Synthesis and biological activity of argiotoxin 636 and analogues: selective antagonists for ionotropic glutamate receptors.
More discerning than the parent: Analogues of the polyamine toxin argiotoxin 636 (shown docked in the ion channel of an ionotropic glutamate (iGlu) receptor; N blue, O red) distinguish subtypes of iGlu receptors. Depending on which of the two internal amine groups is replaced with a methylene group, the analogue inhibits one or other of two receptor subtypes as potently as the natural compound, which itself inhibits both subtypes nonselectively.
Nelson
Jared K
JK
Department of Medicinal Chemistry, University of Copenhagen, Universitetsparken 2, 2100 Copenhagen, Denmark.
Frølund
Sidsel U
SU
Tikhonov
Dennis B
DB
Kristensen
Anders S
AS
Strømgaard
Kristian
K
D018691:Excitatory Amino Acid Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007210:Indoleacetic Acids; D010648:Phenylacetates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011073:Polyamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011487:Protein Conformation; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors* / Q000737:chemistry; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors* / Q000737:chemistry
D018691:Excitatory Amino Acid Antagonists; D007210:Indoleacetic Acids; D010648:Phenylacetates; D011073:Polyamines; D018091:Receptors, AMPA; D016194:Receptors, N-Methyl-D-Aspartate; C558368:argiotoxin-636