Peptide and small molecule agonists of EphA and their uses
| Title: | Peptide and small molecule agonists of EphA and their uses |
|---|---|
| Patent Number: | 8,222,253 |
| Publication Date: | July 17, 2012 |
| Appl. No: | 11/577770 |
| Application Filed: | October 21, 2005 |
| Abstract: | Methods and compositions for activating an EphA receptor can be used for identifying therapeutic agents for cancer. |
| Inventors: | Wang, Bingchen (Strongsville, OH, US); Myshkin, Eugene (Cleveland, OH, US); Miao, Hui (Rocky River, OH, US) |
| Assignees: | Case Western Reserve University (Cleveland, OH, US) |
| Claim: | 1. A method of treating cancer in an individual, comprising administering to the individual a therapeutically effective amount of doxazosin, wherein the cancer is selected from the group consisting of skin cancer, lung cancer, pancreatic cancer and melanomas. |
| Claim: | 2. A method of treating cancer in an individual, comprising administering to the individual a therapeutically effective amount of an agonist of EphA receptor protein, the agonist inhibiting proliferation of cancer cells, the EphA receptor protein comprising at least one of EphA1, EphA2, or EphA3, the agonist having the general formula: [chemical expression included] wherein R 1 is selected from H, C 1-6 alkyl, C 1-6 aralkyl, C 1-6 alkanoyl, aryl, heterocyclyl, C 1-6 heterocyclylalkyl, C 1-6 carbocyclylalkyl, and carbocyclyl, or two occurrences of R 1 together are C 1-6 alkyl, thereby forming a ring; R 2 , R 3 , and R 4 are independently selected from H, C 1-6 alkyl, C 1-6 aralkyl, C 1-6 heterocyclylalkyl, and C 1-6 carbocyclylalkyl; R 5 is selected from C 1-6 alkyl, C 1-6 alkoxy, halogen, C 1-6 alkanoyl, C 1-6 alkoxycarbonyl, C(O)N(R 6)(R 7), and SO 2 N(R 6)(R 7); R 6 and R 7 are independently selected from H and C 1-6 alkyl; X is selected from CH 2 , NH, and O; each Y is independently selected from CH and N; m is an integer from 1 to 2; n is an integer from 1 to 3; and p is an integer from 0 to 3, wherein the cancer is selected from the group consisting of skin cancer, lung cancer, pancreatic cancer, and melanomas. |
| Current U.S. Class: | 51425/217 |
| Patent References Cited: | 10-101579 April 1998 |
| Other References: | Kyprianou et al. (Cancer Research 2000; 60: 4550-4555). cited by examiner Fox et al. (Biochemical and Biophysical Research Communications 2006; 342: 1263-1272). cited by examiner Keledjian et al., The journal of Uroloy, 2003;169:1150-1156. cited by examiner Cheng et al., Molecular Cancer Research, 2002;1:2-11. cited by examiner Machine English Translation of JP10-101579A. cited by examiner |
| Primary Examiner: | Hui, San-Ming |
| Attorney, Agent or Firm: | Tarolli, Sundheim, Covell & Tummino LLP |
| Accession Number: | edspgr.08222253 |
| Database: | USPTO Patent Grants |
| Language: | English |
|---|