Výsledky vyhledávání - "Simon J. Hocart"

Elucidation of Vasoactive Intestinal Peptide Pharmacophore for VPAC1Receptors in Human, Rat, and Guinea Pig

Autor: Robert T. Jensen, Tetsuhide Ito, David H. Coy, Simon J. Hocart, Charles D. Ulrich, Samuel A. Mantey, Tapas K. Pradhan, Hisato Igarashi, Wei Hou

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 301:37-50

Vasoactive intestinal peptide (VIP) is a neurotransmitter involved in a number of pathological and physiological processes. VIP is rapidly degraded and simplified stable analogs are needed. VIP's action was extensively studied in rat and guinea pig.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dde2b19c3d27e7e8f60d4927fcb920f8
https://doi.org/10.1124/jpet.301.1.37

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Highly Potent and Subtype Selective Ligands Derived by N-Methyl Scan of a Somatostatin Antagonist

Autor: Rajeswaran Walajapet G, John E. Taylor, Simon J. Hocart, David H. Coy, William A. Murphy

Publikováno v: Journal of Medicinal Chemistry. 44:1305-1311

The search for synthetic peptide analogues of somatostatin (SRIF) which exhibit selective affinities for the five known receptor subtypes (sst1-5) has generated a large number of potent agonists. Some of these agonists display good subtype selectivit

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6a4c5d9bb9e6dbf625889cd639a4c8ea
https://doi.org/10.1021/jm0005048

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Tyrosine 220 in the 5th Transmembrane Domain of the Neuromedin B Receptor Is Critical for the High Selectivity of the Peptoid Antagonist PD168368

Autor: Tatsuro Katsuno, Kenji Tokita, Robert T. Jensen, Simon J. Hocart, Samuel A. Mantey, David H. Coy

Publikováno v: Journal of Biological Chemistry. 276:495-504

Peptoid antagonists are increasingly being described for G protein-coupled receptors; however, little is known about the molecular basis of their binding. Recently, the peptoid PD168368 was found to be a potent selective neuromedin B receptor (NMBR)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e3a6faec3feb2e2f9700f200f6d5b22
https://doi.org/10.1074/jbc.m006059200

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Three-Dimensional Quantitative Structure-Activity Relationships of Somatostatin Analogs. 1. Comparative Molecular Field Analysis of Growth Hormone Release-Inhibiting Potencies

Autor: Vik Reddy, Simon J. Hocart, William A. Murphy, David H. Coy

Publikováno v: Journal of Medicinal Chemistry. 38:1974-1989

Somatostatin is a hypothalamic hormone that inhibits the release of growth hormone (GH). It has also been shown to inhibit the release of a broad range of hormones including insulin, glucagon, and gastrin. Presently, five different receptor subtypes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::489dc6ce06df957556da9986d2ff81bf
https://doi.org/10.1021/jm00011a017

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4-Aminoquinolines Active against Chloroquine-Resistant Plasmodium falciparum: Basis of Antiparasite Activity and Quantitative Structure-Activity Relationship Analyses▿

Autor: Haiyan Deng, Donald J. Krogstad, Huayin Liu, Dibyendu De, Frances M. Krogstad, Simon J. Hocart

Chloroquine (CQ) is a safe and economical 4-aminoquinoline (AQ) antimalarial. However, its value has been severely compromised by the increasing prevalence of CQ resistance. This study examined 108 AQs, including 68 newly synthesized compounds. Of th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ca17cfc66115aaa2a3ec2faa1f94966
https://europepmc.org/articles/PMC3088224/

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Human growth hormone-releasing hormone analogues with much improved in vitro growth hormone-releasing potencies in rat pituitary cells

Autor: Simon J. Hocart, David H. Coy, William A. Murphy

Publikováno v: European Journal of Pharmacology. 204:179-185

Enhancement of the amphiphilic α-helical properties of the central and C-terminal regions of growth hormone-releasing hormone (GRH) by substitution with helix-favouring amino acids, particularly Ala, can result in significant improvements in GH-rele

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5e1959119069b3faf7cf7a3c6d555b25
https://doi.org/10.1016/0014-2999(91)90703-s

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Examination of the 1,4-disubstituted azetidinone ring system as a template for combretastatin A-4 conformationally restricted analogue design

Autor: David H. Coy, Natalya I. Vasilevich, Lichun Sun, Simon J. Hocart, Joseph A. Fuselier

Publikováno v: Bioorganicmedicinal chemistry letters. 14(9)

A series of novel 1,4-diaryl-2-azetidinones was prepared by stereospecific Staudinger reaction as conformationally restricted analogues of combretastatin A-4 because molecular modeling studies suggested close geometric similarities. They were evaluat

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95c8468fc94fdff69264d6db384b65f3
https://pubmed.ncbi.nlm.nih.gov/15080975

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Molecular basis of the selectivity of gastrin-releasing peptide receptor for gastrin-releasing peptide

Autor: David H. Coy, Robert T. Jensen, Simon J. Hocart, Kenji Tokita

Publikováno v: Molecular pharmacology. 61(6)

The mammalian bombesin peptides [gastrin-releasing peptide (GRP) and neuromedin B (NMB)] are important in numerous biological and pathological processes. These effects are mediated by the heptahelical GRP receptor (GRPR) and NMB receptor (NMBR). GRP

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::981ae92ef032274d2a85c41025eba24d
https://pubmed.ncbi.nlm.nih.gov/12021405

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