Search Results - "Pinon, Delia"

Transmembrane Segment IV Contributes a Functionally Important Interface for Oligomerization of the Class II G Protein-coupled Secretin Receptor by Harikumar, Kaleeckal G., Pinon, Delia I., Miller, Laurence J.

“…Oligomerization of the Class II G protein-coupled secretin receptor has been reported, but the molecular basis for this and its functional significance have…”
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Glucagon-like peptide-1 receptor dimerization differentially regulates agonist signaling but does not affect small molecule allostery by Harikumar, Kaleeckal G, Wootten, Denise, Pinon, Delia I, Koole, Cassandra, Ball, Alicja M, Furness, Sebastian G. B, Graham, Bim, Dong, Maoqing, Christopoulos, Arthur, Miller, Laurence J, Sexton, Patrick M

“…The glucagon-like peptide-1 receptor (GLP-1R) is a family B G protein-coupled receptor and an important drug target for the treatment of type II diabetes, with…”
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Spatial Approximations between Residues 6 and 12 in the Amino-terminal Region of Glucagon-like Peptide 1 and Its Receptor: A REGION CRITICAL FOR BIOLOGICAL ACTIVITY by Chen, Quan, Pinon, Delia I, Miller, Laurence J, Dong, Maoqing

“…Understanding the molecular basis of natural ligand binding and activation of the glucagon-like peptide 1 (GLP1) receptor may facilitate the development of…”
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Molecular Basis of Glucagon-like Peptide 1 Docking to Its Intact Receptor Studied with Carboxyl-terminal Photolabile Probes by Chen, Quan, Pinon, Delia I., Miller, Laurence J., Dong, Maoqing

“…The glucagon-like peptide 1 (GLP1) receptor is a member of Family B G protein-coupled receptors and represents an important drug target for type 2 diabetes…”
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Refinement of Glucagon-like Peptide 1 Docking to Its Intact Receptor Using Mid-region Photolabile Probes and Molecular Modeling by Miller, Laurence J., Chen, Quan, Lam, Polo C.-H., Pinon, Delia I., Sexton, Patrick M., Abagyan, Ruben, Dong, Maoqing

“…The glucagon-like peptide 1 (GLP1) receptor is an important drug target within the B family of G protein-coupled receptors. Its natural agonist ligand, GLP1,…”
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Mapping spatial approximations between the amino terminus of secretin and each of the extracellular loops of its receptor using cysteine trapping by Dong, Maoqing, Xu, Xiequn, Ball, Alicja M., Makhoul, Joshua A., Lam, Polo C.‐H., Pinon, Delia I., Orry, Andrew, Sexton, Patrick M., Abagyan, Ruben, Miller, Laurence J.

“…While it is evident that the carboxyl‐terminal region of natural peptide ligands bind to the amino‐terminal domain of class B GPCRs, how their biologically…”
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Insights into the Structural Basis of Endogenous Agonist Activation of Family B G Protein-Coupled Receptors by Dong, Maoqing, Gao, Fan, Pinon, Delia I, Miller, Laurence J

“…Agonist drugs targeting the glucagon-like peptide-1 (GLP1) receptor represent important additions to the clinical management of patients with diabetes…”
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Importance of Each Residue within Secretin for Receptor Binding and Biological Activity by Dong, Maoqing, Le, Angela, Te, Jerez A, Pinon, Delia I, Bordner, Andrew J, Miller, Laurence J

“…Secretin is a linear 27-residue peptide hormone that stimulates pancreatic and biliary ductular bicarbonate and water secretion by acting at its family B G…”
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Molecular Basis of Secretin Docking to Its Intact Receptor Using Multiple Photolabile Probes Distributed throughout the Pharmacophore by Dong, Maoqing, Lam, Polo C.-H., Pinon, Delia I., Hosohata, Keiko, Orry, Andrew, Sexton, Patrick M., Abagyan, Ruben, Miller, Laurence J.

“…The molecular basis of ligand binding and activation of family B G protein-coupled receptors is not yet clear due to the lack of insight into the structure of…”
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Site of action of a pentapeptide agonist at the glucagon-like peptide-1 receptor. Insight into a small molecule agonist-binding pocket by Dong, Maoqing, Pinon, Delia I., Miller, Laurence J.

“…The development of small molecule agonists for class B G protein-coupled receptors (GPCRs) has been quite challenging. With proof-of-concept that exenatide,…”
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Insights into the impact of phenolic residue incorporation at each position along secretin for receptor binding and biological activity by Dong, Maoqing, Pinon, Delia I., Miller, Laurence J.

“…Understanding of the structural importance of each position along a peptide ligand can provide important insights into the molecular basis for its receptor…”
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Lactam Constraints Provide Insights into the Receptor-Bound Conformation of Secretin and Stabilize a Receptor Antagonist by Dong, Maoqing, Te, Jerez A, Xu, Xiequn, Wang, Jinhui, Pinon, Delia I, Storjohann, Laura, Bordner, Andrew J, Miller, Laurence J

“…The natural ligands for family B G protein-coupled receptors are moderate-length linear peptides having diffuse pharmacophores. The amino-terminal regions of…”
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Spatial approximation between secretin residue five and the third extracellular loop of its receptor provides new insight into the molecular basis of natural agonist binding by Dong, Maoqing, Lam, Polo C-H, Pinon, Delia I, Sexton, Patrick M, Abagyan, Ruben, Miller, Laurence J

“…The amino terminus of class II G protein-coupled receptors plays an important role in ligand binding and receptor activation. Understanding of the conformation…”
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Possible endogenous agonist mechanism for the activation of secretin family G protein-coupled receptors by Dong, Maoqing, Pinon, Delia I, Asmann, Yan W, Miller, Laurence J

“…The class B family of G protein-coupled receptors contains several potentially important drug targets, yet our understanding of the molecular basis of ligand…”
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Elucidation of the Molecular Basis of Cholecystokinin Peptide Docking to Its Receptor Using Site-Specific Intrinsic Photoaffinity Labeling and Molecular Modeling by Dong, Maoqing, Lam, Polo C.-H, Pinon, Delia I, Abagyan, Ruben, Miller, Laurence J

“…G protein-coupled receptors represent the largest family of receptors and the major target of current drug development efforts. Understanding of the mechanisms…”
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Elucidation of the active conformation of the amino terminus of receptor-bound secretin using intramolecular disulfide bond constraints by Dong, Maoqing, Pinon, Delia I., Bordner, Andrew J., Miller, Laurence J.

“…Family B G protein-coupled receptors include several potentially important drug targets, yet our understanding of the molecular basis of ligand binding to and…”
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Spatial Approximation between the Amino Terminus of a Peptide Agonist and the Top of the Sixth Transmembrane Segment of the Secretin Receptor by Dong, Maoqing, Li, Zhijun, Pinon, Delia I., Lybrand, Terry P., Miller, Laurence J.

“…Distinct spatial approximations between residues within the secretin pharmacophore and its receptor can provide important constraints for modeling this…”
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Fluorescent Indicators Distributed throughout the Pharmacophore of Cholecystokinin Provide Insights into Distinct Modes of Binding and Activation of Type A and B Cholecystokinin Receptors by Harikumar, Kaleeckal G., Pinon, Delia I., Miller, Laurence J.

“…Ligand probes with fluorescent indicators positioned throughout the pharmacophoric domain can provide important insights into the molecular basis of receptor…”
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Transmembrane Segment Peptides Can Disrupt Cholecystokinin Receptor Oligomerization without affecting Receptor Function by Harikumar, Kaleeckal G., Dong, Maoqing, Cheng, Zhijie, Pinon, Delia I., Lybrand, Terry P., Miller, Laurence J.

“…Oligomerization of the G protein-coupled cholecystokinin (CCK) receptor has been demonstrated, but its molecular basis and functional importance are not clear…”
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Molecular approximations between residues 21 and 23 of secretin and its receptor: development of a model for peptide docking with the amino terminus of the secretin receptor by Dong, Maoqing, Lam, Polo C-H, Gao, Fan, Hosohata, Keiko, Pinon, Delia I, Sexton, Patrick M, Abagyan, Ruben, Miller, Laurence J

“…The structurally unique amino-terminal domain of class II G protein-coupled receptors is critically important for ligand binding and receptor activation…”
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