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Dimers Vc1.1-dimer, RgIA-dimer and PeIA-dimer

A technology of vc1.1-dimer and dimer, which is applied in the field of medicine, can solve the problems of insufficient drug production and decreased activity.

Inactive Publication Date: 2019-03-19
OCEAN UNIV OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the difference of α9α10 nAChR in humans and mice, the activity of these toxins on human α9α10 nAChR is significantly reduced, which is not enough to be used as a drug

Method used

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  • Dimers Vc1.1-dimer, RgIA-dimer and PeIA-dimer
  • Dimers Vc1.1-dimer, RgIA-dimer and PeIA-dimer
  • Dimers Vc1.1-dimer, RgIA-dimer and PeIA-dimer

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Embodiment Construction

[0014] The present invention will be described in detail below in combination with specific embodiments.

[0015] Dimeric α-conotoxin Vc1.1, RgIA and PeIA are polypeptide compounds. By designing a linker containing two alkyne functional groups, modifying the wild-type polypeptide, introducing azide functional groups, and then through the click reaction Thus Vc1.1-dimer, RgIA-dimer and PeIA-dimer were synthesized.

[0016] Its structure is as attached Figure 1-3 Shown (the amino acid structure is represented by the abbreviation of amino acid).

[0017] Experiments have proved that α9α10 acetylcholine receptor (nAChR) is one of the subtypes of acetylcholine receptors newly discovered in recent years. It is a target for the treatment of chronic pain and has obvious effects on pain caused by trauma and chemotherapy. The α-conotoxin Vc1.1 and RgIA exhibited strong activity in the mouse α9α10 nAChR, but when tested on the human α9α10 nAChR, the activity decreased significantly, b...

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Abstract

The invention discloses dimers Vc1.1-dimer, RgIA-dimer and PeIA-dimer. The dimer alpha-conotoxin Vc1.1, RgIA and PeIA are polypeptide compounds. The Vc1.1-dimer, RgIA-dimer and PeIA-dimer are synthesized by designing a linker containing two alkynyl functional groups, modifying wild polypeptide and introducing a nitrine functional group to carrying out a click reaction further. The dimers have thebeneficial effects that the activity and selectivity of alpha-conotoxin to alpha9aphla10 acetyl choline acceptors are improved by way of the dimers, so that a novel polypeptide drug for treating painand tumors is developed conveniently.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to dimers Vc1.1-dimer, RgIA-dimer and PeIA-dimer. Background technique [0002] α9α10 acetylcholine receptor (nAChR) is one of the newly discovered acetylcholine receptor subtypes in recent years, and it is the target for the treatment of chronic pain. It has obvious effects on pain caused by trauma and chemotherapy. In addition, α9α10 is overexpressed in tumor cells, so Can be used as an anti-tumor target. Conotoxin (CTX) is secreted by Conus, a carnivorous mollusc living in tropical oceans, and is used to anesthetize prey. It is a small peptide toxin composed of 10-40 amino acids. , a short peptide rich in disulfide bonds. Among them, α-CTX (Vc1.1, RgIA and PeIA, etc.) can specifically act on the acetylcholine receptors at nerve terminals and block them. Therefore, it is expected to be developed as an analgesic for the treatment of neuralgia. However, due to the difference of α9α...

Claims

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Application Information

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IPC IPC(8): C07K14/435A61P29/00A61P35/00
CPCA61P29/00A61P35/00C07K14/43504
Inventor 于日磊梁家珍
Owner OCEAN UNIV OF CHINA
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