Subtypes Conantokin




1 subtypes

1.1 conantokin-g (con-g)
1.2 conantokin-t (con-t)
1.3 conantokin-r (con-r)
1.4 conantokin-l (con-l)
1.5 conantokin-pr1, -pr2 , –pr3 (con-pr1, con-pr2 , con-pr3)
1.6 conantokin-p (con-p) , conantokin-e (con-e)
1.7 conantokin-rl-a (con-rl-a)
1.8 conantokin-br (con-br)





subtypes
conantokin-g (con-g)

also known “sleeper peptide” or cgx-1007, con-g small peptide isolated fish-hunting snail, conus geographus. best-characterized conantokin, , acts functional inhibitor of nmdar.


con-g shows potential neuroprotective agent in ischemic , excitotoxic brain injury, neuronal apoptosis, pain, epilepsy, , research tool in drug addiction , alzheimer s disease. con-g blocks nmdar-mediated excitatory postsynaptic currents (epscs). con-g reduces strength of excitotoxic intracellular ca actions , blocks different neuronal injuries in vitro. in injuries con-g shows exceptional prolongation of therapeutic window. con-g can reverse established allodynia , can reverse thermal hypersensitivity induced nerve injury.


conantokin-t (con-t)

con-t purified venom of fish-hunting cone-snail, conus tulipa. peptide has 4 residues of gla. con-t acts inhibiting nmdar-mediated ca influx in neurons in central nervous system.


conantokin-r (con-r)

con-r highly potent anticonvulsant compound, derived conus radiatus.


conantokin-l (con-l)

con-l efficient anticonvulsant compound, derived conus lynceus. differs con-r in c-terminal amino acids and, con-r, induces sleep-like symptoms in young mice, faster onset , longer duration.


con-l blocks nmda-evoked currents in powerful way, reversible upon washout, similar con-r , con-g.


conantokin-pr1, -pr2 , –pr3 (con-pr1, con-pr2 , con-pr3)

each peptide in group derived same species, conus parius. con-pr3 has 3 different post-translational modifications. con-pr1 , –pr2 adopt α-helical conformations in presence of mg , ca, otherwise unstructured. conantokin-pr3 adopts α-helical conformation


these peptides have highest potency nr2b subunits of nmdar.


conantokin-p (con-p) , conantokin-e (con-e)

con-p , con-e isolated 2 fish-hunting cone snails of americas (conus purpurascens , conus ermineus, respectively). con-p differs other known conantokins in contains long disulfide loop 2 gla residues. less helical (estimated 44% helical content), unlike con-g, not require calcium stability of structure. notable distinction increased discrimination nr2b. con-e similar in structure con-p, , have similar function.


conantokin-rl-a (con-rl-a)

con-rl-a, derived venom of conus rolani, unique among conantokins in having 2 distinct conformational states between equilibriates. con-p , con-e, helical structure (estimated @ 50%) not depend on presence or absence of calcium. due fact 2 of 5 gla residues present in con-g replaced in con-rl-a lys. con-r1-a discriminates more other known ligand between nr2b , nr2c subunits of nmdar.


conantokin-br (con-br)

con-br isolated conus brettinghami (aka conus sulcatus), , known conantokin high selectivity nr2d subunit of nmdar.








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