lnhibitori histonskih deacetilaza kao protutumorski lijekovi

Znanstveni rad - Pregledni rad

• Autor: Goran Poje
• Autor: Zrinka Rajić
• Autorova ustanova: Sveučilište u Zagrebu; Farmaceutsko-biokemijski fakultet; (Zavod za farmaceutsku kemiju)
• Znanstveno / umjetničko područje, polje i grana: BIOMEDICINA I ZDRAVSTVO; Farmacija; Farmacija

Sažetak (hrvatski)

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.

• Ključne riječi (hrvatski): maligne bolesti; tumori; antitumorski lijekovi; citostatici; inhibitori HDAC enzima
• Jezik: hrvatski
• Vrsta publikacije: Znanstveni rad - Pregledni rad
• Status objave: Objavljen
• Vrsta recenzije: Recenziran - domaća recenzija
• Verzija publikacije: Objavljena verzija rada (izdavačev PDF)
• Naslov časopisa: Farmaceutski glasnik
• Brojčani podaci: vol. 76, br. 4-5, str. 261-280
• p-ISSN: 0014-8202
• URN:NBN: urn:nbn:hr:163:300936
• Datum objave publikacije: 2020
• Vrsta resursa: Tekst
• Prava pristupa: Otvoreni pristup
• Datum i vrijeme pohrane: 2020-07-10 15:41:10