PUBLICATION
Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity
- Authors
- Porter, N.J., Osko, J.D., Diedrich, D., Kurz, T., Hooker, J.M., Hansen, F.K., Christianson, D.W.
- ID
- ZDB-PUB-191016-13
- Date
- 2018
- Source
- Journal of medicinal chemistry 61: 8054-8060 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
-
- Animals
- Coordination Complexes/chemistry
- Coordination Complexes/metabolism
- Crystallography, X-Ray
- Histone Deacetylase 6/antagonists & inhibitors*
- Histone Deacetylase Inhibitors/chemistry*
- Histone Deacetylase Inhibitors/pharmacology*
- Hydroxamic Acids/chemistry*
- Hydroxamic Acids/metabolism
- Molecular Structure
- Protein Conformation
- Zebrafish/metabolism*
- Zebrafish Proteins/antagonists & inhibitors*
- Zebrafish Proteins/metabolism
- Zinc/chemistry*
- Zinc/metabolism
- PubMed
- 30118224 Full text @ J. Med. Chem.
Citation
Porter, N.J., Osko, J.D., Diedrich, D., Kurz, T., Hooker, J.M., Hansen, F.K., Christianson, D.W. (2018) Histone Deacetylase 6-Selective Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity. Journal of medicinal chemistry. 61:8054-8060.
Abstract
Four crystal structures are presented of histone deacetylase 6 (HDAC6) complexes with para-substituted phenylhydromaxamate inhibitors, including bulky peptoids. These structures provide insight regarding the design of capping groups that confer selectivity for binding to HDAC6, specifically with regard to interactions in a pocket formed by the L1 loop. Capping group interactions may also influence hydroxamate-Zn2+ coordination with monodentate or bidentate geometry.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping