abstract |
There is provided a novel series of synthetic analogs of hGH-RH(1 -29)NH 2 (SEQ ID NO: 96) and hGH-RH(1 -3O)NH 2 . 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 CH 3 -(CH 2 ) 10 -CO-Ada, at the N-Terminus and β-Ala, Amc, Apa, Ada, AE 2 A, AE 4 P, ε-Lys(α-NH 2 ), 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. |