Results 91 to 100 of about 5,184,182 (156)

Discovering Uncharted Binding Pockets on E3 Ligases Leads to the Identification of FBW7 Allosteric Modulators

Advanced Science
E3 ligases are key regulators of the ubiquitin‐proteasome system (UPS) and have emerged as attractive drug target candidates for precise therapeutic intervention.
Míriam Martínez‐Cartró, Álvaro Serrano‐Morrás, Andrea Bertran‐Mostazo, Roger Castaño‐Muñiz, Salvatore Scaffidi, Varbina Ivanova, Noémi Csorba, József Simon, Péter Ábrányi‐Balogh, Yunfeng Li, György M. Keserü, Bing Hao, Xavier Barril, Carles Galdeano   +13 more
doaj   +1 more source

Alkylamine-tethered molecules recruit FBXO22 for targeted protein degradation

Targeted protein degradation (TPD) relies on small molecules to recruit proteins to E3 ligases to induce their ubiquitylation and degradation by the proteasome. Only a few of the approximately 600 human E3 ligases are currently amenable to this strategy.
Offensperger, F., Yang, K., Dong, K., Zuber, J., Gygi, S., Scholes, N., Farnung, J., Cisneros, J., Sanchez Avila, J., Tin, G., Winter, G., Andersch, F., Horstmann, C., Fellner, M., Kagiou, C., Paulo, J., Hannich, J., Liwocha, J., Hinterndorfer, M., Kubicek, S., Schulman, B.   +20 more
core   +1 more source

Discovery and mechanism verification of first-in-class hydrophobic tagging-based degraders of HBV core protein

Acta Pharmaceutica Sinica B
Interfering hepatitis B virus (HBV) capsid assembly holds promise as a therapeutic approach for chronic hepatitis B (CHB). Novel anti-HBV agents are urgently needed to overcome drug resistance challenges, with targeted protein degradation (TPD) emerging ...
Shujing Xu, Ya Wang, Dazhou Shi, Shuo Wang, Lijun Qiao, Ge Yang, Yang Zhou, Xinyong Liu, Shuo Wu, Yuhuan Li, Peng Zhan   +10 more
doaj   +1 more source

Evolution of proteolysis-targeting chimeras (PROTAC) technology to overcome challenges of antimicrobial resistance

npj Antimicrobials and Resistance
Targeted protein degradation (TPD) is an innovative therapeutic approach that bypasses traditional drug inhibition methods. Proteolysis-targeting chimeras (PROTACs) are bifunctional molecules that harness degradation machinery to remove target proteins ...
Dhanashree N. Sarwan, Pramod B. Khedekar, Ritesh P. Bhole, Rupesh V. Chikhale   +3 more
doaj   +1 more source

Recent advances in targeting protein degradation for tumor immunotherapy

Journal of Hematology & Oncology
Immunotherapy has revolutionized the landscape of cancer treatment, yet its efficacy is often limited by drug resistance, the immunosuppressive tumor microenvironment (TME), and the “undruggable” nature of key immunoregulatory proteins.
Shuai Li, Yushan Jin, Huanhuan Wu, Hong Yuan, Jingyuan Zhao   +4 more
doaj   +1 more source

HSP70 Interactome‐Mediated Proteolysis Targeting Chimera (HSP70‐PROTAC) for Ferroptosis‐Driven Cancer Treatment

Advanced Science
Targeted protein degradation (TPD) represents a transformative therapeutic paradigm that harnesses the cellular degradation machinery to pharmacologically eliminate disease‐causing proteins with aberrant expression.
Jinyun Dong, Yulong Li, Hui Liang, Zumei Wu, Shiqun Wang, Yichao Wang, Jieyu Xu, Yanning Lan, Maohua Cai, Guangzhao Pan, Haiyan Yang, Kai Miao, Zhe‐Sheng Chen, Fangfang Tao, Xuelei Ma, Jiang‐Jiang Qin   +15 more
doaj   +1 more source

Delivering Degradation: Nanomedicine and Programmable Proximity Platforms for Targeted Protein Degradation. [PDF]

Pharmaceutics
Amin A, Nawaz T, Oliveira Ferreira O, Santana de Oliveira M.   +3 more
europepmc   +1 more source

Targeted protein degradation with small molecules for cancer immunotherapy

Immunotherapy has transformed cancer treatment, marked by the approval of numerous antibody-based drugs. However, the limitations of antibodies in pharmacokinetics including long half-lives, limited oral bioavailability and immunogenicity, have prompted ...
Zichao Yang, Jianwei Xu, Xixiang Yang, Jianjun Chen   +3 more
core   +1 more source

Ubiquitin receptor-mediated, ubiquitin-independent targeted protein degradation via 26<i>S</i> proteasomes. [PDF]

Sci Adv
Park SH, Jang Y, Lee SY, Kim E, Jeong D, Byun I, Kim J, Yang J, Lee CH, Han D, Nam JH, Lee MJ.   +11 more
europepmc   +1 more source

Development of High-Efficiency Mitochondrial Protease Targeting Chimeras (MtPTACs) for Targeted Degradation of POLRMT and Beyond. [PDF]

JACS Au
Chen C, Liu L, Li X, Shi Y, Zhou J, Huang L, Zeng L, Feng D, Wang Y, Nie X, Huang Q, Wu Y, Pang S, Xu J, Xu S, Yao H.   +15 more
europepmc   +1 more source