Small-molecule inhibitors of angiogenin and rnases and in vivo and in vitro methods of using same
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Abstract
Lead compounds were obtained in a high throughput screen (HTS) of angiogenin (ANG; a potent inducer of angiogenesis) enzyme activity, an RNase. One lead was shown to delay appearance of tumors in an animal tumor system, and to reduce the number of animals having tumors. Several lead compound analogs were found to be even more potent inhibitors of ANG activity compared to the original leads, and two were also found to have greater affinity for ANG than for pancreatic RNase. Other embodiments disclose a method comprising obtaining a ribonuclease inhibitor and a composition; and admixing the ribonuclease inhibitor and the composition to form an admixture, wherein a ribonuclease that may be present in the admixture is inhibited.
69 Citations
57 Claims
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1-30. -30. (canceled)
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31. A method comprising:
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(a) obtaining a ribonuclease inhibitor and a composition; and
(b) admixing the ribonuclease inhibitor and the composition to form an admixture, wherein a ribonuclease that may be present in the admixture is inhibited. - View Dependent Claims (32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56)
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57. A compound comprising a structure selected from the group consisting of NCI-65828, NCI 65845, benzopurpurin B, NCI-65841, NCI 79596, NCI-9617, NCI-16224, suramin, direct red 1, NCI-7815, NCI-45618, NCI-47740, prBZBP, NCI-65568, NCI-79741, NCI-65820, NCI-65553, NCI-58047, NCI-65847, xylidene ponceau 2R, eriochrome black T, amaranth, new coccine, acid red 37, acid violet 7, NCI-45608, NCI-75661, NCI-73416, NCI-724225, orange G, NCI 47755, sunset yellow, NCI-47735, NCI-37176, violamine R, NCI-65844, direct red 13, NCI-45601, NCI 75916, NCI-65546, NCI-65855, NCI-75963, NCI-45612, NCI-8674, NCI-75778, NCI-34933, NCI-1698, NCI-7814, NCI-45550, NCI-77521, cefsulodin, NCI-174066, NCI-12455, NCI-45541, NCI-79744, NCI-42067, NCI-45571, NCI-45538, NCI-45540, NCI-9360, NCI-12857, NCI-D726712, NCI-45542, NCI-7557, S321443, NCI-224131, NCI-45557, NCI-1741, NCI-1743, NCI-227726, NCI-16163, NCI-16169, NCI-88947, NCI-17061, NCI-37169, beryllon II, CB-0181431, CB-473872, JLJ-1, JLJ-2, JLJ-3, CB-467929, CB-534510, CB-540408, CB-180582, CB-180553, CB-186847, CB-477474, CB-152591, NCI-37136, NCI-202516, CB-039263, CB-181145, CB-181429, CB-205125, and CB-224197.
Specification