Results 31 to 40 of about 151,004 (296)
p185(BCR/ABL) has a lower sensitivity than p210(BCR/ABL) to the allosteric inhibitor GNF-2 in Philadelphia chromosome-positive acute lymphatic leukemia [PDF]
, 2011 Background: The t(9;22) translocation leads to the formation of the chimeric breakpoint cluster region/c-abl oncogene 1 (BCR/ABL) fusion gene on der22, the Philadelphia chromosome.
Mahajna, Jamal +12 more
core +1 more source
Discovery of Potential GSK-3β Allosteric Modulators for Alzheimer’s Disease [PDF]
, 2023 Glycogen Synthase Kinase-3 beta (GSK-3β) is a validated target-enzyme associated with Alzheimer’s Disease (AD). Usage of allosteric inhibitors of this enzyme represents a valid and promising therapeutic strategy due to their selective and subtle ...
Alexander, Tropsha +6 more
core +2 more sources
Antibodies targeting enzyme inhibition as potential tools for research and drug development
Biomolecular Concepts, 2021 Antibodies have transformed biomedical research and are now being used for different experimental applications. Generally, the interaction of enzymes with their specific antibodies can lead to a reduction in their enzymatic activity.
Pérez de la Lastra José Manuel +5 more
doaj +1 more source
Dynamic extracellular vestibule of human SERT: unveiling druggable potential with novel high-affinity allosteric inhibitors [PDF]
, 2023 The serotonin transporter (SERT) tightly regulates synaptic serotonin levels and has been the primary target of antidepressants. Binding of inhibitors to the allosteric site of human SERT (hSERT) impedes the dissociation of antidepressants bound at the ...
Benny, Bang-Andersen +6 more
core +1 more source
Molecules, 2020 The polypeptide backbone of proteins is held together by two main types of covalent bonds: the peptide bonds that link the amino acid residues and the disulfide bonds that link pairs of cysteine amino acids. Disulfide bonds form as a protein folds in the
Philip J. Hogg
doaj +1 more source
Pharmaceutics, 2022 The acquisition of penicillin-binding protein (PBP) 2a in resistant strains of Staphylococcus aureus allows for the continuous production of cell walls even after the inactivation of intrinsic PBPs. Thus, the discovery of novel therapeutics with enhanced
Jamiu Olaseni Aribisala, Saheed Sabiu
doaj +1 more source
Bohr equation and the lost allosteric Bohr effects in symmetry
Biophysics and Physicobiology, 2019 Bohr, Hasselbalch and Krogh demonstrated a group of sigmoid curves under various carbon dioxide contents in 1904. Hill fitted these curves in 1910 with Hill equation without the physical meanings of Hill coefficient and dissociation constant.
Lihsin Lee
doaj +1 more source
Unravelling the allosteric binding mode of αD-VxXXB at nicotinic acetylcholine receptors
Frontiers in Pharmacology, 2023 αD-conotoxins are 11 kDa homodimers that potently inhibit nicotinic acetylcholine receptors (nAChRs) through a non-competitive (allosteric) mechanism. In this study, we describe the allosteric binding mode of the granulin-like C-terminal (CTD) of VxXXB ...
Thao NT Ho +2 more
doaj +1 more source
Antibodies, 2018 Therapeutic antibodies have shifted the paradigm of disease treatments from small molecules to biologics, especially in cancer therapy. Despite the increasing number of antibody candidates, much remains unknown about the antibody and how its various ...
Chinh Tran-To Su +3 more
doaj +1 more source
PASSer2.0: Accurate Prediction of Protein Allosteric Sites Through Automated Machine Learning [PDF]
, 2021 Allostery is a fundamental process in regulating proteins’ activity. The discovery, design and development of allosteric drugs demand for better identification of allosteric sites.
Sian, Xiao, Peng, Tao, Hao, Tian
core +2 more sources