The United States Government As Represented by the Department of Veterans Affairs

University of Miami

The Administrators of the Tulane Educational Fund

Other

Ren Zhi Cai

Andrew V Schally

Marta Zarandi

Jozsef L Varga

There is provided a novel series of synthetic analogs of hGH-RH(1-29)NH(SEQ ID NO: 1) and hGH-RH(1-30)NH. 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&#x2014;(CH)&#x2014;CO-Ada, at the N-Terminus and &#x3b2;-Ala, Amc, Apa, Ada, AEA, AEP, &#x3b5;-Lys(&#x3b1;-NH), 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.

N- and C-terminal substituted antagonistic analogs of GH-RH

There are provided a novel series of peptide analogs of hGH-RH(1-29)NHand hGH-RH(1-30)NHwhich show high activities in stimulating the release of pituitary GH in animals. They retain their physiological activity in solution for extended periods of time and resist enzymic degradation in the body. These novel and useful properties appear to be due to novel substitution patterns ant at the 1, 15, 27 and 29 positions on the peptide.

GH-RH analogs with potent agonistic effects

N- and C- terminal substituted antagonistic analogs of GH-RH

Novel fluorinated synthetic analogs of hGH-RH(1-30)NHthat 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, and to therapeutic compositions containing these novel peptides and their use.

Fluorinated GHRH antagonists

There is provided a novel series of synthetic antagonistic analogs of hGH-RH(1-29)NH. These analogs inhibit the activity of endogenous hGH-RH on the pituitary GH-RH receptors, and therefore prevent the release of growth hormone. The analogs also inhibit the proliferation of human cancers through a direct effect on the cancer cells. The higher inhibitory potencies of the new analogs, as compared to previously described ones, results from replacement of various amino acids.

Antagonistic analogs of GH RH (2003)

Novel compositions of the formula ##STR1## wherein A represents an L, D or DL amino-acid selected from the group consisting of Ala, Val, Phe, p-Cl-Phe, Trp, Pro, Ser, Thr, Glu, Gly, Beta Ala, Abu, N-Me Ala, 5-F-Trp, 5-Br-Trp, 5-Cl-Trp, their acetylated derivatives or a pharmaceutically acceptable acid addition salt thereof;

Growing community of inventors

Miami, FL, United States of America

Ren Zhi Cai