NOVEL N- AND C-TERMINAL SUBSTITUTED ANTAGONISTIC ANALOGS OF GH-RH

摘要

There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH2 (SEQ ID NO: 96) and hGH-RH(1-30)NH2. Of particular interest are those carrying PhAc, N-Me-Aib, Dca, Ac- Ada, Fer, Ac-Anic, 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 .beta.-Ala, Amc, Apa, Ada, AE2A, AE4P, .epsilon.-Lys(.alpha.-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 through a direct effect on the cancer cells. The stronger inhibitory potencies of the new analogs, as compared to previously described ones, result from replacement of various amino acids.