Marek et al., 2018 - Google Patents
Characterization of histone deacetylase 8 (HDAC8) selective inhibition reveals specific active site structural and functional determinantsMarek et al., 2018
View PDF- Document ID
- 6424416104902775218
- Author
- Marek M
- Shaik T
- Heimburg T
- Chakrabarti A
- Lancelot J
- Ramos-Morales E
- Da Veiga C
- Kalinin D
- Melesina J
- Robaa D
- Schmidtkunz K
- Suzuki T
- Holl R
- Ennifar E
- Pierce R
- Jung M
- Sippl W
- Romier C
- Publication year
- Publication venue
- Journal of medicinal chemistry
External Links
Snippet
Metal-dependent histone deacetylases (HDACs) are key epigenetic regulators that represent promising therapeutic targets for the treatment of numerous human diseases. Yet the currently FDA-approved HDAC inhibitors nonspecifically target at least several of the 11 …
- 230000002401 inhibitory effect 0 title abstract description 333
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
Similar Documents
Publication | Publication Date | Title |
---|---|---|
Marek et al. | Characterization of histone deacetylase 8 (HDAC8) selective inhibition reveals specific active site structural and functional determinants | |
Ho et al. | Thirty years of HDAC inhibitors: 2020 insight and hindsight | |
Porter et al. | Entropy as a driver of selectivity for inhibitor binding to histone deacetylase 6 | |
Ali et al. | Lysine acetylation goes global: from epigenetics to metabolism and therapeutics | |
Porter et al. | Histone deacetylase 6-selective inhibitors and the influence of capping groups on hydroxamate-zinc denticity | |
Rodrigues et al. | Design, synthesis, and pharmacological evaluation of novel N-acylhydrazone derivatives as potent histone deacetylase 6/8 dual inhibitors | |
Pontiki et al. | Histone deacetylase inhibitors (HDACIs). Structure—Activity relationships: History and new QSAR perspectives | |
Suzuki et al. | Rapid discovery of highly potent and selective inhibitors of histone deacetylase 8 using click chemistry to generate candidate libraries | |
McAllister et al. | Recent progress in histone demethylase inhibitors | |
Heimburg et al. | Structure-based design and biological characterization of selective histone deacetylase 8 (HDAC8) inhibitors with anti-neuroblastoma activity | |
Osko et al. | Structural basis of catalysis and inhibition of HDAC6 CD1, the enigmatic catalytic domain of histone deacetylase 6 | |
Schiedel et al. | Aminothiazoles as potent and selective Sirt2 inhibitors: a structure–activity relationship study | |
Sammak et al. | Crystal structures and nuclear magnetic resonance studies of the apo form of the c-MYC: MAX bHLHZip complex reveal a helical basic region in the absence of DNA | |
Watson et al. | Insights into the activation mechanism of class I HDAC complexes by inositol phosphates | |
Simon et al. | KATching-up on small molecule modulators of lysine acetyltransferases | |
Osko et al. | Exploring structural determinants of inhibitor affinity and selectivity in complexes with histone deacetylase 6 | |
Ragno et al. | Design, molecular modeling, synthesis, and anti-HIV-1 activity of new indolyl aryl sulfones. Novel derivatives of the indole-2-carboxamide | |
Decroos et al. | Biochemical and structural characterization of HDAC8 mutants associated with Cornelia de Lange syndrome spectrum disorders | |
Decroos et al. | Variable active site loop conformations accommodate the binding of macrocyclic largazole analogues to HDAC8 | |
Leu et al. | Structural basis for the inhibition of HSP70 and DnaK chaperones by small-molecule targeting of a C-terminal allosteric pocket | |
Dowling et al. | Structures of metal-substituted human histone deacetylase 8 provide mechanistic inferences on biological function | |
Fabbrizi et al. | Emerging roles of SIRT5 in metabolism, cancer, and SARS-CoV-2 infection | |
You et al. | Structural basis of sirtuin 6 inhibition by the hydroxamate trichostatin A: implications for protein deacylase drug development | |
Bergman et al. | S-Farnesyl-thiopropionic acid triazoles as potent inhibitors of isoprenylcysteine carboxyl methyltransferase | |
Auzzas et al. | Non-natural macrocyclic inhibitors of histone deacetylases: design, synthesis, and activity |