Non-enzymatic protein targeting agents as a promising strategy for cancer treatment DOI Creative Commons

M. Ambrose,

Jin-Hyung Lee, Aleem Syed

et al.

Frontiers in Drug Discovery, Journal Year: 2025, Volume and Issue: 5

Published: Jan. 29, 2025

Increased research attention has been brought to non-enzymatic protein targeting agents as a new and effective strategy for advancing cancer treatment. To discover this class of anticancer drugs, two molecular approaches the activities proteins have shown promising experimental, preclinical, clinical results. In first approach, selective known PROteolysis-TArgeting Chimeras (PROTACs) employ innate endogenous degradation machinery in cells proteolyze targeted protein. The combination highly PROTACs exploitation cellular pathways provides opportunity treat diseases that were previously deemed incurable due lack enzymatic proteins. second approach targets protein-protein interactions (PPIs) an alternative route alters functional complexes thus significantly influence cell fitness survival. efficiently identify potential chemical leads these approaches, high-throughput screening (HTS) extremely valuable its ability quickly screen large libraries compounds. review paper, we will provide overview developing anti-cancer impact inhibitors.

Language: Английский

P53: A key player in diverse cellular processes including nuclear stress and ribosome biogenesis, highlighting potential therapeutic compounds DOI
Gazmend Temaj, Silvia Chichiarelli, Pelin Telkoparan‐Akillilar

et al.

Biochemical Pharmacology, Journal Year: 2024, Volume and Issue: 226, P. 116332 - 116332

Published: June 1, 2024

Language: Английский

Citations

5
Advances in designing ternary complexes: Integrating in-silico and biochemical methods for PROTAC optimisation in target protein degradation DOI Creative Commons
Shareef Shaik,

Prasanna Kumar Reddy Gayam,

Manish Chaudhary

et al.

Bioorganic Chemistry, Journal Year: 2024, Volume and Issue: 153, P. 107868 - 107868

Published: Oct. 4, 2024

Language: Английский

Citations

5
Targeted regulated cell death with small molecule compounds in colorectal cancer: Current perspectives of targeted therapy and molecular mechanisms DOI
Ru Li, Yongya Wu, Yan Li

et al.

European Journal of Medicinal Chemistry, Journal Year: 2023, Volume and Issue: 265, P. 116040 - 116040

Published: Dec. 12, 2023

Language: Английский

Citations

11
Ubiquitin recruiting chimera: more than just a PROTAC DOI Creative Commons
Tatyana A. Grigoreva, Daria Novikova, Gerry Melino

et al.

Biology Direct, Journal Year: 2024, Volume and Issue: 19(1)

Published: July 9, 2024

Abstract Ubiquitinylation of protein substrates results in various but distinct biological consequences, among which ubiquitin-mediated degradation is most well studied for its therapeutic application. Accordingly, artificially targeted ubiquitin-dependent proteins has evolved into the therapeutically relevant PROTAC technology. This tethered ubiquitinylation targets coupled with a broad assortment modifying E3 ubiquitin ligases been made possible by rational design bi-specific chimeric molecules that bring these proximity. However, forced inflicted binary warheads molecule should not necessarily result can be used to modulate other cellular functions. In this respect it noted diverse set known control their transport, transcriptional activity, and protein-protein interactions. review provides examples potential usage based on non-degradable ubiquitinylation.

Language: Английский

Citations

4
Non-enzymatic protein targeting agents as a promising strategy for cancer treatment DOI Creative Commons

M. Ambrose,

Jin-Hyung Lee, Aleem Syed

et al.

Frontiers in Drug Discovery, Journal Year: 2025, Volume and Issue: 5

Published: Jan. 29, 2025

Increased research attention has been brought to non-enzymatic protein targeting agents as a new and effective strategy for advancing cancer treatment. To discover this class of anticancer drugs, two molecular approaches the activities proteins have shown promising experimental, preclinical, clinical results. In first approach, selective known PROteolysis-TArgeting Chimeras (PROTACs) employ innate endogenous degradation machinery in cells proteolyze targeted protein. The combination highly PROTACs exploitation cellular pathways provides opportunity treat diseases that were previously deemed incurable due lack enzymatic proteins. second approach targets protein-protein interactions (PPIs) an alternative route alters functional complexes thus significantly influence cell fitness survival. efficiently identify potential chemical leads these approaches, high-throughput screening (HTS) extremely valuable its ability quickly screen large libraries compounds. review paper, we will provide overview developing anti-cancer impact inhibitors.

Language: Английский

Citations

0