Results 161 to 170 of about 4,452,404 (339)

Targeting the Spliceosomal Protein USP39 Through Allosteric Ligands and PROTAC‐Induced Degradation

Angewandte Chemie International Edition, EarlyView.
Proteolysis‐targeting chimeras (PROTACs) enable degradation of proteins previously considered undruggable by harnessing the cellular ubiquitin–proteasome system. In this study, Schäfer et al. identify thiazole‐based small molecules that allosterically bind the zinc finger domain of ubiquitin‐specific protease 39 (USP39), a non‐enzymatic scaffold ...
Daniel Schäfer, Cristian Prieto‐Garcia, Jianhui Wang, Marcel Heinz, Vigor Matkovic, Pavel Kielkowski, Sebastian Hasselbeck, Varun Jayeshkumar Shah, Stefan Knapp, Gerhard Hummer, Ivan Dikic, Xinlai Cheng   +11 more
wiley   +1 more source

Discovery of Hit Compounds Targeting the P4 Allosteric Site of K-RAS, Identified through Ensemble-Based Virtual Screening. [PDF]

J Chem Inf Model, 2023
Gomez-Gutierrez P, Rubio-Martinez J, Perez JJ.   +2 more
europepmc   +1 more source

Targeting an allosteric site in dynamin-related protein 1 to inhibit Fis1-mediated mitochondrial dysfunction. [PDF]

Nat Commun, 2023
Rios L, Pokhrel S, Li SJ, Heo G, Haileselassie B, Mochly-Rosen D.   +5 more
europepmc   +1 more source

The N-Terminus of Human Sulfotransferase 2B1b─a Sterol-Sensing Allosteric Site. [PDF]

Biochemistry, 2022
Cook I, Leyh TS.
europepmc   +1 more source

Transplanting allosteric control of enzyme activity by protein–protein interactions: Coupling a regulatory site to the conserved catalytic core

, 2002
Aaron C. Pawlyk, Donald W. Pettigrew
openalex   +1 more source

Distinct roles of the Na ⁺ binding sites in the allosteric coupling mechanism of the glutamate transporter homolog, Glt _Ph

, 2022
Erika Riederer, Pierre Moënne‐Loccoz, Francis I. Valiyaveetil   +2 more
openalex   +2 more sources

Cryo-EM reveals an extrahelical allosteric binding site at the M5 mAChR

Nature Communications
The M5 muscarinic acetylcholine receptor (M5 mAChR) represents a promising therapeutic target for neurological disorders. However, the high conservation of its orthosteric binding site poses significant challenges for drug development.
Wessel A. C. Burger, Jesse I. Mobbs, Bhavika Rana, Jinan Wang, Keya Joshi, Patrick R. Gentry, Mahmuda Yeasmin, Hariprasad Venugopal, Aaron M. Bender, Craig W. Lindsley, Yinglong Miao, Arthur Christopoulos, Celine Valant, David M. Thal   +13 more
doaj   +1 more source

Allosteric Site of ACE-2 as a Drug Target for COVID-19. [PDF]

ACS Pharmacol Transl Sci, 2022
Dutta K.
europepmc   +1 more source

Development of Peptide Glucosyltransferase Inhibitors With Comprehensive Coverage Across Clostridioides difficile Toxin B Sub‐Types

Biotechnology and Bioengineering, EarlyView.
ABSTRACT Clostridioides difficile infection presents an escalating clinical challenge due to the proliferation of hypervirulent and antibiotic‐resistant strains. The primary symptoms of disease, namely colitis and diarrhea, are induced by the release of two toxins: TcdA and TcdB.
Carly M. Catella, Sudeep Sarma, Caroline M. Hinesley, Corey E. Febo, Keith A. Breau, Deniz Durmusoglu, Ethan Purnell, Scott T. Magness, Carol K. Hall, Stefano Menegatti, Nathan Crook   +10 more
wiley   +1 more source

Identification, Synthesis, and Characterization of New Glycogen Phosphorylase Inhibitors Binding to the Allosteric AMP Site

, 2004
Marit Kristiansen, Birgitte Andersen, Lars Iversen, Niels Westergaard   +3 more
openalex   +1 more source