Structure–activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists
| Autor: | Hiroaki Ohno, Shinya Oishi, Taro Noguchi, Nobutaka Fujii, Ryosuke Misu |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
medicine.medical_specialty
Neurokinin B Tachykinin peptides Clinical Biochemistry Pharmaceutical Science Peptide CHO Cells Pharmacology Biochemistry Structure-Activity Relationship chemistry.chemical_compound Cricetulus Tachykinins Internal medicine Drug Discovery medicine Animals Humans Structure–activity relationship Amino Acid Sequence Receptor Molecular Biology Peptide sequence chemistry.chemical_classification biology musculoskeletal neural and ocular physiology Organic Chemistry Receptors Neurokinin-3 biology.organism_classification Peptide Fragments [MePhe7]-neurokinin B Endocrinology NK3R chemistry GnRH Molecular Medicine Tachykinin Peptides Tachykinin receptor |
| Zdroj: | Bioorganic & Medicinal Chemistry. 21:2413-2417 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2013.01.036 |
| Popis: | Neurokinin B (NKB) is a potential regulator of pulsatile gonadotropin-releasing hormone (GnRH) secretion via activation of the neurokinin-3 receptor (NK3R). NKB with the consensus sequence of the tachykinin peptide family also binds to other tachykinin receptors [neurokinin-1 receptor (NK1R) and neurokinin-2 receptor (NK2R)] with low selectivity. In order to identify the structural requirements for the development of novel potent and selective NK3R agonists, a structure-activity relationship (SAR) study of [MePhe(7)]-NKB and other naturally occurring tachykinin peptides was performed. The substitutions to naturally occurring tachykinins with Asp and MePhe improved the receptor binding and agonistic activity for NK3R. The corresponding substitutions to NKB provided an NK3R selective analog. |
| Databáze: | OpenAIRE |
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