Abstract

This is a proposal which outlines approaches for the development of potent and selective somatostatin (also known as somatotropin release inhibiting factor or SRIF) agonists and antagonist to each of the five recently discovered and cloned receptor subtypes SSTR1, SSTR2, SSTR3, SSTR4 and SSTR5. This area of research is highly desired since selective and potent SRIF analogs are needed as tools to unravel multiple SRIF actions and SRIF involvement in the control of neurotransmission, glandular secretion, smooth muscle contractility and cell proliferation.

  Funding Agency

Agency
National Institute of Health (NIH)
Institute
National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)
Type
Research Project (R01)
Project #
5R01DK050124-04
Application #
2905766
Study Section
Bio-Organic and Natural Products Chemistry Study Section (BNP)
Program Officer
Sato, Sheryl M
Project Start
1996-09-27
Project End
2001-08-31
Budget Start
1999-09-01
Budget End
2001-08-31
Support Year
4
Fiscal Year
1999
Total Cost
Indirect Cost

  Institution

Name
Salk Institute for Biological Studies
Department
Type
DUNS #
005436803
City
La Jolla
State
CA
Country
United States
Zip Code
92037

  Publications

Grace, Christy Rani R; Cervini, Laura; Gulyas, Jozsef et al. (2007) Astressin-amide and astressin-acid are structurally different in dimethylsulfoxide. Biopolymers 87:196-205
Grace, Christy Rani R; Erchegyi, Judit; Koerber, Steven C et al. (2006) Novel sst2-selective somatostatin agonists. Three-dimensional consensus structure by NMR. J Med Chem 49:4487-96
Erchegyi, Judit; Waser, Beatrice; Schaer, Jean-Claude et al. (2003) Novel sst(4)-selective somatostatin (SRIF) agonists. 3. Analogues amenable to radiolabeling. J Med Chem 46:5597-605
Erchegyi, Judit; Penke, Botond; Simon, Lajos et al. (2003) Novel sst(4)-selective somatostatin (SRIF) agonists. 2. Analogues with beta-methyl-3-(2-naphthyl)alanine substitutions at position 8. J Med Chem 46:5587-96
Rivier, Jean; Erchegyi, Judit; Hoeger, Carl et al. (2003) Novel sst(4)-selective somatostatin (SRIF) agonists. 1. Lead identification using a betide scan. J Med Chem 46:5579-86
Reubi, Jean Claude (2003) Peptide receptors as molecular targets for cancer diagnosis and therapy. Endocr Rev 24:389-427
Grace, Christy Rani R; Koerber, Steven C; Erchegyi, Judit et al. (2003) Novel sst(4)-selective somatostatin (SRIF) agonists. 4. Three-dimensional consensus structure by NMR. J Med Chem 46:5606-18
Yunker, Warren K; Smith, Sean; Graves, Chad et al. (2003) Endogenous hypothalamic somatostatins differentially regulate growth hormone secretion from goldfish pituitary somatotropes in vitro. Endocrinology 144:4031-41
Rivier, J E; Hoeger, C; Erchegyi, J et al. (2001) Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1). J Med Chem 44:2238-46
Reubi, J C; Schaer, J C; Wenger, S et al. (2000) SST3-selective potent peptidic somatostatin receptor antagonists. Proc Natl Acad Sci U S A 97:13973-8

Showing the most recent 10 out of 14 publications