Patent · US Expired

Non-endogenous, constitutively activated human protein-coupled receptors

US6555339B1 · kind B1 · utility

76Cited by
8References
2Claims
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Key dates

Filing dateOct 13, 1998
Grant dateApr 29, 2003
Priority date
Expiry dateOct 13, 2018

Classification

  • Technology area (CPC G)Physics
  • CPC primaryG01N2500/00
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

Disclosed are constitutively activated, non-endogenous versions of endogenous human GPCRs comprising the following amino acid sequence region (C-terminus to N-terminus orientation) and/or the following nucleic acid sequence region (3′ to 5′ orientation) transversing the transmembrane-6 (TM6) and intracellular loop-3 (IC3) regions of the GPCR:P1AA15X  (a)and/orPcodon(AA-codon)15Xcodon,  (b)respectively. In a preferred embodiment, P1 and Pcodon are endogenous proline and an endogenous nucleic acid encoding region encoding proline, respectively, located within TM6 of the non-endogenous GPCR; AA15 and (AA-codon)15 are 15 endogenous amino acid residues and 15 codons encoding endogenous amino acid residues, respectively; and X and Xcodon are non-endogenous lysine and non-endogenous nucleic acid region encoding lysine, respectively, located within IC3 of the non-endogenous GPCR. The purified and isolated non-endogenous human GPCRs having these mutations, and the receptors incorporated into mammalian cells, are well within the present disclosure.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.