Mechanisms accelerating tachykinin's biological activities

加速速激肽生物活性的机制

• 批准号: 13671959
• 负责人: ABE Kimio
• 金额: $ 1.86万
• 依托单位: Fukuoka Dental College
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 2001
• 资助国家: 日本
• 起止时间: 2001 至 2002
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-13671959/
• 关键词: Tachykinin; Active site; Sialogogue; Salivary Gland; Oligopeptide; Rat; Aminosequence; Synthetic peptide; 唾液腺; 睡眠剤; 活性調節機構

The biological activities of natural and synthetic tachykinins are elaborately controlled in the amino acid sequence. Especially methionylamide (M-NH2), a terminal amino acid, and phenylalanine (F) including in a C-terminal pentapeptide are essential to keep tachykinin's activities and to work as an address domain for the NK receptors. However, there are many other regulatory mechanisms in not only C-terminals but N-terminals. When a C-terminal heptapeptide has strong activity, the N-terminals work inhibitedly and vice visa. In addition, the intensity of biological activities are drastically dependent on the combination mode of three amino acids in positions 5, 6 and 8 present in amino acid sequence. The D-type amino acids are also replaceable with L-type ones. The nonapeptide (QKQQFYGLM-NH2) with the strongest activities for salivation has newly been determined, but its dimmer does not show any effectiveness for salivation. We have carried out using many synthetic tachykinins to find out the active site for salivation. But, it is very complicated to elucidate how to control the active site. Unfortunately the nonapeptide was too short to determine the secondary or tertiary structure with a high technology machine.

天然和合成的速激肽的生物活性是在氨基酸序列中精心控制的。尤其是末端氨基酸甲硫氨酰酰胺 (M-NH2) 和 C 末端五肽中的苯丙氨酸 (F) 对于保持速激肽的活性和作为 NK 受体的地址域至关重要。然而，不仅在C端而且在N端还存在许多其他调节机制。当C端七肽活性较强时，N端活性受到抑制，反之亦然。此外，生物活性的强度很大程度上取决于氨基酸序列中第5、6和8位的三个氨基酸的组合方式。 D型氨基酸也可以用L型氨基酸替代。新近确定了具有最强流涎活性的九肽（QKQQFYGLM-NH2），但其二聚体并未表现出任何流涎功效。我们已经使用许多合成的速激肽来找出流涎的活性位点。但是，阐明如何控制活性位点非常复杂。不幸的是，九肽太短，无法用高科技机器确定二级或三级结构。

项目成果

A. Letio-Gavrilovic, A. Piattelli and K. Abe: "Nerve growth factor β delivery via a collagen/hydroxyapatite composite and its effects on new bone ingrowth"Journal of Materials Science: Materials in Medicine. 14. 1-8 (2003)

A. Letio-Gavrilovic、A. Piattelli 和 K. Abe：“通过胶原蛋白/羟基磷灰石复合材料传递神经生长因子 β 及其对新骨向内生长的影响”材料科学杂志：医学材料 14. 1-8 (2003)。 ）

K. Abe, K. Higa and C. Gao: "The active sites for salivation of natural and synthetic tachykinins (Abstract)"6th European Symposium on Saliva. 6. 42 (2002)

K.Abe、K.Higa 和 C.Gao：“天然和合成速激肽唾液分泌的活性位点（摘要）”第六届欧洲唾液研讨会。

T. Nishiura, C. Gao, W. Motokawa and K. Abe: "Expression and postnatal change of adrenergic receptor subtype mRNA in rat submandibular glands"Archives of Oral Biology. 46. 573-584 (2001)

T. Nishiura、C. Gau、W. Motokawa 和 K. Abe：“大鼠颌下腺中肾上腺素能受体亚型 mRNA 的表达和出生后变化”口腔生物学档案。

A.Letic-Gavrilovic, A.Piattelli, K.Abe: "Nerve growth factor β delivery via a collagen/hydroxyapatite composite and its effects on new bone ingrowth"Journal of Materials Science : Materials in Medicine. 14. 1-8 (2003)

A.Letic-Gavrilovic、A.Piattelli、K.Abe：“通过胶原蛋白/羟基磷灰石复合材料传递神经生长因子 β 及其对新骨向内生长的影响”材料科学杂志：医学材料 14. 1-8 (2003)。 ）

K.Abe, K.Higa, C.Gao: "The active sites for salivation of natural and synthetic tachykinins"6^<th> European symposium on saliva (Abstract). 6. 42 (2002)

K.Abe、K.Higa、C.Gao：“天然和合成速激肽唾液分泌的活性位点”第 6 届欧洲唾液研讨会（摘要）。