Highly potent metallopeptide analogues of luteinizing hormone-releasing hormone.
نویسندگان
چکیده
منابع مشابه
Highly potent analogues of luteinizing hormone-releasing hormone containing D-phenylalanine nitrogen mustard in position 6.
The nitrogen mustard derivatives of 4-phenylbutyric acid and L-phenylalanine, called chlorambucil (Chl) and melphalan (Mel), respectively, have been incorporated into several peptide hormones, including luteinizing hormone-releasing hormone (LH-RH). The alkylating analogues of LH-RH were prepared by linking Chl, as an N-acyl moiety, to the complete amino acid sequence of agonistic and antagonis...
متن کاملAnalogues of luteinizing hormone-releasing hormone containing cytotoxic groups.
In an attempt to produce better cytotoxic analogues, chemotherapeutic antineoplastic radicals including an alkylating nitrogen mustard derivative of D-phenylalanine (D-melphalan), reactive cyclopropane, anthraquinone derivatives [2-(hydroxymethyl)anthraquinone and the anticancer antibiotic doxorubicin], and an antimetabolite (methotrexate) were coupled to suitably modified agonists and antagoni...
متن کاملHighly potent antagonists of luteinizing hormone-releasing hormone free of edematogenic effects.
To eliminate the undesirable edematogenic effect of the luteinizing hormone-releasing hormone (LH-RH) antagonists containing basic D amino acids at position 6, exemplified by [Ac-D-Phe(pCl)1,2,D-Trp3,D-Arg6,D-Ala10]LH-RH [Phe(pCl) indicates 4-chlorophenylalanine], analogs with D-ureidoalkyl amino acids such as D-citrulline (D-Cit) or D-homocitrulline (D-Hci) at position 6 were synthesized and t...
متن کاملLuteinizing hormone-releasing hormone antagonists.
BACKGROUND Luteinizing hormone-releasing hormone (LH-RH) plays a central role in the vertebrate reproduction by regulating gonadal activity. Based on its binding to pituitary LH-RH receptors, as well as to LH-RH receptors expressed on cancer cells, LH-RH agonists and antagonists have been developed for different therapeutic applications. OBJECTIVE/METHOD Here we give an overview of the most r...
متن کاملLuteinizing hormone-releasing hormone analogues and hormone ablation for prostate cancer: state of the art.
Substitution at positions 6 and 10 can result in super-active peptides. Therefore, several LHRH analogues substituted at position 6, 10, or both are much more active than LHRH and have prolonged activity [5]. Of these analogues, the most important are [D-Trp 6 ]LHRH (triptorelin), [D-Leu 6 ,Pro 9 NHET]LHRH (leuprolide), [D-Ser(Bu t ) 6 ,Pro 9 NHET]LHRH (buserelin), and [D-Ser(Bu t ) 6 ,AzaGly 1...
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ژورنال
عنوان ژورنال: Proceedings of the National Academy of Sciences
سال: 1989
ISSN: 0027-8424,1091-6490
DOI: 10.1073/pnas.86.16.6313