Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation
Allosteric nanobodies reveal the dynamic range and diverse mechanisms of G-protein-coupled receptor activation
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Tuplin EW, Holahan MR (November 2017). "Aripiprazole, A Drug that Displays Partial Agonism and Functional Selectivity". Current ... Mailman RB, Murthy V (May 2010). "Third generation antipsychotic drugs: partial agonism or receptor functional selectivity?". ... and drug use. In addition to aripiprazoles partial agonism and functional selectivity characteristics, its effectiveness may ... of agonism is a function of more than a drugs inherent properties as well as in vitro demonstration of aripiprazoles partial ...
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Partial agonism. This is a form of MMOA in which only partial efficacy is produced following drug binding to the orthosteric ... the drugs targeted ion channel activity (c); their MMOAs included uncompetitive antagonism and partial agonism. One drug, ... Their MMOAs included agonism, partial agonism, antagonism and allosteric modulation. Two drugs - fulvestrant and mifepristone ... Copeland, R. A., Pompliano, D. L. & Meek, T. D. source for new drugs.. and the nature and number of drug targets. Nature Drug- ...
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The development of a new drug targeting a member of this family requires to take into account the pharmacological profile of ... partial and inverse agonism. Curr Opin Pulm Med 16:1-5. https://doi.org/10.1097/MCP.0b013e328333def8 ... Sriram K, Insel PA (2018) G Protein-coupled receptors as targets for approved drugs: how many targets and how many drugs? Mol ... The initial set of molecules was selected from the ADRB2 (CHEMBL210) target page on ChEMBL [59], in the section "Drugs and ...
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From structure to clinic: Design of a muscarinic M1 receptor agonist with potential to treatment of Alzheimer's disease -...
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