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The Glycine Receptor Allosteric Ligands Library (GRALL)

Adrien H Cerdan, Marion Sisquellas, Gilberto Pereira, Diego E Barreto Gomes, Jean-Pierre Changeux, Marco Cecchini, Arne Elofsson
2020 Bioinformatics  
Availability The GRALL library is distributed as a web-accessible database at the following link:  ...  Motivation Glycine receptors (GlyR) mediate fast inhibitory neurotransmission in the brain and have been recognized as key pharmacological targets for pain.  ...  Acknowledgements For the preparation of ligands, access to HPC resources of the University of Strasbourg (Mesocentre) is gratefully acknowledged.  ... 
doi:10.1093/bioinformatics/btaa170 pmid:32163115 pmcid:PMC7267813 fatcat:wpqqmkvgxnc5pdyad6apdb5lua

Rational design of allosteric modulators: challenges and successes

Alexios Chatzigoulas, Zoe Cournia
2021 Zenodo  
In this review article, we highlight the advantages and disadvantages of allosteric modulators and present structure-based and ligand-based drug design methodologies for the identification of allosteric  ...  have led to exciting advancements of designing bioactive allosteric ligands rationally.  ...  Glycine receptors Glycine receptors (GlyRs) are pentameric glycine-gated chloride ion channels with a critical role in CNS that mediate inhibitory neurotransmission in the spinal cord and brain stem and  ... 
doi:10.5281/zenodo.4889093 fatcat:4o3cx7wrgja35dvjfbmjoac4v4

Jahrestagung der Deutschen, Österreichischen und Schweizerischen Gesellschaften für Hämatologie und Onkologie. Basel, 30.09.–04.10. 2011, pp 1-89

2011 Onkologie (Basel)  
Chemokine receptors, such as CXCR4 and CXCR5, in concert with adhesion molecules (VLA-4 and others), regulate CLL cell trafficking and tissue homing via tissue gradients of the respective ligands.  ...  TNF family members (CD40 ligand, BAFF, APRIL) activate CLL cells via corresponding receptors (BCMA, BAFF-R, TACI), promoting immune recognition and/or survival and expansion of the leukemia cells.  ...  The CB1 antagonist LY320135 or JTE-907, a selective CB2 inverse ligand agonist were used to confirm involvement of CB1 (mainly expressed in brain tissue) or CB2 (expression in hematologic/lymphoid cells  ... 
doi:10.1159/000333299 fatcat:ciesjvjdxzds5fgtsxclqaovde