evolution of inhibitors, challenges, and future directions
Nika Strašek (Avtor), Matic Proj (Avtor), Christian Steinebach (Avtor), Matej Sova (Avtor), Izidor Sosič (Avtor)

Povzetek

The increasing incidence of inflammatory and malignant diseases signifies the need to develop first-in-class drugs with novel mechanisms of action. In this respect, the transforming growth factor (TGF)-β-activated kinase 1 (TAK1), an essential part of several signaling pathways, is considered relevant and promising. This manuscript provides a brief overview of the signal transduction orchestrated by TAK1 within these pathways, followed by an in-depth and thorough analysis of the chemical matter demonstrated to inhibit this kinase. Special attention is given to the selectivity profiling of inhibitors, as well as to the outcomes of their biological characterization. Because published TAK1 inhibitors differ significantly in their kinome selectivity, active-site binding, and biological activity, we hope that this review will allow a judicial estimation of their quality and usefulness for TAK1-addressing assays. Our thoughts on the perspectives and possible developments of the field are also provided to assist scientists who are involved in the design and development of TAK1-targeting modulators.

Ključne besede

transforming growth factor-β-activated kinase 1;inhibitors;inflammation;tumor necrosis factor;signaling pathways;structure-activity relationship;

Podatki

Jezik: Angleški jezik
Leto izida:
Tipologija: 1.02 - Pregledni znanstveni članek
Organizacija: UL FFA - Fakulteta za farmacijo
UDK: 615.4:54
COBISS: 224969475 Povezava se bo odprla v novem oknu
ISSN: 1879-016X
Št. ogledov: 23
Št. prenosov: 9
Ocena: 0 (0 glasov)
Metapodatki: JSON JSON-RDF JSON-LD TURTLE N-TRIPLES XML RDFA MICRODATA DC-XML DC-RDF RDF

Ostali podatki

Sekundarni jezik: Slovenski jezik
Sekundarne ključne besede: transformacijski rastni faktor-β-aktivirana kinaza 1;inhibitorji;vnetje;faktor tumorske nekroze;signalne poti;razmerje struktura-aktivnost;Farmacevtska kemija;
Vrsta dela (COBISS): Članek v reviji
Strani: <v tisku>
Letnik: ǂVol. ǂ
Zvezek: [article no.] 108810
Čas izdaje: 2025
DOI: 10.1016/j.pharmthera.2025.108810
ID: 25877355