Типы конотоксинов
Структурный |
Масса (Da) |
тип |
|
4-Cys/2-loop |
1250-2100 |
CC-C-C |
|
6-Cys/3-loop 2500-2700 CC-C-C-CC 2378
6-Cys/4-loop 2400-3400 C-C-CC-C-C 2900-3400
3200
6-Cys/4-loop 2600-3100 CC-C-C-C-C 1750-1900
Класс токсинов
α-conotoxin
-conotoxin-PIIIE
-conotoxin-conotoxin-PVIIA
αA-conotoxin-PnIVA/B
Мишень
действия AcChR
Na-channel
AcChR
Ca-channel
Na-channel
K-channel
AcChR
Na-channel
The are toxins acting on:
a)Ca2+ channels
b)K+ channels
c)Na+ chennels
d)Cl- chennels
e)nAChR
f)NMDA-R
g)natriuretic peptide receptor
h)glucagon like peptide receptor
i)adrenoreceptor
j)neurotensin receptor
k)angiotensin receptor
l)noradrenoline transporter
Natural toxins: a well known source of drugs
Drug |
Origin |
Action |
Date |
Status |
References |
Captopril |
Bradykinin |
Decrease hypertension |
1975 |
A major drug |
Ferreira S, 1965, J. |
|
potentiating |
|
|
|
Pharm. 24, 163 |
|
peptides from |
|
|
|
|
|
Bothrops jararaca. |
|
|
|
|
Batroxobin |
Serine protease |
Thrombinlike agent |
1980 |
Drug |
Stocker et al., 1986, |
|
(Bothrops) |
|
|
(Pentapharm) |
Toxicon 24, 81 |
Ancrod |
Serine protease |
Thrombinlike agent |
1980 |
Drug |
Illig, 1996, Semin. |
|
(Bothrops) |
|
|
(Pentapharm) |
Vasc. Surg. 9, 315 |
Tracrium |
Curare from plant |
Curarelike agent : |
1980 |
Drug |
Stenlake et al., 1983, |
|
Chondrodendron |
Paralyses skeletal |
|
|
Br. J. Anaesth. 55, 3S |
|
tomentosum |
muscles |
|
|
|
Botulinum toxin |
Clostridium |
Block release mediator : |
1985 |
Drug |
Bakheit, 2001, Dev. |
|
botulinum |
antispasms, |
|
|
Med. Child. Neurol. |
|
|
antiwrinckles |
|
|
43, 234 |
Ziconitide |
conotoxin MVIIA |
Block Ntype Ca2+ |
2004 |
Drug |
Uchitel, 1997, |
|
from Conus magus |
channels : antipain |
|
|
Toxicon 35, 1161 |
Conantokins |
Cone snail : Conus |
Block NMDA receptors : |
1990 |
Potential drug in |
Mena, 1990, |
|
geographus |
epileptic properties |
|
Phase I |
Neurosci. Lett. 118, |
|
|
|
|
|
241 |
Aggrastat |
African sawscaled |
Inhibits platelet |
1992 |
Drug |
Proimos, 2001, J. |
|
viper : Echis |
aggregation : prevents |
|
|
Thrombolysis 11, 99 |
|
carinatus |
clots from growing |
|
|
|
ABT594 |
Frog : Epipedobates |
Agonist of neuronal |
1998 |
Potential drug in |
Bannon et al., 1998, |
|
tricolor |
nAchR : analgesic |
|
Phase II |
Science, 279, 77 |
|
|
activity |
|
|
|
MiniCD4 |
Engineered |
Block gp120 & |
2003 |
To enter |
Martin et al., |
|
scorpion toxin |
unmask neutralizing |
|
preclinical |
2003 Nat. Biotech. |
|
fold |
epitopes : antiHIV |
|
trials |
21, 1 |
|
|
vaccine: |
|
|
|