lnhibitori histonskih deacetilaza kao protutumorski lijekovi

Scientific paper - Review paper

• Author: Goran Poje
• Author: Zrinka Rajić
• Author's institution: University of Zagreb; Faculty of Pharmacy and Biochemistry; (Department of medicinal chemistry)
• Scientific / art field, discipline and subdiscipline: BIOMEDICINE AND HEALTHCARE; Pharmacy; Pharmacy

Abstract (croatian)

Histone deacetylases (HDACs) catalyze the removal of the
acetyl group from an e-N-acetyl lysine on a histone, resulting in
a more tight DNA structure. In this way, they affect chromatin structure and
gene expression. They catalyze the same reaction on some non-histone proteins.
Inhibition of overexpressed HDACs in tumour cells results in cell cycle arrest,
induction of apoptosis, inhibition of angiogenesis and regulation of cellular
signaling pathways in a survival-negative manner. Out of 4 known HDAC classes,
classes I, II and IV are zinc-dependent enzymes, while class III is NAD+
dependent. All known HDACs inhibitors contain zinc-binding group, responsible
for complexation of Zn2+ from the enzyme's active site. Other main structural
features include cap group and the linker. With respect to the zinc-binding
group, inhibitors can be divided into hydroxamic acids (the most pronounced
ability to chelate Zn2+), carboxylic acids, cyclic peptides, and o-aminoanilides.
Up to date, five HDACs inhibitors have reached the market: vorinostat, belinostat,
and panobinostat (hydroxamic acids), romidepsin (cyclic peptide) and chidamide
(o-aminoanilide). They are used in the therapy of T-cell lymphomas and
multiple myeloma.

• Keywords (croatian): maligne bolesti; tumori; antitumorski lijekovi; citostatici; inhibitori HDAC enzima
• Language: croatian
• Publication type: Scientific paper - Review paper
• Publication status: Published
• Peer review: Peer review - domestic
• Publication version: Published version
• Journal title: Farmaceutski glasnik
• Numbering: vol. 76, no. 4-5, pp. 261-280
• p-ISSN: 0014-8202
• URN:NBN: urn:nbn:hr:163:300936
• Publication: 2020
• Type of resource: Text
• Access conditions: Open access
• Created on: 2020-07-10 15:41:10