., Dominguez, C.
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==Function==
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[[http://www.uniprot.org/uniprot/HDAC4_HUMAN HDAC4_HUMAN]] Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Involved in muscle maturation via its interaction with the myocyte enhancer factors such as MEF2A, MEF2C and MEF2D.<ref>PMID:10523670</ref>
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Description: Design, synthesis, and biological evaluation of potent and selective Class IIa HDAC inhibitors as a potential therapy for Huntingtons disease
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==About this Structure==
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[[4cbt]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4CBT OCA].
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==Reference==
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<ref group="xtra">PMID:024261862</ref><references group="xtra"/><references/>
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[[Category: Histone deacetylase]]
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[[Category: Aziz, O.]]
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[[Category: Beaumont, V.]]
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[[Category: Beconi, M.]]
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[[Category: Breccia, P.]]
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[[Category: Burli, R W.]]
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[[Category: Dominguez, C.]]
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[[Category: Haughan, A F.]]
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[[Category: Hughes, S.]]
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[[Category: Jarvis, R.]]
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[[Category: Lamers, M.]]
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[[Category: Leonard, P.]]
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[[Category: Luckhurst, C A.]]
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[[Category: Lyons, K A.]]
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[[Category: Maillard, M.]]
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[[Category: Mangette, J.]]
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[[Category: Matthews, K L.]]
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[[Category: McAllister, G.]]
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[[Category: McNeil, H.]]
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[[Category: Mead, T.]]
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[[Category: Mueller, I.]]
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[[Category: Munoz-Sanjuan, I.]]
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[[Category: OConnell, C.]]
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[[Category: Penrose, S D.]]
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[[Category: Richardson, C M.]]
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[[Category: Stones, L.]]
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[[Category: Stott, A J.]]
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[[Category: Vann, J.]]
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[[Category: Wall, M.]]
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[[Category: Wishart, G.]]
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[[Category: Yates, D.]]
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[[Category: Amyotrophic lateral sclerosis]]
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[[Category: Class iia histone deacetylase inhibitor]]
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[[Category: Cyclopropanation]]
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[[Category: Huntingtons disease]]
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[[Category: Hydrolase]]
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[[Category: Hydroxamic acid]]
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[[Category: Muscle atrophy]]
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[[Category: Neurodegeneration]]
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[[Category: Sar]]

Revision as of 13:38, 11 December 2013

Template:STRUCTURE 4cbt

Contents

Design, synthesis, and biological evaluation of potent and selective Class IIa HDAC inhibitors as a potential therapy for Huntingtons disease

Template:ABSTRACT PUBMED 24261862

Disease

[HDAC4_HUMAN] Defects in HDAC4 are the cause of brachydactyly-mental retardation syndrome (BDMR) [MIM:600430]. A syndrome resembling the physical anomalies found in Albright hereditary osteodystrophy. Common features are mild facial dysmorphism, congenital heart defects, distinct brachydactyly type E, mental retardation, developmental delay, seizures, autism spectrum disorder, and stocky build. Soft tissue ossification is absent, and there are no abnormalities in parathyroid hormone or calcium metabolism.[1]

Function

[HDAC4_HUMAN] Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Involved in muscle maturation via its interaction with the myocyte enhancer factors such as MEF2A, MEF2C and MEF2D.[2]

About this Structure

4cbt is a 3 chain structure. Full crystallographic information is available from OCA.

Reference

  • Burli RW, Luckhurst CA, Aziz O, Matthews KL, Yates D, Lyons KA, Beconi M, McAllister G, Breccia P, Stott AJ, Penrose SD, Wall M, Lamers MB, Leonard P, Mueller I, Richardson CM, Jarvis R, Stones L, Hughes S, Wishart G, Haughan AF, O'Connell C, Mead T, McNeil H, Vann J, Mangette J, Maillard M, Beaumont V, Munoz-Sanjuan I, Dominguez C. Design, synthesis, and biological evaluation of potent and selective Class IIa histone deacetylase (HDAC) inhibitors as a potential therapy for Huntington's disease. J Med Chem. 2013 Nov 21. PMID:24261862 doi:http://dx.doi.org/10.1021/jm4011884
  1. ↑ Williams SR, Aldred MA, Der Kaloustian VM, Halal F, Gowans G, McLeod DR, Zondag S, Toriello HV, Magenis RE, Elsea SH. Haploinsufficiency of HDAC4 causes brachydactyly mental retardation syndrome, with brachydactyly type E, developmental delays, and behavioral problems. Am J Hum Genet. 2010 Aug 13;87(2):219-28. doi: 10.1016/j.ajhg.2010.07.011. PMID:20691407 doi:10.1016/j.ajhg.2010.07.011
  2. ↑ Wang AH, Bertos NR, Vezmar M, Pelletier N, Crosato M, Heng HH, Th'ng J, Han J, Yang XJ. HDAC4, a human histone deacetylase related to yeast HDA1, is a transcriptional corepressor. Mol Cell Biol. 1999 Nov;19(11):7816-27. PMID:10523670

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