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US 2002/0173618 A1Published application
SSTR1-selective analogs
AssigneeThe Salk Institute for Bilogical Studies
InventorsJean E.F. Rivier, Jean Claude Reubi
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AssigneeThe Salk Institute for Bilogical Studies
InventorsJean E.F. Rivier, Jean Claude Reubi
Estimating the term…
Analogs of SRIF which are selective for SSTR1 in contrast to the other cloned SRIF receptors. These analogs are useful in determining the tissue and cellular expression of the receptor SSTR1 and its biological role in the endocrine, exocrine and nervous system, as well as in regulating tumor growth. SRIF analog peptides, such as des-AA1,2,5[D-Trp8, NMeIAmp9, Tyr11]-SRIF and counterparts incorporating Cbm at the N-terminus and/or NαSer13, inhibit the binding of a universal SRIF radioligand to the cloned human receptor SSTR1, but they do not bind with significant affinity to human SSTR2, SSTR3, SSTR4 or SSTR5. By incorporating an iodinated tyrosine in position-2 or in position-11 in these SSTR1-selective SRIF analogs, a labeled compound useful in drug-screening methods is provided. The N-terminus accommodates bulky moieties without loss of selectivity, and a carbamoyl moiety or a conjugating agent that will accept a radioactive nuclide or will link to a cytotoxin may be present at the N-terminus.
A cyclic somatostatin(SRIF) analog peptide which selectively binds the SRIF receptor SSTR1, which peptide has the amino acid sequence (cyclo)Xaa1-Xaa2-Xaa3-Lys-Phe-Xaa7-D-Xaa8-Xaa9-Thr-Xaa11-Thr-Xaa13-Cys wherein Xaa1 is H, Ala, D-Ala, Cbm, Biu, (lower alkyl)Cbm, L-Hor, an acyl group having up to 20 carbon atoms, lower alkyl or a conjugating/complexing agent;
A cyclic somatostatin (SRIF) analog peptide having the amino acid sequence:
A cyclic somatostatin(SRIF) analog peptide having specific affinity for the SRIF receptor SSTR1, which peptide has an amino acid sequence at least 11 residues in length, contains a Cys-Cys disulfide bond with a sequence of at least 9 residues located between said Cys residues as a ring, and contains Lys-Phe-Phe-D-Xaa8-Xaa9-Thr-Xaa11 or its equivalent linked to the Cys residue near the N-terminus, which analog peptide is characterized by D-Xaa8 being an aromatic D-isomer amino acid, by Xaa9 being IAmp or NαMeIAmp, and by Xaa1l being Tyr or ITyr.
Dependencies are inferred from the claim text.