Results 121 to 130 of about 4,452,404 (339)
Advanced Science, EarlyView.This study reports a novel targeted protein degradation strategy termed “HSP70‐PROTAC” that recruits Hsc70 complex to a target protein for inducing degradation. Among them, GDAz‐3 exhibits effective GPX4 degradation activity via UPS/CMA processes, triggering ferroptosis‐driven anticancer activity in vitro and in vivo.
Jinyun Dong +15 more
wiley +1 more source
Advanced Science, EarlyView.A mutually exclusive screening system is established to identify negative regulators of highly plastic genes. Dual specificity phosphatase (DUSP9) is a novel negative regulatory molecule of PD‐L1 by dephosphorylating STAT3, and acts as a target molecule in combination with PD‐1 antibody for tumor immunotherapy and a new clinical biomarker for ...
Yuzhe Hu +9 more
wiley +1 more source
Advanced Science, EarlyView.Here, the study shows for the first time that Forsythoside E (FE) can promote PKM2 tetramerization by binding to its K311 site. Furthermore, it induces metabolic reprogramming of macrophages and inhibits NLRP3 expression. Finally, it can alleviate sepsis‐induced liver injury by promoting M2 anti‐inflammatory polarization.
Bingxin Wu +8 more
wiley +1 more source
Frontiers in Molecular BiosciencesAnti-COVID19 drugs, such as nirmatrelvir, have been developed targeting the SARS-CoV-2 main protease, Mpro, based on the critical requirement of its proteolytic processing of the viral polyproteins into functional proteins essential for viral replication.
Asma Fatima +3 more
doaj +1 more source
Omicron P132H of SARS-CoV-2 Mpro is an allosteric mutant involved in modulating the dynamics of catalytic site entry loop [PDF]
, 2023 Zahoor Ahmad Bhat +4 more
openalex +1 more source
Citation: 'allosteric site' in the IUPAC Compendium of Chemical Terminology, 5th ed.; International Union of Pure and Applied Chemistry; 2025. Online version 5.0.0, 2025. 10.1351/goldbook.14107 • License: The IUPAC Gold Book is licensed under Creative Commons Attribution-ShareAlike CC BY-SA 4.0 International for individual terms.
openaire +1 more source
Advanced Science, EarlyView.Our research reveals that small‐molecule icariin (ICA) directly binds Ras‐GTPase‐activating protein SH3 domain‐binding protein 1 (G3BP1), inducing conformational change and oligomerization. This interaction confers neuroprotection by recruiting insulin‐like growth factor 2 mRNA‐binding protein 1 (IGF2BP1) and modulating N6‐methyladenosine (m6A ...
Ling Li +17 more
wiley +1 more source
Biochemistry, 2014 Protein tyrosine phosphatases (PTPs) have been the subject of considerable pharmaceutical-design efforts because of the ubiquitous connections between misregulation of PTP activity and human disease. PTP-inhibitor discovery has been hampered, however, by
C. Chio, C. S. Lim, Anthony C. Bishop
semanticscholar +1 more source
Advanced Science, EarlyView.Halorotetin B, a novel small‐molecule terpenoid identified from an edible marine ascidian, exhibits strong anti‐tumor activity both in vitro and in vivo through direct targeting UBE2C to induce tumor cell cycle arrest and then lead tumor cell senescence. As a newly discovered UBE2C inhibitor, Halorotetin B can serve as a novel potential cell senescence
Shanhao Han +6 more
wiley +1 more source
Unraveling the Allosteric Cross-Talk Between Coactivator Peptide and Ligand Binding Site in Glucocorticoid Receptor [PDF]
, 2021 Giuseppina La Sala +5 more
openalex +1 more source