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Molecular Basis of Action of a Small-Molecule Positive Allosteric Modulator Agonist at the Type 1 Cholecystokinin Holoreceptor.

Desai AJ, Mechin I, Nagarajan K, Valant C, Wootten D, Lam PCH, Orry A, Abagyan R, Nair A, Sexton PM, Christopoulos A, Miller LJ.

Mol Pharmacol. 2019 Mar;95(3):245-259. doi: 10.1124/mol.118.114082. Epub 2018 Dec 27.


Elimination of a cholecystokinin receptor agonist 'trigger' in an effort to develop positive allosteric modulators without intrinsic agonist activity.

Desai AJ, Henke BR, Miller LJ.

Bioorg Med Chem Lett. 2015 May 1;25(9):1849-55. doi: 10.1016/j.bmcl.2015.03.051. Epub 2015 Mar 24.


Molecular Mechanism of Action of Triazolobenzodiazepinone Agonists of the Type 1 Cholecystokinin Receptor. Possible Cooperativity across the Receptor Homodimeric Complex.

Desai AJ, Lam PC, Orry A, Abagyan R, Christopoulos A, Sexton PM, Miller LJ.

J Med Chem. 2015 Dec 24;58(24):9562-77. doi: 10.1021/acs.jmedchem.5b01110. Epub 2015 Dec 10.


Metabolic Actions of the Type 1 Cholecystokinin Receptor: Its Potential as a Therapeutic Target.

Miller LJ, Desai AJ.

Trends Endocrinol Metab. 2016 Sep;27(9):609-619. doi: 10.1016/j.tem.2016.04.002. Epub 2016 May 4. Review.


Development of a highly selective allosteric antagonist radioligand for the type 1 cholecystokinin receptor and elucidation of its molecular basis of binding.

Dong M, Vattelana AM, Lam PC, Orry AJ, Abagyan R, Christopoulos A, Sexton PM, Haines DR, Miller LJ.

Mol Pharmacol. 2015 Jan;87(1):130-40. doi: 10.1124/mol.114.095430. Epub 2014 Oct 15.


SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. I. In vitro studies.

Bignon E, Bachy A, Boigegrain R, Brodin R, Cottineau M, Gully D, Herbert JM, Keane P, Labie C, Molimard JC, Olliero D, Oury-Donat F, Petereau C, Prabonnaud V, Rockstroh MP, Schaeffer P, Servant O, Thurneyssen O, Soubrié P, Pascal M, Maffrand JP, Le Fur G.

J Pharmacol Exp Ther. 1999 May;289(2):742-51.


The biologically crucial C terminus of cholecystokinin and the non-peptide agonist SR-146,131 share a common binding site in the human CCK1 receptor. Evidence for a crucial role of Met-121 in the activation process.

Escrieut C, Gigoux V, Archer E, Verrier S, Maigret B, Behrendt R, Moroder L, Bignon E, Silvente-Poirot S, Pradayrol L, Fourmy D.

J Biol Chem. 2002 Mar 1;277(9):7546-55. Epub 2001 Nov 27.


A type 1 cholecystokinin receptor mutant that mimics the dysfunction observed for wild type receptor in a high cholesterol environment.

Desai AJ, Harikumar KG, Miller LJ.

J Biol Chem. 2014 Jun 27;289(26):18314-26. doi: 10.1074/jbc.M114.570200. Epub 2014 May 13.


Small-Molecule Positive Allosteric Modulators of the β2-Adrenoceptor Isolated from DNA-Encoded Libraries.

Ahn S, Pani B, Kahsai AW, Olsen EK, Husemoen G, Vestergaard M, Jin L, Zhao S, Wingler LM, Rambarat PK, Simhal RK, Xu TT, Sun LD, Shim PJ, Staus DP, Huang LY, Franch T, Chen X, Lefkowitz RJ.

Mol Pharmacol. 2018 Aug;94(2):850-861. doi: 10.1124/mol.118.111948. Epub 2018 May 16.


Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors.

Croy CH, Schober DA, Xiao H, Quets A, Christopoulos A, Felder CC.

Mol Pharmacol. 2014 Jul;86(1):106-15. doi: 10.1124/mol.114.091751. Epub 2014 May 7.


SR146131: a new potent, orally active, and selective nonpeptide cholecystokinin subtype 1 receptor agonist. II. In vivo pharmacological characterization.

Bignon E, Alonso R, Arnone M, Boigegrain R, Brodin R, Gueudet C, Héaulme M, Keane P, Landi M, Molimard JC, Olliero D, Poncelet M, Seban E, Simiand J, Soubrié P, Pascal M, Maffrand JP, Le Fur G.

J Pharmacol Exp Ther. 1999 May;289(2):752-61.


Identification of tyrosine 189 and asparagine 358 of the cholecystokinin 2 receptor in direct interaction with the crucial C-terminal amide of cholecystokinin by molecular modeling, site-directed mutagenesis, and structure/affinity studies.

Galés C, Poirot M, Taillefer J, Maigret B, Martinez J, Moroder L, Escrieut C, Pradayrol L, Fourmy D, Silvente-Poirot S.

Mol Pharmacol. 2003 May;63(5):973-82.


Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators.

Berizzi AE, Gentry PR, Rueda P, Den Hoedt S, Sexton PM, Langmead CJ, Christopoulos A.

Mol Pharmacol. 2016 Oct;90(4):427-36. doi: 10.1124/mol.116.104182. Epub 2016 Jul 26.


Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Nguyen AT, Vecchio EA, Thomas T, Nguyen TD, Aurelio L, Scammells PJ, White PJ, Sexton PM, Gregory KJ, May LT, Christopoulos A.

Mol Pharmacol. 2016 Dec;90(6):715-725. Epub 2016 Sep 28.


Measurement of intermolecular distances for the natural agonist Peptide docked at the cholecystokinin receptor expressed in situ using fluorescence resonance energy transfer.

Harikumar KG, Pinon DI, Wessels WS, Dawson ES, Lybrand TP, Prendergast FG, Miller LJ.

Mol Pharmacol. 2004 Jan;65(1):28-35.


Benzodiazepine ligands can act as allosteric modulators of the Type 1 cholecystokinin receptor.

Gao F, Sexton PM, Christopoulos A, Miller LJ.

Bioorg Med Chem Lett. 2008 Aug 1;18(15):4401-4. doi: 10.1016/j.bmcl.2008.06.053. Epub 2008 Jun 20.


Fluorescence polarization screening for allosteric small molecule ligands of the cholecystokinin receptor.

Harikumar KG, Cawston EE, Miller LJ.

Assay Drug Dev Technol. 2011 Aug;9(4):394-402. doi: 10.1089/adt.2010.0310. Epub 2011 Mar 11.


SR146131, a cholecystokinin-A receptor agonist, antagonizes prepulse inhibition deficits produced by dizocilpine and DOI.

Shilling PD, Feifel D.

Psychopharmacology (Berl). 2002 Nov;164(3):285-93. Epub 2002 Sep 4.


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