Claims
- 1. A crystal comprising Ras and PI3K.
- 2. A crystal according to claim 1, wherein the Ras and PI3K are present in the form of a complex.
- 3. A crystal according to claim 1 or claim 2, comprising a further molecule capable of interacting with Ras, PI3K and/or a Ras/PI3K complex.
- 4. A crystal according to claim 1, wherein Ras and/or PI3K is a Ras and/or PI3K variant, which variant comprises an amino acid insertion, deletion or substitution.
- 5. A crystal according to claim 1, wherein Ras is human Ras.
- 6. A crystal according to claim 1, wherein Ras is H-Ras
- 7. A crystal according to claim 1, wherein Ras is the Ras effector domain.
- 8. A crystal according to claim 1, wherein PI3K is PI3Kγ.
- 9. A crystal according to claim 8, wherein the PI3K is human PI3K.
- 10. A crystal according to claim 1, wherein the PI3K is the catalytic subunit of PI3K.
- 11. A crystal according to any of claim 1, wherein the PI3K comprises the mutation V223K.
- 12. A crystal having the structural coordinates shown in table 1.
- 13. A model for at least part of the Ras effector domain and/or at least part of the PI3K catalytic subunit, made using a crystal according to claim 1.
- 14. A method of screening for or designing a ligand capable of modulating the interaction between Ras and PI3K, comprising the use of a model according to claim 13.
- 15. A method of screening for or designing a ligand capable of modulating the activation of PI3K by Ras, comprising the use of a model according to claim 13.
- 16. A computer readable medium having stored thereon: the structure of a crystal according to claim 1, or a model for at least part of the Ras effector domain and/or at least part of the PI3K catalytic subunit according to claim 13.
- 17. A ligand identified by the method according to claim 14 or 15.
- 18. A ligand according to claim 17, which interacts with any one or more residues present in the β-2 strand of Ras or the Rβ2 strand of PI3K.
- 19. The use of a ligand according to claim 17, in the manufacture of a medicament to treat and/or prevent a disease in a mammalian patient.
- 20. A pharmaceutical composition comprising a ligand according to claim 17 and optionally a pharmaceutically acceptable carrier, diluent, excipient or adjuvant or any combination thereof.
- 21. A method of treating and/or preventing a disease comprising administering a ligand according to claim 17 a mammalian patient.
- 22. Method of claim 21 further comprising administering a pharmaceutical composition according to claim 20.
- 23. A method of treating and/or preventing a disease comprising administering a pharmaceutical composition according to claim 20.
Priority Claims (1)
Number |
Date |
Country |
Kind |
0020958.5 |
Aug 2000 |
GB |
|
RELATED APPLICATIONS
[0001] This application claims priority under 35 U.S.C. §120 to International Application No. PCT/GB01/03810, filed Aug. 24, 2001, which, in turn claims priority to GB0020958.5, filed Aug. 24, 2000.
Continuations (1)
|
Number |
Date |
Country |
Parent |
PCT/GB01/03810 |
Aug 2001 |
US |
Child |
10371617 |
Feb 2003 |
US |