Determining Potency of Inhibitors Targeting Histone Deacetylase 6 by Quantification of Acetylated Tubulin in Cells

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F86652036%3A_____%2F23%3A00578923" target="_blank" >RIV/86652036:_____/23:00578923 - isvavai.cz</a>

Výsledek na webu

<a href="https://link.springer.com/protocol/10.1007/978-1-0716-2788-4_29" target="_blank" >https://link.springer.com/protocol/10.1007/978-1-0716-2788-4_29</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1007/978-1-0716-2788-4_29" target="_blank" >10.1007/978-1-0716-2788-4_29</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Determining Potency of Inhibitors Targeting Histone Deacetylase 6 by Quantification of Acetylated Tubulin in Cells

Popis výsledku v původním jazyce

During the preclinical development of small molecule inhibitors, compounds or compound libraries are typically first screened using purified target enzymes in vitro to select candidates with high potency. In the later stages of the development, however, functional cell-based assays may provide biologically more relevant data. In this chapter, we describe a detailed protocol for determining the potency of inhibitors targeting human histone deacetylase 6 in complex cellular environments. Cells are first treated with a dilution series of tested compounds, cell lysates separated by SDS-PAGE, and electrotransferred to a blotting membrane. The inhibitor potency is then determined indirectly by quantifying the levels of acetylated tubulin as a surrogate readout.

Název v anglickém jazyce

Determining Potency of Inhibitors Targeting Histone Deacetylase 6 by Quantification of Acetylated Tubulin in Cells

Popis výsledku anglicky

During the preclinical development of small molecule inhibitors, compounds or compound libraries are typically first screened using purified target enzymes in vitro to select candidates with high potency. In the later stages of the development, however, functional cell-based assays may provide biologically more relevant data. In this chapter, we describe a detailed protocol for determining the potency of inhibitors targeting human histone deacetylase 6 in complex cellular environments. Cells are first treated with a dilution series of tested compounds, cell lysates separated by SDS-PAGE, and electrotransferred to a blotting membrane. The inhibitor potency is then determined indirectly by quantifying the levels of acetylated tubulin as a surrogate readout.

Druh

C - Kapitola v odborné knize

CEP obor

—

OECD FORD obor

10608 - Biochemistry and molecular biology

Projekt

<a href="/cs/project/GA21-31806S" target="_blank" >GA21-31806S: Ovlivnění strukturních a funkčních charakteristik chaperonu HSP90 prostřednictvím reverzibilní acetylace</a><br>

Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2023

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název knihy nebo sborníku

HDAC/HAT Function Assessment and Inhibitor Development

ISBN

978-1-0716-2788-4

Počet stran výsledku

12

Strana od-do

455-466

Počet stran knihy

511

Název nakladatele

Springer Nature

Místo vydání

New York

Kód UT WoS kapitoly

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