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US 2010/0144678 A1Published application
Compositions and methods for treating bone cancer
AssigneeThe Regents of the University of Colorado, a body corporate
InventorsLajos Gera, John M. Stewart, Leland W.K. Chung, Daqing Wu
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Abstract
Small molecule bradykinin inhibitor bisphosphonate amide derivatives useful for inhibiting cancer growth and treating cancer residing in and around bone are disclosed. These compounds and pharmaceutical compositions containing these compounds are particularly useful for the treatment of prostate cancer bone metastases.
Claims19
A compound having the chemical structure:
- B-L-A
- or a pharmaceutically acceptable salt thereof,
- wherein,
- B is a fragment of an anti-cancer bradykinin receptor antagonist having a formula:
- F5c-OC2Y-, F5c-OC2Y-Pipe-, F5c-OC2Y-Arg-, Bcpa-Bip-, Bipa-, Bip-, F5c-Bip-, Pcin-Bip-, Pcn-Bip-, Pya-Bip-, Bcpa-OC2Y-, Bipa-OC2Y-, Pcn-OC2Y-, F5c-Bip-Pipe-, Pcn-Bip-Pipe-, Bcpa-Bip-Pipe-, Bipa-Bip-Pipe-, Pcin-Bip-Pipe-, F5c-ChG-Arg-, F5c-Bip-Arg-, Bcpa-Bip-Arg-, Bcpa-Bip-Arg, F5c-PFF-Arg-, Fmba-OC2Y-, or F5c-D-OC2Y-.
- L is absent or is the linker piperidinyl;
- and,
- A is an aminobisphosphonate having the chemical structure:
- wherein R1, R2, R3 and R4 are independently H, methyl or ethyl.
6 more elements
A method of identifying an inhibitor of cancer cell growth comprising:
- a. exposing a cancer cell to an anti-cancer therapy;
- and,
- b. monitoring an indicator of bradykinin receptor signaling selected from the group consisting of antagonism or blockade of bradykinin receptors, inhibition of c-src signaling, inhibition of MAPK, and decreased expression of a survivin gene,
- wherein, inhibition of bradykinin receptor signaling is indicative of an effective anti-cancer therapy.
1 more element
Dependencies are inferred from the claim text.