Patent spotlight: small-molecule lysine acetyltransferase inhibitors (KATi)

Pharm Pat Anal. 2020 Jan;9(1):17-28. doi: 10.4155/ppa-2019-0025. Epub 2020 Feb 3.

Abstract

Lysine (or histone) acetyltransferases plays a key role in genome maintenance and gene regulation and dysregulation of acetylation is a recognized feature of many diseases, including several cancers. Here, the patent landscape surrounding lysine acetyltransferase inhibitors (KATi or HATi), with a focus on small-molecule compounds, is outlined and assessed. Overall, the 36 KATi-specific patents found were categorized into two distinct groups: specific small-molecule inhibitors (compounds and molecules) and patents applying KATi for targeted disease treatment. These patents recognize the emergent potential of KATi to significantly impact on the management of many diseases (including multiple cancer types, neurological disorders and immunological syndromes), improving the range of treatments (and drug classes) available for personalized medicine.

Keywords: HAT; KAT; acetylation; acetyltransferase; disease; histone; inhibitor; lysine.

MeSH terms

  • Drug Development* / legislation & jurisprudence
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Humans
  • Lysine Acetyltransferases / antagonists & inhibitors*
  • Molecular Targeted Therapy
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Patents as Topic* / legislation & jurisprudence
  • Small Molecule Libraries / chemistry
  • Small Molecule Libraries / pharmacology*

Substances

  • Enzyme Inhibitors
  • Small Molecule Libraries
  • Lysine Acetyltransferases