Creighton University

Solvo Biotechnology

Istvan Palyi

Istvan Teplan

Borbala Vincze

Janos Seprodi

Zsolt Vadasz

Imre Mezo

Sandor Lovas

Geza Toth

Adrienn Kalnay

J Michael Conlon

Magdolna Kovacs

Orsolya Csuka

Dezso Gaal

Maria Magocsi

Melinda Mora

Gizella Turi

Imre Mezom

Richard F Murphy

The present invention provides peptides and pharmacologically active compounds including gonadotropin-releasing hormone (GnRH) analogues according to formulas of the invention, wherein the compounds show an antitumor effect. The invention additionally provides compositions including these peptides and compounds.

GnRH analogues with antitumour effects and pharmaceutical compositions thereof

The invention features novel peptide derivatives called Reversins, and provides for their use in a method of reducing the activity of the multi-drug transporter protein MDR1 in order to overcome multidrug resistance in a mammal. The peptide derivatives are of the formula (I) X,-X,-X,(X,),-X,, wherein n is 0 or 1, and each n is the same or different; X,is BOC, BOC-Asu, Z-Asu, benzyloxycarbonyl, Glu(OBzl)-OBzl, Trp-OMe, Trp-Phe-OMe, Phe-Trp-OMe, Phe-Phe-OtBu, Trp-Trp-OtBu, indoloacetyl, benzoyl, an alkylanine of 1-4 carbons, dibenzylamide, tryptamide, 1-amino-adamantine, aminomethylcyclohexane, indoline, phenylethylamide or dicyclohexylamide; X,is Glu(OBzl), Asp(OBzl), succinyl, O,O-dibenzoyltartaroyl, diphenoyl, muconyl, Thx, Cpa, Asu, Nal, Pen, Phg, Dbt, Lys(BOC), Lys(Z), Cys(Bzl), Thr(Bzl), Glu(OtBu), tert.-Leu, Leu, Nle, Pro, Phe, Tyr(Bzl), or Ser(Bal); X,is Asp, Asu, Lys, Glu, Trp, Thx, Cpa, Nal, Pen, Phg, Dbt, Glu(OtBu), tert.-Leu, Leu, Nle, Pro, Tyr, Phe, or Tyr(Bzl); X,is BOC-Glu(OBzl), Glu(OBzl), Asu, OBzl, Bzl, BOC, BOC-Lys(BOC), Z-Glu(OtBu), Asp(OBzl), Asp(OBz)-OBzl, benzyloxycarbonyl, O-(cyclo-hexyl), fluorenylmethyl ester, Glu(OtBu), Glu(OtBu)-OBzl, 1-amino-adamantine, aminomethylcyclohexane, indoline, phenylethylarnide, or dicyclohexylamide; and X,is OMe, OBzl, OtBu, Phe-OMe, -O-(cyclohexyl), Trp-OMe, (chlorophenyl)-isobutylamide, fluorenylmethyl ester, ONp, 1-aminoadamantane, aminomethylcyclohexane, indoline, phenylethylamide, or dicyclohexylamide.

Compounds for reversing drug resistance

The present invention provides a novel pharmaceutical composition for the treatment of breast cancer. Also provided are various methods of treating breast cancer.

Anti-tumor effects of GnRH-III

Growing community of inventors

Budapest, Hungary

Istvan Palyi