{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,23]],"date-time":"2026-10-23T06:42:40Z","timestamp":1792737760145,"version":"4.5.0"},"reference-count":47,"publisher":"Elsevier BV","issue":"2","license":[{"start":{"date-parts":[[2012,2,1]],"date-time":"2012-02-01T00:00:00Z","timestamp":1328054400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2012,2,1]],"date-time":"2012-02-01T00:00:00Z","timestamp":1328054400000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"}],"content-domain":{"domain":["jpet.aspetjournals.org","elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["The Journal of Pharmacology and Experimental Therapeutics"],"published-print":{"date-parts":[[2012,2]]},"DOI":"10.1124\/jpet.111.187104","type":"journal-article","created":{"date-parts":[[2011,11,17]],"date-time":"2011-11-17T12:39:39Z","timestamp":1321533579000},"page":"463-472","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":11,"title":["Roscovitine Inhibits CaV3.1 (T-Type) Channels by Preferentially Affecting Closed-State Inactivation"],"prefix":"10.1016","volume":"340","author":[{"given":"Viktor","family":"Yarotskyy","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Keith S.","family":"Elmslie","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1124\/jpet.111.187104_bib1","doi-asserted-by":"crossref","first-page":"225","DOI":"10.1002\/047002142X.ch17","article-title":"Expression and role of hERG channels in cancer cells","volume":"266","author":"Arcangeli","year":"2005","journal-title":"Novartis Found Symp"},{"key":"10.1124\/jpet.111.187104_bib2","doi-asserted-by":"crossref","first-page":"29","DOI":"10.1038\/sj.bjc.6603509","article-title":"A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days","volume":"96","author":"Benson","year":"2007","journal-title":"Br J Cancer"},{"key":"10.1124\/jpet.111.187104_bib3","doi-asserted-by":"crossref","first-page":"341","DOI":"10.1113\/jphysiol.1986.sp016157","article-title":"Inactivation of the low-threshold transient calcium current in rat sensory neurones: evidence for a dual process","volume":"376","author":"Bossu","year":"1986","journal-title":"J Physiol"},{"key":"10.1124\/jpet.111.187104_bib4","doi-asserted-by":"crossref","first-page":"1681","DOI":"10.1529\/biophysj.104.052837","article-title":"Slowed N-type calcium channel (CaV2.2) deactivation by the cyclin-dependent kinase inhibitor roscovitine","volume":"89","author":"Buraei","year":"2005","journal-title":"Biophys J"},{"key":"10.1124\/jpet.111.187104_bib5","doi-asserted-by":"crossref","first-page":"1450","DOI":"10.1111\/j.1471-4159.2008.05248.x","article-title":"The separation of antagonist from agonist effects of trisubstituted purines on CaV2.2 (N-type) channels","volume":"105","author":"Buraei","year":"2008","journal-title":"J Neurochem"},{"key":"10.1124\/jpet.111.187104_bib6","doi-asserted-by":"crossref","first-page":"883","DOI":"10.1016\/j.neuropharm.2006.10.006","article-title":"Roscovitine differentially affects CaV2 and Kv channels by binding to the open state","volume":"52","author":"Buraei","year":"2007","journal-title":"Neuropharmacology"},{"key":"10.1124\/jpet.111.187104_bib7","doi-asserted-by":"crossref","first-page":"411","DOI":"10.1124\/pr.57.4.5","article-title":"International Union of Pharmacology. XLVIII. Nomenclature and structure-function relationships of voltage-gated calcium channels","volume":"57","author":"Catterall","year":"2005","journal-title":"Pharmacol Rev"},{"key":"10.1124\/jpet.111.187104_bib8","doi-asserted-by":"crossref","first-page":"3200","DOI":"10.1111\/j.1460-9568.2006.04849.x","article-title":"The effects of presynaptic calcium channel modulation by roscovitine on transmitter release at the adult frog neuromuscular junction","volume":"23","author":"Cho","year":"2006","journal-title":"Eur J Neurosci"},{"key":"10.1124\/jpet.111.187104_bib9","doi-asserted-by":"crossref","first-page":"518","DOI":"10.1111\/j.1432-1033.1997.0518a.x","article-title":"Inhibition of cyclin-dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine","volume":"243","author":"De Azevedo","year":"1997","journal-title":"Eur J Biochem"},{"key":"10.1124\/jpet.111.187104_bib10","doi-asserted-by":"crossref","first-page":"58","DOI":"10.1016\/j.neuropharm.2010.03.016","article-title":"Mechanisms of inhibition of CaV3.1 T-type calcium current by aliphatic alcohols","volume":"59","author":"Eckle","year":"2010","journal-title":"Neuropharmacology"},{"key":"10.1124\/jpet.111.187104_bib11","doi-asserted-by":"crossref","first-page":"733","DOI":"10.1002\/jnr.10872","article-title":"Calcium channel blockers in the treatment of disease","volume":"75","author":"Elmslie","year":"2004","journal-title":"J Neurosci Res"},{"key":"10.1124\/jpet.111.187104_bib12","doi-asserted-by":"crossref","first-page":"955","DOI":"10.1517\/13543784.12.6.955","article-title":"CDK inhibitors in clinical development for the treatment of cancer","volume":"12","author":"Fischer","year":"2003","journal-title":"Expert Opin Investig Drugs"},{"key":"10.1124\/jpet.111.187104_bib13","doi-asserted-by":"crossref","first-page":"C701","DOI":"10.1152\/ajpcell.00633.2008","article-title":"State-dependent block of HERG potassium channels by R-roscovitine: implications for cancer therapy","volume":"296","author":"Ganapathi","year":"2009","journal-title":"Am J Physiol Cell Physiol"},{"key":"10.1124\/jpet.111.187104_bib14","doi-asserted-by":"crossref","first-page":"115","DOI":"10.1016\/j.ceca.2006.04.014","article-title":"The pharmacology and regulation of T type calcium channels: new opportunities for unique therapeutics for cancer","volume":"40","author":"Gray","year":"2006","journal-title":"Cell Calcium"},{"key":"10.1124\/jpet.111.187104_bib15","doi-asserted-by":"crossref","first-page":"747","DOI":"10.1038\/sj.leu.2403295","article-title":"Cyclin-dependent kinase inhibitor roscovitine induces apoptosis in chronic lymphocytic leukemia cells","volume":"18","author":"Hahntow","year":"2004","journal-title":"Leukemia"},{"key":"10.1124\/jpet.111.187104_bib16","doi-asserted-by":"crossref","first-page":"3899","DOI":"10.1016\/j.bmcl.2008.06.034","article-title":"T-type Ca2+ channel blockers suppress the growth of human cancer cells","volume":"18","author":"Heo","year":"2008","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1124\/jpet.111.187104_bib17","doi-asserted-by":"crossref","first-page":"213","DOI":"10.1152\/jn.1992.68.1.213","article-title":"Kinetic and pharmacological properties of low voltage-activated Ca2+ current in rat clonal (GH3) pituitary cells","volume":"68","author":"Herrington","year":"1992","journal-title":"J Neurophysiol"},{"key":"10.1124\/jpet.111.187104_bib18","doi-asserted-by":"crossref","first-page":"682","DOI":"10.1038\/nchembio.118","article-title":"Network pharmacology: the next paradigm in drug discovery","volume":"4","author":"Hopkins","year":"2008","journal-title":"Nat Chem Biol"},{"key":"10.1124\/jpet.111.187104_bib19","doi-asserted-by":"crossref","first-page":"387","DOI":"10.1016\/j.cell.2008.04.019","article-title":"Xenohormesis: sensing the chemical cues of other species","volume":"133","author":"Howitz","year":"2008","journal-title":"Cell"},{"key":"10.1124\/jpet.111.187104_bib20","doi-asserted-by":"crossref","first-page":"3151","DOI":"10.1152\/jn.01031.2007","article-title":"Up-regulation of the T-type calcium current in small rat sensory neurons after chronic constrictive injury of the sciatic nerve","volume":"99","author":"Jagodic","year":"2008","journal-title":"J Neurophysiol"},{"key":"10.1124\/jpet.111.187104_bib21","doi-asserted-by":"crossref","first-page":"153","DOI":"10.1016\/0896-6273(89)90028-7","article-title":"On the resting potential of isolated frog sympathetic neurons","volume":"3","author":"Jones","year":"1989","journal-title":"Neuron"},{"key":"10.1124\/jpet.111.187104_bib22","doi-asserted-by":"crossref","first-page":"5014","DOI":"10.1016\/j.bmcl.2006.07.046","article-title":"Growth inhibition of human cancer cells in vitro by T-type calcium channel blockers","volume":"16","author":"Lee","year":"2006","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1124\/jpet.111.187104_bib23","doi-asserted-by":"crossref","first-page":"339","DOI":"10.3109\/07357907.2011.568565","article-title":"Blockade of T-type Ca2+ channels inhibits human ovarian cancer cell proliferation","volume":"29","author":"Li","year":"2011","journal-title":"Cancer Invest"},{"key":"10.1124\/jpet.111.187104_bib24","first-page":"1229","article-title":"A role of functional T-type Ca2+ channel in hepatocellular carcinoma cell proliferation","volume":"22","author":"Li","year":"2009","journal-title":"Oncol Rep"},{"key":"10.1124\/jpet.111.187104_bib25","doi-asserted-by":"crossref","first-page":"323","DOI":"10.1016\/S0006-3495(81)84899-0","article-title":"Relationship between presynaptic calcium current and postsynaptic potential in squid giant synapse","volume":"33","author":"Llin\u00e1s","year":"1981","journal-title":"Biophys J"},{"key":"10.1124\/jpet.111.187104_bib26","doi-asserted-by":"crossref","first-page":"2415","DOI":"10.1073\/pnas.79.7.2415","article-title":"Transmission by presynaptic spike-like depolarization in the squid giant synapse","volume":"79","author":"Llin\u00e1s","year":"1982","journal-title":"Proc Natl Acad Sci U S A"},{"key":"10.1124\/jpet.111.187104_bib27","doi-asserted-by":"crossref","first-page":"49","DOI":"10.1016\/j.ceca.2007.03.006","article-title":"T-type Ca2+ channel expression in human esophageal carcinomas: a functional role in proliferation","volume":"43","author":"Lu","year":"2008","journal-title":"Cell Calcium"},{"key":"10.1124\/jpet.111.187104_bib28","doi-asserted-by":"crossref","first-page":"302","DOI":"10.1016\/S0022-3565(24)38902-5","article-title":"Mibefradil block of cloned T-type calcium channels","volume":"295","author":"Martin","year":"2000","journal-title":"J Pharmacol Exp Ther"},{"key":"10.1124\/jpet.111.187104_bib29","doi-asserted-by":"crossref","first-page":"781","DOI":"10.1038\/sj.bjc.6602775","article-title":"hERG1 channels are overexpressed in glioblastoma multiforme and modulate VEGF secretion in glioblastoma cell lines","volume":"93","author":"Masi","year":"2005","journal-title":"Br J Cancer"},{"key":"10.1124\/jpet.111.187104_bib30","doi-asserted-by":"crossref","first-page":"1080","DOI":"10.1124\/mol.54.6.1080","article-title":"Mibefradil inhibition of T-type calcium channels in cerebellar purkinje neurons","volume":"54","author":"McDonough","year":"1998","journal-title":"Mol Pharmacol"},{"key":"10.1124\/jpet.111.187104_bib31","doi-asserted-by":"crossref","first-page":"527","DOI":"10.1111\/j.1432-1033.1997.t01-2-00527.x","article-title":"Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5","volume":"243","author":"Meijer","year":"1997","journal-title":"Eur J Biochem"},{"key":"10.1124\/jpet.111.187104_bib32","first-page":"285","article-title":"Voltage-gated potassium channels in cell proliferation","volume":"19","author":"Pardo","year":"2004","journal-title":"Physiology (Bethesda)"},{"key":"10.1124\/jpet.111.187104_bib33","doi-asserted-by":"crossref","first-page":"115","DOI":"10.1007\/s00232-005-0776-1","article-title":"Role of voltage-gated potassium channels in cancer","volume":"205","author":"Pardo","year":"2005","journal-title":"J Membr Biol"},{"key":"10.1124\/jpet.111.187104_bib34","doi-asserted-by":"crossref","first-page":"117","DOI":"10.1152\/physrev.00018.2002","article-title":"Molecular physiology of low-voltage-activated T-type calcium channels","volume":"83","author":"Perez-Reyes","year":"2003","journal-title":"Physiol Rev"},{"key":"10.1124\/jpet.111.187104_bib35","doi-asserted-by":"crossref","first-page":"1238","DOI":"10.1182\/blood-2006-02-003772","article-title":"VEGFR-1 (FLT-1), \u03b21 integrin, and hERG K+ channel for a macromolecular signaling complex in acute myeloid leukemia: role in cell migration and clinical outcome","volume":"110","author":"Pillozzi","year":"2007","journal-title":"Blood"},{"key":"10.1124\/jpet.111.187104_bib36","doi-asserted-by":"crossref","first-page":"181","DOI":"10.1016\/j.phrs.2008.01.009","article-title":"The hERG K+ channel: target and antitarget strategies in drug development","volume":"57","author":"Raschi","year":"2008","journal-title":"Pharmacol Res"},{"key":"10.1124\/jpet.111.187104_bib37","doi-asserted-by":"crossref","first-page":"185","DOI":"10.1085\/jgp.114.2.185","article-title":"State-dependent inactivation of the \u03b11G T-type calcium channel","volume":"114","author":"Serrano","year":"1999","journal-title":"J Gen Physiol"},{"key":"10.1124\/jpet.111.187104_bib38","doi-asserted-by":"crossref","first-page":"116","DOI":"10.1016\/j.canlet.2008.03.032","article-title":"Selective blockade of T-type Ca2+ channels suppresses human breast cancer cell proliferation","volume":"267","author":"Taylor","year":"2008","journal-title":"Cancer Lett"},{"key":"10.1124\/jpet.111.187104_bib39","doi-asserted-by":"crossref","first-page":"4984","DOI":"10.3748\/wjg.14.4984","article-title":"Calcium signaling and T-type calcium channels in cancer cell cycling","volume":"14","author":"Taylor","year":"2008","journal-title":"World J Gastroenterol"},{"key":"10.1124\/jpet.111.187104_bib40","doi-asserted-by":"crossref","first-page":"1659","DOI":"10.1172\/JCI36954","article-title":"Antagonism of T-type calcium channels inhibits high-fat diet-induced weight gain in mice","volume":"119","author":"Uebele","year":"2009","journal-title":"J Clin Invest"},{"key":"10.1124\/jpet.111.187104_bib41","doi-asserted-by":"crossref","first-page":"865","DOI":"10.1002\/jcb.21211","article-title":"Roscovitine-activated HIP2 kinase induces phosphorylation of wt p53 at Ser-46 in human MCF-7 breast cancer cells","volume":"100","author":"Wesierska-Gadek","year":"2007","journal-title":"J Cell Biochem"},{"key":"10.1124\/jpet.111.187104_bib42","doi-asserted-by":"crossref","first-page":"228","DOI":"10.1038\/msb.2008.60","article-title":"Finding multiple target optimal intervention in disease-related molecular network","volume":"4","author":"Yang","year":"2008","journal-title":"Mol Syst Biol"},{"key":"10.1124\/jpet.111.187104_bib43","doi-asserted-by":"crossref","first-page":"386","DOI":"10.1038\/sj.bjp.0707414","article-title":"Roscovitine, a cyclin-dependent kinase inhibitor, affects several gating mechanisms to inhibit cardiac L-type (CaV1.2) calcium channels","volume":"152","author":"Yarotskyy","year":"2007","journal-title":"Br J Pharmacol"},{"key":"10.1124\/jpet.111.187104_bib44","doi-asserted-by":"crossref","first-page":"43","DOI":"10.1074\/jbc.M109.076448","article-title":"Roscovitine binds to novel L-channel (CaV1.2) sites that separately affect activation and inactivation","volume":"285","author":"Yarotskyy","year":"2010","journal-title":"J Biol Chem"},{"key":"10.1124\/jpet.111.187104_bib45","doi-asserted-by":"crossref","first-page":"551","DOI":"10.1113\/jphysiol.2008.161737","article-title":"The Timothy syndrome mutation of cardiac CaV1.2 (L-type) channels: multiple altered gating mechanisms and pharmacological restoration of inactivation","volume":"587","author":"Yarotskyy","year":"2009","journal-title":"J Physiol"},{"key":"10.1124\/jpet.111.187104_bib46","doi-asserted-by":"crossref","first-page":"230","DOI":"10.1038\/nature09855","article-title":"Using induced pluripotent stem cells to investigate cardiac phenotypes in Timothy syndrome","volume":"471","author":"Yazawa","year":"2011","journal-title":"Nature"},{"key":"10.1124\/jpet.111.187104_bib47","doi-asserted-by":"crossref","first-page":"59","DOI":"10.2337\/diabetes.49.1.59","article-title":"Cloning of a T-type Ca2+ channel isoform in insulin-secreting cells","volume":"49","author":"Zhuang","year":"2000","journal-title":"Diabetes"}],"container-title":["The Journal of Pharmacology and Experimental Therapeutics"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0022356524467360?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0022356524467360?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/syndication.highwire.org\/content\/doi\/10.1124\/jpet.111.187104","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,2,20]],"date-time":"2025-02-20T02:42:15Z","timestamp":1740019335000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0022356524467360"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2012,2]]},"references-count":47,"journal-issue":{"issue":"2","published-print":{"date-parts":[[2012,2]]}},"alternative-id":["S0022356524467360"],"URL":"https:\/\/doi.org\/10.1124\/jpet.111.187104","relation":{},"ISSN":["0022-3565"],"issn-type":[{"value":"0022-3565","type":"print"}],"subject":[],"published":{"date-parts":[[2012,2]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Roscovitine Inhibits CaV3.1 (T-Type) Channels by Preferentially Affecting Closed-State Inactivation","name":"articletitle","label":"Article Title"},{"value":"The Journal of Pharmacology and Experimental Therapeutics","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1124\/jpet.111.187104","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2012 by The American Society for Pharmacology and Experimental Therapeutics","name":"copyright","label":"Copyright"}]}}