发明授权
- 专利标题: N- and C- terminal substituted antagonistic analogs of GH-RH
- 专利标题(中): GH-RH的N-和C-末端取代的拮抗类似物
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申请号: US12890626申请日: 2010-09-25
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公开(公告)号: US08691942B2公开(公告)日: 2014-04-08
- 发明人: Andrew V. Schally , Marta Zarandi , Jozsef L. Varga , Ren Zhi Cai
- 申请人: Andrew V. Schally , Marta Zarandi , Jozsef L. Varga , Ren Zhi Cai
- 申请人地址: US FL Miami US DC Washington
- 专利权人: University of Miami,U.S.A. Represented by the Dept. of Veterans Affairs
- 当前专利权人: University of Miami,U.S.A. Represented by the Dept. of Veterans Affairs
- 当前专利权人地址: US FL Miami US DC Washington
- 代理机构: Pepper Hamilton LLP
- 主分类号: C07K14/60
- IPC分类号: C07K14/60 ; A61K38/25
摘要:
There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 1) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac-Ada, Fer, Ac-Amc, Me-NH-Sub, PhAc-Ada, Ac-Ada-D-Phe, Ac-Ada-Phe, Dca-Ada, Dca-Amc, Nac-Ada, Ada-Ada, or CH3—(CH2)10—CO-Ada, at the N-Terminus and β-Ala, Amc, Apa, Ada, AE2A, AE4P, ε-Lys(α-NH2), Agm, Lys(Oct) or Ahx, at the C-terminus. These analogs inhibit the release of growth hormone from the pituitary in mammals as well as inhibit the proliferation of human cancers, and inhibit the hyperplastic and benign proliferative disorders of various organs, through a direct effect on the cancerous and non-malignant cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.
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