Bioactivities and Secondary Structures of Constrained Analogues of Human Parathyroid Hormone: Cyclic Lactams of the Receptor Binding Region

In a search for analogues of human parathyroid hormone (hPTH) with improved activities and bioavailabilities, we have prepared the following three lactam analogues of hPTH-(1−31)-NH2 (1) or [Leu27]hPTH-(1−31)-NH2 (2): [Leu27]cyclo(Glu22−Lys26)-hPTH-(1−31)-NH2 (3), [Leu27]cyclo(Lys26−Asp30)-hPTH-(1−...

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Veröffentlicht in:	Journal of medicinal chemistry 1997-04, Vol.40 (9), p.1373-1380
Hauptverfasser:	Barbier, Jean-René, Neugebauer, Witold, Morley, Paul, Ross, Virginia, Soska, Mark, Whitfield, James F, Willick, Gordon
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenylyl Cyclases - metabolism Amino Acid Sequence Amino Acids - analysis Animals Antihypertensive Agents - chemical synthesis Antihypertensive Agents - chemistry Antihypertensive Agents - metabolism Antihypertensive Agents - pharmacology Biological and medical sciences Blood Pressure - drug effects Circular Dichroism Enzyme Activation Hormones. Endocrine system Humans Lactams - chemical synthesis Lactams - chemistry Lactams - metabolism Lactams - pharmacology Medical sciences Models, Molecular Molecular Sequence Data Osteoblasts - enzymology Parathyroid Hormone - chemistry Parathyroid Hormone - metabolism Parathyroid Hormone - pharmacology Peptide Fragments - chemical synthesis Peptide Fragments - pharmacology Pharmacology. Drug treatments Protein Conformation Protein Structure, Secondary Rats Receptors, Parathyroid Hormone - metabolism Tumor Cells, Cultured
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