Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors.

Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors. Research Abstract Details 

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Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors. Abstract Text:

Gregory V Nikiforovich,Garland R Marshall,Samuel Achilefu,

Several analogs of somatostatin with conformational constraints in their peptide backbones have been modeled to determine energetically feasible conformations. Comparison of low-energy backbone structures of these peptides suggested unique conformations of the central Phe/Ala(i)-D-Trp(i+1)-Lys(i+2)-Thr(i+3) fragment characteristic for specific interactions of somatostatin with each of the five distinct subtypes of somatostatin receptors (SSTRs). The conformations obtained were in good agreement with experimental data obtained earlier by NMR measurements and/or X-ray crystallography. The results help rationalize experimental observations on the specificity of binding of various somatostatin analogs with different subtypes of the SSTRs. They also serve as templates for the design of conformationally constrained non-peptide scaffolds that effectively and selectively interact with different subtypes of SSTRs. Such scaffolds can be convenient carriers of radiolabels and near-infrared labels in specific agents for imaging tumors expressing different SSTR subtypes.

Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors. Publishing Authors By Initials

GV Nikiforovich,GR Marshall,S Achilefu,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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MEDLINE DATE:

Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Chemical biology & drug design

VOLUME: 69

Page Numbers: 163-9

Journal Abbreviation:

ISSN: 1747-0277

DAY: 3

MONTH: Mar

YEAR: 2007

Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 101262549

Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: metabolism

Chemical & Substance for Abstract: Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors. Information

Substance Name: Somatostatin

Registry Number: 51110-01-1

Grant and Affiliation Information for Molecular modeling suggests conformational scaffolds specifically targeting five subtypes of somatostatin receptors.

AFFILIATION: Department of Biochemistry and Molecular Biology, Washington University Medical School, St. Louis, MO 63110, USA. gregory@ccb.wustl.edu

Country: England

AGENCY: United States NIGMS

GRANT: GM 68460

ACRONYM: GM

MEDLINETA: Chem Biol Drug Des

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