The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Apr. 21, 1998
Filed:
Jan. 21, 1994
Ritu Bala Dhand, London, GB;
Michael Derek Waterfield, Speen Newbury, GB;
Ian Donald Hiles, Bromley, GB;
Ivan Tarasovich Gout, London, GB;
Masato Kasuga, Kobe, JP;
Kazuyoshi Yonezawa, Kobe, JP;
Peter End, London, GB;
Michael Fry, London, GB;
George Panayotou, London, GB;
Ludwig Institute for Cancer Research, New York, NY (US);
Abstract
The invention provides for a method to inhibit the binding between the p85 and p110 subunits of said PI3-kinase and thus a method to modulate PI3-kinase activity and modulate the response of cells to external stimuli. In particular, disabling, by conventional means, residues located in the inter-SH2 domain of said p85 subunit, specifically a region containing amino acid residue 478 to amino acid residue 513 of p85.alpha. subunit, or amino acid residue 445 to amino acid residue 485 of p85.beta. subunit of said PI3-kinase. Interference with these binding regions will affect binding between the subunits and results in inhibiting PI3-kinase activity. This invention further relates to a methods to modulate the serine kinase activity of the PI3-kinase which can be achieved by disabling the DRHNSN sequence of the p110 subunit and can also be used to effect changes in overall PI3-kinase activity. This invention is further related to an (ant)agonist which affects serine kinase activity of PI3-kinase. An agonist is provided which stimulates the phosphorylation of the p85 subunit at the serine residue at position 608, wherein phosphorylation at the serine residue indirectly results in inhibiting PI3-kinase activity.