Structural and in vivo characterization of Tubastatin A, a widely used histone deacetylase 6 inhibitor
S Shen, M Svoboda, G Zhang… - ACS medicinal …, 2020 - ACS Publications
… In this work, we provide new insights into this HDAC6i by … for its selective inhibition of HDAC6
by solving the structure of … its functional ability to enhance the levels of Ac-α-tubulin in vitro …
by solving the structure of … its functional ability to enhance the levels of Ac-α-tubulin in vitro …
The disordered N-terminus of HDAC6 is a microtubule-binding domain critical for efficient tubulin deacetylation
K Ustinova, Z Novakova, M Saito, M Meleshin… - Journal of Biological …, 2020 - ASBMB
… We found that HDAC6-microtubule interactions are entirely independent of the catalytic domains
and are … Structural insights into HDAC6 tubulin deacetylation and its selective inhibition. …
and are … Structural insights into HDAC6 tubulin deacetylation and its selective inhibition. …
Exploring new histone deacetylase 6 inhibitors and their effects on reversing the α-tubulin deacetylation and cell morphology changes caused by methamphetamine
… HDAC6-selective inhibitors, we anticipate that indazole could serve as a good capping group
for HDAC6 inhibitors… and introduced diverse zinc-binding groups into the indazole scaffold. …
for HDAC6 inhibitors… and introduced diverse zinc-binding groups into the indazole scaffold. …
HDAC6 as privileged target in drug discovery: A perspective
… structure determinations of HDAC6 CD2 with HDAC6i complexes provided structural and
catalytic mechanism insights into … Unlike tubulin deacetylation by HDAC6, the cortactin-HDAC6 …
catalytic mechanism insights into … Unlike tubulin deacetylation by HDAC6, the cortactin-HDAC6 …
A review of progress in histone deacetylase 6 inhibitors research: structural specificity and functional diversity
XH Zhang, Qin-Ma, HP Wu, MY Khamis… - Journal of medicinal …, 2021 - ACS Publications
… , its selective inhibition of HDAC6 blocked migration and invasion in human CRC cells. Notably,
it … , with an IC 50 value of 199 nM, and specifically upregulated tubulin acetylation levels …
it … , with an IC 50 value of 199 nM, and specifically upregulated tubulin acetylation levels …
Development of first-in-class dual Sirt2/HDAC6 inhibitors as molecular tools for dual inhibition of tubulin deacetylation
L Sinatra, A Vogelmann, F Friedrich… - Journal of medicinal …, 2023 - ACS Publications
… For 32 and 33, we observed a selective inhibition of the targeted enzymes Sirt2 and … To
obtain structural insights into the HDAC6 binding modes of the dual Sirt2/HDAC6 inhibitors 32 …
obtain structural insights into the HDAC6 binding modes of the dual Sirt2/HDAC6 inhibitors 32 …
Structure‐Based Discovery of A Small Molecule Inhibitor of Histone Deacetylase 6 (HDAC6) that Significantly Reduces Alzheimer's Disease Neuropathology
… inhibitor of HDAC6 PB118 in improving acetyl-α-tubulin and … evaluated their activity by the
HDACs enzyme inhibition assay … PB118 had the most selectivity toward HDAC6 enzymes and …
HDACs enzyme inhibition assay … PB118 had the most selectivity toward HDAC6 enzymes and …
Design, synthesis, and biological evaluation of HDAC6 inhibitors targeting L1 loop and serine 531 residue
S Jha, JH Kim, M Kim, AH Nguyen, KH Ali… - European Journal of …, 2024 - Elsevier
… promoted the acetylation of α-tubulin, resulting in microtubule … did not induce any acetylation
of α-tubulin, as expected. Taken … acetylation of α-tubulin via inhibition of HDAC6, leading to …
of α-tubulin, as expected. Taken … acetylation of α-tubulin via inhibition of HDAC6, leading to …
Recent advances in small molecular modulators targeting histone deacetylase 6
… the structural features and biological functions of HDAC6 and … in HDAC6 modulators, including
selective inhibitors, chimeric … Structural insights into HDAC6 tubulin deacetylation and its …
selective inhibitors, chimeric … Structural insights into HDAC6 tubulin deacetylation and its …
Recent development of novel HDAC6 isoform-selective Inhibitors
Y Zhao, T Liang, X Hou, H Fang - Current Medicinal Chemistry, 2021 - ingentaconnect.com
… Abnormal expression of HDAC6 gives rise to cancer, … structure and development of
HDAC6 selective inhibitors. … 47) is a dual inhibitor of HDAC6 and tubulin, and it has an …
HDAC6 selective inhibitors. … 47) is a dual inhibitor of HDAC6 and tubulin, and it has an …