1xxz

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{{STRUCTURE_1xxz| PDB=1xxz | SCENE= }}
{{STRUCTURE_1xxz| PDB=1xxz | SCENE= }}
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'''Solution structure of sst1-selective somatostatin (SRIF) analog'''
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===Solution structure of sst1-selective somatostatin (SRIF) analog===
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==Overview==
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The three-dimensional NMR structures of six analogues of somatostatin (SRIF) are described. These analogues with the amino acid 4-(N-isopropyl)-aminomethylphenylalanine (IAmp) at position 9 exhibit potent and highly selective binding to human SRIF subtype 1 receptors (sst(1)). The conformations reveal that the backbones of these analogues have a hairpin-like structure similar to the sst(2)-subtype-selective analogues. This structure serves as a scaffold for retaining a unique arrangement of the side chains of d-Trp(8), IAmp(9), Phe(7), and Phe(11) or m-I-Tyr(11) (m-I-Tyr = mono-iodo-tyrosine). The conformational preferences and results from biological analyses of these analogues(1,2) allow a detailed study of the structure-activity relationship of SRIF. The proposed consensus pharmacophore of the sst(1)-selective analogues requires a unique set of distances between an indole/2-naphthyl ring, an IAmp side chain, and two aromatic rings. This motif is necessary and sufficient to explain the binding affinities of all of the analogues studied and is distinct from the existing models suggested for sst(4) as well as sst(2)/sst(5) selectivity.
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(as it appears on PubMed at http://www.pubmed.gov), where 15658866 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15658866}}
==About this Structure==
==About this Structure==
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Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XXZ OCA].
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Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1XXZ OCA].
==Reference==
==Reference==
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[[Category: Rivier, J E.]]
[[Category: Rivier, J E.]]
[[Category: Gamma turn]]
[[Category: Gamma turn]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 08:31:36 2008''

Revision as of 05:31, 28 July 2008

Image:1xxz.png

Template:STRUCTURE 1xxz

Solution structure of sst1-selective somatostatin (SRIF) analog

Template:ABSTRACT PUBMED 15658866

About this Structure

Full experimental information is available from OCA.

Reference

Somatostatin receptor 1 selective analogues: 4. Three-dimensional consensus structure by NMR., Grace CR, Durrer L, Koerber SC, Erchegyi J, Reubi JC, Rivier JE, Riek R, J Med Chem. 2005 Jan 27;48(2):523-33. PMID:15658866

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