LONG-ACTING GONADOTROPIN-RELEASING HORMONE ANALOGS AND METHODS OF USE THEREOF

摘要

The present invention relates to the design, synthesis and biological evaluation of potent long-acting gonadotropin-releasing hormone (GnRH) analogs including agonists and antagonists comprising a GnRH peptide conjugated to emodic acid or an emodic acid derivative. These long acting analogs bind to GnRH receptors with high affinity and are devoid of any toxicity or antiproliferative effects. The present invention further relates to therapeutic uses of these GnRH analogs as contraceptives, in controlling fertility, and in treating and/or preventing sex-hormone dependent diseases or conditions.