The General Hospital Corporation

Hisashi Takasu

F Richard Bringhurst

Thomas J Gardella

John T Potts, Jr

The present invention is related to synthetic and/or recombinant biologically active peptide derivatives of PTH(1-28). Some of the peptides of the invention are at least 90% identical to a peptide consisting essentially of the amino acid sequence XValSerGluIleGlnLeuMetHis AsnLeuGlyLysHisLeuAsnSer MetXArgValGluTrpLeuArgLysLysLeu (SEQ ID NO:1), wherein Xis Ser, Ala or Gly; and Xis Glu or Arg.

Human parathyroid hormone modifications, preparation and use

Parathyroid hormone (PTH) and its closely related peptide, PTHrP, share the same receptor, PTHR. LLC-PK1 cells are porcine renal epithelial cells which do not normally express PTHR. The present-invention provides stably transfected LLC-PK1 cells which express human PTHR. Also provided are methods for determining whether a compound of interest is an agonist or antagonist of a Gs or Gq protein coupled receptor.

Screening assays for G protein coupled receptor agonists and antagonists

The present invention is related to a synthetic and/or recombinant biologically active peptide derivatives of PTH( - ). Some of the peptides of the invention are at least 90% identical to a peptide consisting essentially of the amino acid sequence X ValSerGluIleGlnLeuMetHisAsnLeuGlyLysHisLeuAsnSerMetX ArgValGluTrpLeuArgLysLysLeu (SEQ ID NO:1), wherein X is Ser, Ala or Gly; and X is Glu or Arg.

Nucleic acids encoding modified parathyroid hormone

Disclosed are novel parathyroid hormone (PTH) peptide derivatives. In particular, the invention relates to PTH derivatives having amino acid substitutions that confer PTH-1/PTH-2 receptor agonist or antagonist properties to the derivatives. Also disclosed are methods of preparing these novel derivatives, and methods of using these derivatives to treat mammalian conditions.

Amino-terminal modified parathyroid hormone (PTH) analogs

The present invention is related to novel synthetic and/or recombinant biologically active peptide derivatives of parathyroid hormone (PTH). In particular, the invention relates to PTH derivatives of 28 amino acids or less, with one or more amino acid substitutions, methods of their preparation and use.

Modified human parathyroid hormone

Parathyroid hormone (PTH) and its closely related peptide, PTHrP, share the same receptor, PTHR. LLC-PK1 cells are porcine renal epithelial cells which do not normally express PTHR. The present invention provides stably transfected LLC-PK1 cells which express human PTHR. Also provided are methods for determining whether a compound of interest is an agonist or antagonist of a Gs or Gq protein coupled receptor.

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Mishima, Japan

Hisashi Takasu