Results 21 to 30 of about 4,995,094 (293)

Biochemical pharmacology of the positive allosteric modulation of the GABAb receptor "in Vitro" and "in Vivo" [PDF]

, 2007
Allosteric modulators of G-protein coupled receptors (GPCRs) interact with binding sites on the receptor molecule that are topographically distinct from the classic orthosteric site.
Gjoni, Tina
core   +1 more source

Allosteric Modulation of Muscarinic Acetylcholine Receptors

Pharmaceuticals, 2010
An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.
Esam E. El-Fakahany, Jan Jakubík
doaj   +1 more source

Conformational transitions and allosteric modulation in a heteromeric glycine receptor

Nature Communications, 2023
Glycine receptors (GlyR) are a critical postsynaptic component of spinal neurons. Here, the auhtors present cryo-EM structures of a heteromeric GlyR in the presence of an antagonist, agonist and agonist with a positive allosteric modulator.
Eric Gibbs, Emily Klemm, David Seiferth, Arvind Kumar, Serban L. Ilca, Philip C. Biggin, Sudha Chakrapani   +6 more
doaj   +1 more source

Development of allosteric modulators of GPCRs for treatment of CNS disorders

Neurobiology of Disease, 2014
The discovery of allosteric modulators of G protein-coupled receptors (GPCRs) provides a promising new strategy with potential for developing novel treatments for a variety of central nervous system (CNS) disorders.
Hilary Highfield Nickols, P. Jeffrey Conn   +1 more
doaj   +1 more source

The unconventional activation of the muscarinic acetylcholine receptor M4R by diverse ligands

Nature Communications, 2022
The authors report the structural characterization of M4R selective allosteric agonist, compound-110, as well as agonist iperoxo and positive allosteric modulator LY2119620.
Jingjing Wang, Meng Wu, Zhangcheng Chen, Lijie Wu, Tian Wang, Dongmei Cao, Huan Wang, Shenhui Liu, Yueming Xu, Fei Li, Junlin Liu, Na Chen, Suwen Zhao, Jianjun Cheng, Sheng Wang, Tian Hua   +15 more
doaj   +1 more source

Allosterism vs. Orthosterism: Recent Findings and Future Perspectives on A2B AR Physio-Pathological Implications

Frontiers in Pharmacology, 2021
The development of GPCR (G-coupled protein receptor) allosteric modulators has attracted increasing interest in the last decades. The use of allosteric modulators in therapy offers several advantages with respect to orthosteric ones, as they can fine ...
Elisabetta Barresi, Claudia Martini, Federico Da Settimo, Giovanni Greco, Sabrina Taliani, Chiara Giacomelli, Maria Letizia Trincavelli   +6 more
doaj   +1 more source

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, Y. Najajreh, Ruthardt, Martin, M. Ruthardt, Ottmann, Oliver G., J. Mahajna, Mian, Afsar Ali, Mian, Afsar A., Metodieva, Anna, Najajreh, Yousef, A. Metodieva, A. A. Mian, O. G. Ottmann   +12 more
core   +1 more source

PTK7 is a positive allosteric modulator of GPR133 signaling in glioblastoma

Cell Reports, 2023
Summary: The adhesion G-protein-coupled receptor GPR133 (ADGRD1) supports growth of the brain malignancy glioblastoma. How the extracellular interactome of GPR133 in glioblastoma modulates signaling remains unknown.
Joshua D. Frenster, Hediye Erdjument-Bromage, Gabriele Stephan, Niklas Ravn-Boess, Shuai Wang, Wenke Liu, Devin Bready, Jordan Wilcox, Björn Kieslich, Manuel Jankovic, Caroline Wilde, Susanne Horn, Norbert Sträter, Ines Liebscher, Torsten Schöneberg, David Fenyo, Thomas A. Neubert, Dimitris G. Placantonakis   +17 more
doaj   +1 more source

Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I [PDF]

, 2012
Background: Chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphatic leukemia (Ph + ALL) are caused by the t(9;22), which fuses BCR to ABL resulting in deregulated ABL-tyrosine kinase activity.
Ruimi, Nili, Martin Ruthardt, Mahajna, Jamal, Khateb, Mamduh, Jamal Mahajna, Ruthardt, Martin, Ottmann, Oliver G., Oliver Gerhard Ottmann, Mian, Afsar Ali, Nili Ruimi, Yousef Najajreh, Afsar Ali Mian, Ottmann, Oliver Gerhard, Susanne Badura, Metodieva, Anna, Najajreh, Yousef, Anna Metodieva, Mamduh Khateb, Badura, Susanne   +18 more
core   +2 more sources

Allosteric modulators enhance agonist efficacy by increasing the residence time of a GPCR in the active state

Nature Communications, 2021
Here, the authors use smFRET to assess the structural dynamics of metabotropic glutamate receptor mGlu2 and show that a positive allosteric modulator or the Gi protein stabilize mGlu2 in the glutamate-induced active state, leading to the full activation ...
Anne-Marinette Cao, Robert B. Quast, Fataneh Fatemi, Philippe Rondard, Jean-Philippe Pin, Emmanuel Margeat   +5 more
doaj   +1 more source