{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,2]],"date-time":"2026-10-02T11:28:05Z","timestamp":1790940485556,"version":"4.1.0"},"reference-count":0,"publisher":"National Academy of Sciences","issue":"14","content-domain":{"domain":["www.pnas.org"],"crossmark-restriction":true},"short-container-title":["Proc. Natl. Acad. Sci. U.S.A."],"published-print":{"date-parts":[[1993,7,15]]},"abstract":"<jats:p>Joro spider toxin (JSTX) is one of the most potent antagonists of glutamatergic AMPA\/KA (alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate\/kainate) receptor channels in invertebrates and vertebrates. A differential blocking effect on certain types of glutamatergic synapses--e.g., parallel and climbing fiber synaptic inputs to rat cerebellar Purkinje neurons--has been shown by using a synthetic analog of the spider toxin. By investigating the molecular basis of the JSTX action on the recombinant AMPA\/KA receptors GluR1-GluR4 and GluR6 expressed in Xenopus oocytes, we found that submicromolar concentrations of JSTX exert a subunit-specific block. Thus, receptor subunits forming a receptor channel with a linear current-voltage (I-V) relationship (GluR1\/2, GluR2\/3, and GluR6) were not affected, while receptor subunits with rectifying I-V relationships (GluR1, GluR3, GluR4, and GluR1\/3) were reversibly blocked by JSTX. By using receptor-subunit mutants obtained by site-directed mutagenesis, we have identified a single amino acid position (glutamine in the proposed second transmembrane domain) that is critical for the JSTX block. Since this site has previously been shown to control the I-V relationship of the AMPA\/KA receptor channel and to participate in the regulation of the channel's permeability for calcium ions, our findings suggest that JSTX binds close to the central pore region of the channel.<\/jats:p>","DOI":"10.1073\/pnas.90.14.6528","type":"journal-article","created":{"date-parts":[[2006,5,31]],"date-time":"2006-05-31T08:27:18Z","timestamp":1149064038000},"page":"6528-6532","update-policy":"https:\/\/doi.org\/10.1073\/pnas.cm10313","source":"Crossref","is-referenced-by-count":194,"title":["A single amino acid determines the subunit-specific spider toxin block of alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate\/kainate receptor channels."],"prefix":"10.1073","volume":"90","author":[{"given":"M","family":"Blaschke","sequence":"first","affiliation":[{"name":"Max-Planck-Institut f\u00fcr Biophysikalische Chemie, G\u00f6ttingen, Germany."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"B U","family":"Keller","sequence":"additional","affiliation":[{"name":"Max-Planck-Institut f\u00fcr Biophysikalische Chemie, G\u00f6ttingen, Germany."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"R","family":"Rivosecchi","sequence":"additional","affiliation":[{"name":"Max-Planck-Institut f\u00fcr Biophysikalische Chemie, G\u00f6ttingen, Germany."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"M","family":"Hollmann","sequence":"additional","affiliation":[{"name":"Max-Planck-Institut f\u00fcr Biophysikalische Chemie, G\u00f6ttingen, Germany."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"S","family":"Heinemann","sequence":"additional","affiliation":[{"name":"Max-Planck-Institut f\u00fcr Biophysikalische Chemie, G\u00f6ttingen, Germany."}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"A","family":"Konnerth","sequence":"additional","affiliation":[{"name":"Max-Planck-Institut f\u00fcr Biophysikalische Chemie, G\u00f6ttingen, Germany."}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"341","published-online":{"date-parts":[[1993,7,15]]},"container-title":["Proceedings of the National Academy of Sciences"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/pnas.org\/doi\/pdf\/10.1073\/pnas.90.14.6528","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2022,4,13]],"date-time":"2022-04-13T13:31:34Z","timestamp":1649856694000},"score":1,"resource":{"primary":{"URL":"https:\/\/pnas.org\/doi\/full\/10.1073\/pnas.90.14.6528"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[1993,7,15]]},"references-count":0,"journal-issue":{"issue":"14","published-print":{"date-parts":[[1993,7,15]]}},"alternative-id":["10.1073\/pnas.90.14.6528"],"URL":"https:\/\/doi.org\/10.1073\/pnas.90.14.6528","relation":{},"ISSN":["0027-8424","1091-6490"],"issn-type":[{"value":"0027-8424","type":"print"},{"value":"1091-6490","type":"electronic"}],"subject":[],"published":{"date-parts":[[1993,7,15]]},"assertion":[{"value":"1993-07-15","order":2,"name":"published","label":"Published","group":{"name":"publication_history","label":"Publication History"}}]}}