Allele-specific activation of genetically engineered receptors.
- C. Strader, T. Gaffney, R. Dixon
- Biology, ChemistryJournal of Biological Chemistry
- 5 January 1991
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
- B. Henke, C. Aquino, T. Willson
- Biology, ChemistryJournal of Medicinal Chemistry
- 15 August 1997
We previously described a series of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepine CCK-A agonists exemplified by compound 1 (GW 5823), which is the first reported binding selective CCK-A full agonist…
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
GW7854 is a potent mixed CCK-A agonist/CCK-B antagonist which is orally active in two in vivo models of CCK -A-mediated agonist activity.
Biarylaniline phenethanolamines as potent and selective beta3 adrenergic receptor agonists.
- D. Uehling, B. Shearer, C. Cowan
- Biology, ChemistryJournal of Medicinal Chemistry
- 13 April 2006
The ease of synthesis and superior dog pharmacokinetics of compound 38 relative to that of 44 in combination with its in vitro profile led us to choose this compound as a development candidate for the treatment of type 2 diabetes.
Chapter 28. Nonpeptide Agonists for Peptide Receptors: Lessons from Ligands
- E. Sugg
- Biology, Chemistry
- 1997
Synthetic charybdotoxin-iberiotoxin chimeric peptides define toxin binding sites on calcium-activated and voltage-dependent potassium channels.
- K. Giangiacomo, E. Sugg, M. L. García
- BiologyBiochemistry
- 9 March 1993
Two chimeric toxins are constructed by solid-phase synthesis and both inhibited [125I]ChTX binding to sarcolemmal membranes from smooth muscle, and they both blocked the maxi-K channel in planar lipid bilayers.
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
Screening of compounds selected from the Glaxo registry file for contractile activity on the isolated guinea pig gallbladder identified a series of 1,5-benzodiazepines with peripheral cholecystokinin (CCK) receptor agonist activity that are equipotent to CCK as anorectic agents in rats following intraperitoneal administration.
Synthesis and structural characterization of charybdotoxin, a potent peptidyl inhibitor of the high conductance Ca2(+)-activated K+ channel.
- E. Sugg, M. L. García, J. Reuben, A. Patchett, G. Kaczorowski
- Biology, ChemistryJournal of Biological Chemistry
- 5 November 1990
Analysis of the sequence and amino acid composition of the resulting fragments defines a disulfide bond arrangement that predicts a highly folded tertiary structure for ChTX which, together with observations from electrophysiological and binding experiments, suggests a possible mechanism by which ChTX interacts with PK,Ca to block channel function.
Cyclic lactam analogues of Ac-[Nle4]alpha-MSH4-11-NH2.
- E. Sugg, A. M. Castrucci, M. Hadley, G. Van Binst, V. Hruby
- Chemistry, BiologyBiochemistry
- 18 October 1988
Two side-chain cyclic lactam analogues of the 4-11 fragment of alpha-melanocyte-stimulating hormone (alpha-MSH) were prepared on p-methylbenzhydrylamine resin by using a combination of Nalpha-Boc and N alpha-Fmoc synthetic strategies with diphenyl phosphorazidate mediated cyclization and the solution conformation was examined.
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