2. Academic Validation
  3. Trapoxin A Analogue as a Selective Nanomolar Inhibitor of HDAC11

Trapoxin A Analogue as a Selective Nanomolar Inhibitor of HDAC11

  • ACS Chem Biol. 2023 Apr 21;18(4):803-809. doi: 10.1021/acschembio.2c00840.
Thanh Tu Ho 1,  Changmin Peng 2,  Edward Seto 2,  Hening Lin 1 3
Affiliations

Affiliations

  • 1 Department of Chemistry and Chemical Biology, Cornell University, Ithaca, New York 14853, United States.
  • 2 Department of Biochemistry & Molecular Medicine, School of Medicine & Health Sciences, George Washington Cancer Center, George Washington University, Washington, District of Columbia 20037, United States.
  • 3 Howard Hughes Medical Institute, Cornell University, Ithaca, New York 14853, United States.
PMID: 36977486 DOI: 10.1021/acschembio.2c00840
Abstract

Histone deacetylases (HDACs) are Enzymes that regulate many important biological pathways. There is a need for the development of isoform-selective HDAC inhibitors for further biological applications. Here, we report the development of trapoxin A analogues as potent and selective inhibitors of HDAC11, an enzyme that can efficiently remove long-chain fatty acyl groups from proteins. In particular, we show that one of the trapoxin A analogues, TD034, has nanomolar potency in enzymatic assays. We show that in cells, TD034 is active at low micromolar concentrations and inhibits the defatty acylation of SHMT2, a known HDAC11 substrate. The high potency and selectivity of TD034 would permit further development of HDAC11 inhibitors for biological and therapeutic applications.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-176542
    HDAC11抑制剂
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