書誌事項
- タイトル別名
-
- Medicinal Chemistry of Mid-sized Molecules on Biologically Active Peptides
- ペプチド カガク オ リヨウ シタ セイタイ ブンシ カラ ノ チュウ ブンシソウヤク
この論文をさがす
説明
Neuromedin U (NMU) displays various physiological activities including an anorexigenic effect, and the C-terminal heptapeptide-amide sequence is necessary to activate two NMU receptors (NMUR1 and NMUR2). Based on this heptapeptide, we recently developed highly active NMUR1 hexapeptide agonist 4d and NMUR2-selective hexapeptide agonist 8c. Moreover, we identified two major biodegradation sites (Phe2-Arg3 and Arg5-Asn6) by the stability analysis of 4d in serum. On the other hand, myostatin is an endogenous negative regulator of skeletal muscle mass, which is recognized as a therapeutic target for muscle atrophic disorders. Recently, we successfully identified myostatin inhibitory peptides 9 and 16 (24 and 23 amino acids, respectively) with minimum sequence derived from mouse myostatin prodomain. These peptides directly bind to myostatin with KD values of 30-36 nM. Moreover, peptide 9 significantly increased tibialis anterior muscle mass in Duchenne muscular dystrophy model mice. Therefore, these synthesized peptides would be promising mid-sized molecules for peptide-based medicinal chemistry.
収録刊行物
-
- 有機合成化学協会誌
-
有機合成化学協会誌 73 (7), 737-748, 2015
公益社団法人 有機合成化学協会
- Tweet
キーワード
詳細情報 詳細情報について
-
- CRID
- 1390282680318245504
-
- NII論文ID
- 130005093746
-
- NII書誌ID
- AN0024521X
-
- ISSN
- 18836526
- 00379980
-
- NDL書誌ID
- 026607969
-
- 本文言語コード
- ja
-
- データソース種別
-
- JaLC
- NDL
- Crossref
- CiNii Articles
-
- 抄録ライセンスフラグ
- 使用不可