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Unexpected binding of an octapeptide to the angiotensin II receptor

Journal Article · · Proc. Natl. Acad. Sci. U.S.A.; (United States)
; ; ; ; ; ; ;

An octapeptide, TBI-22 (Lys-Gly-Val-Tyr-Ile, His-Ala-Leu), inhibited binding of angiotensin II by a solubilized angiotensin receptor partially purified from rabbit liver. This inhibition appears to result from competition for binding to the same receptor. Radioiodinated TBI-22, like angiotensin II, bound to the solubilized receptor with an affinity such that the binding was inhibited 50% by unlabeled TBI-22 or angiotensin II at nanomolar concentrations. The binding reaction, like that for angiotensin II, required p-chloromercuriphenylsulfonic acid and was reversed in the presence of dithiothreitol. TBI-22 and angiotensin II share the sequence Val-Tyr-Ile-His; this tetrapeptide alone, however, did not inhibit binding of angiotensin II. Replacement of the tyrosine residue by aspartic acid in TBI-22 greatly reduced the ability of the peptide to compete with angiotensin II for binding, suggesting an important contribution of this residue to the configuration required for recognition by the receptor.

Research Organization:
Cornell Univ. Medical College, New York, NY (USA)
OSTI ID:
6271555
Journal Information:
Proc. Natl. Acad. Sci. U.S.A.; (United States), Journal Name: Proc. Natl. Acad. Sci. U.S.A.; (United States) Vol. 84:24; ISSN PNASA
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
59 BASIC BIOLOGICAL SCIENCES
ALKALI METAL COMPOUNDS
ANGIOTENSIN
BETA DECAY RADIOISOTOPES
BLOOD PRESSURE
CARDIOVASCULAR AGENTS
CHEMICAL REACTIONS
CHROMATOGRAPHY
CROSS-LINKING
DAYS LIVING RADIOISOTOPES
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
ENZYMES
GLOBULINS
HALIDES
HALOGEN COMPOUNDS
HYDROLASES
INORGANIC PHOSPHORS
INTERMEDIATE MASS NUCLEI
IODIDES
IODINE 125
IODINE COMPOUNDS
IODINE ISOTOPES
ION EXCHANGE CHROMATOGRAPHY
ISOTOPES
LIGANDS
MEMBRANE PROTEINS
NONSPECIFIC PEPTIDASES
NUCLEI
ODD-EVEN NUCLEI
ORGANIC COMPOUNDS
PEPTIDE HYDROLASES
PEPTIDES
PHOSPHORS
PHYSIOLOGY
POLYMERIZATION
POLYPEPTIDES
PROTEINS
RADIOISOTOPES
RECEPTORS
RENIN
SEPARATION PROCESSES
SODIUM COMPOUNDS
SODIUM IODIDES
VASOCONSTRICTORS