NOVEL INHIBITORS OF HUMAN CARBONIC ANHYDRASE

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14160%2F24%3A00137525" target="_blank" >RIV/00216224:14160/24:00137525 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

NOVEL INHIBITORS OF HUMAN CARBONIC ANHYDRASE

Popis výsledku v původním jazyce

Carbonic anhydrases (CA, EC 4.2.1.1) are metalloenzymes catalyzing the reversible hydration of CO2, thereby affecting the pH and related physiological processes in various organisms. In human bodies, 15 different isoforms of CAs can be found, including two tumor-associated: hCA IX and hCA XII (human CA). These two isoforms are responsible for up-regulated metabolism, growth, and survival of cancer cells. They are involved in spreading metastasis, and correlated with resistance towards chemotherapy or radiotherapy.1 Given the above, it is clear that CA inhibitors are very promising compounds in cancer treatment. However, for now, their crucial limitation is their selectivity towards specific isoenzymes. A new series of inhibitors of tumor-associated CA was designed and synthesized, specifically 1,3,5-triazines containing aminobenzenesulfonamide, piperazine, aniline, and other structural moieties. New compounds' inhibitory activity and selectivity were determined against hCA IX, hCA XII, and hCA II.

Název v anglickém jazyce

NOVEL INHIBITORS OF HUMAN CARBONIC ANHYDRASE

Popis výsledku anglicky

Carbonic anhydrases (CA, EC 4.2.1.1) are metalloenzymes catalyzing the reversible hydration of CO2, thereby affecting the pH and related physiological processes in various organisms. In human bodies, 15 different isoforms of CAs can be found, including two tumor-associated: hCA IX and hCA XII (human CA). These two isoforms are responsible for up-regulated metabolism, growth, and survival of cancer cells. They are involved in spreading metastasis, and correlated with resistance towards chemotherapy or radiotherapy.1 Given the above, it is clear that CA inhibitors are very promising compounds in cancer treatment. However, for now, their crucial limitation is their selectivity towards specific isoenzymes. A new series of inhibitors of tumor-associated CA was designed and synthesized, specifically 1,3,5-triazines containing aminobenzenesulfonamide, piperazine, aniline, and other structural moieties. New compounds' inhibitory activity and selectivity were determined against hCA IX, hCA XII, and hCA II.

Druh

O - Ostatní výsledky

CEP obor

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OECD FORD obor

30104 - Pharmacology and pharmacy

Projekt

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Návaznosti

S - Specificky vyzkum na vysokych skolach

Rok uplatnění

2024

Kód důvěrnosti údajů

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