Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015–2021)

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F62690094%3A18470%2F22%3A50019214" target="_blank" >RIV/62690094:18470/22:50019214 - isvavai.cz</a>

Nalezeny alternativní kódy

RIV/00179906:_____/22:10445942

Výsledek na webu

<a href="https://www.sciencedirect.com/science/article/pii/S0223523422004007?via%3Dihub" target="_blank" >https://www.sciencedirect.com/science/article/pii/S0223523422004007?via%3Dihub</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.ejmech.2022.114498" target="_blank" >10.1016/j.ejmech.2022.114498</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015–2021)

Popis výsledku v původním jazyce

Mechanistic target of rapamycin (mTOR) is a highly conserved protein kinase acting as a central regulator of cell functions. The kinase forms two distinct mTOR complexes termed as mTORC1 and mTORC2. Dysregulation of mTOR activity is associated with various pathological conditions. Inhibition of overactivated mTOR represent a rational approach in the treatment of numerous human diseases. Rapamycin is a potent natural inhibitor of mTOR exhibiting significant antitumor and immunosuppressive activity. Derivatization of rapamycin provided rapalogs, the first generation of mTOR inhibitors that selectively inhibit mTORC1 activity. Further interest of research community resulted in creation of the second generation of mTOR inhibitors involving both, mTOR kinase inhibitors and dual phosphoinositide 3-kinase (PI3K)/mTOR inhibitors. Recently, combining advances of first and second generation of mTOR inhibitors yielded in the third generation of inhibitors termed as rapalinks. Nowadays, novel inhibitors belonging to all of the three generations are still under development. These inhibitors help us better to understand role of mTOR in mTOR signaling pathway as well as in diverse human diseases. In this review, we summarize recent reported mTOR inhibitors or methods of use thereof in the treatment of various diseases. © 2022 Elsevier Masson SAS

Název v anglickém jazyce

Contemporary mTOR inhibitor scaffolds to diseases breakdown: A patent review (2015–2021)

Popis výsledku anglicky

Mechanistic target of rapamycin (mTOR) is a highly conserved protein kinase acting as a central regulator of cell functions. The kinase forms two distinct mTOR complexes termed as mTORC1 and mTORC2. Dysregulation of mTOR activity is associated with various pathological conditions. Inhibition of overactivated mTOR represent a rational approach in the treatment of numerous human diseases. Rapamycin is a potent natural inhibitor of mTOR exhibiting significant antitumor and immunosuppressive activity. Derivatization of rapamycin provided rapalogs, the first generation of mTOR inhibitors that selectively inhibit mTORC1 activity. Further interest of research community resulted in creation of the second generation of mTOR inhibitors involving both, mTOR kinase inhibitors and dual phosphoinositide 3-kinase (PI3K)/mTOR inhibitors. Recently, combining advances of first and second generation of mTOR inhibitors yielded in the third generation of inhibitors termed as rapalinks. Nowadays, novel inhibitors belonging to all of the three generations are still under development. These inhibitors help us better to understand role of mTOR in mTOR signaling pathway as well as in diverse human diseases. In this review, we summarize recent reported mTOR inhibitors or methods of use thereof in the treatment of various diseases. © 2022 Elsevier Masson SAS

Druh

J_imp - Článek v periodiku v databázi Web of Science

CEP obor

—

OECD FORD obor

30107 - Medicinal chemistry

Projekt

<a href="/cs/project/GA20-22037S" target="_blank" >GA20-22037S: Terapeutický potenciál nových inhibitorů mTOR v procesu stárnutí.</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2022

Kód důvěrnosti údajů

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

Název periodika

European Journal of Medicinal Chemistry

ISSN

0223-5234

e-ISSN

1768-3254

Svazek periodika

238

Číslo periodika v rámci svazku

August

Stát vydavatele periodika

FR - Francouzská republika

Počet stran výsledku

29

Strana od-do

"Article number: 114498"

Kód UT WoS článku

000810543200004

EID výsledku v databázi Scopus

2-s2.0-85131533377