icagen PUBLICATIONS

Castle N.A.
Pharmacological Modulation of Voltage-gated Potassium Channels as a Therapeutic Strategy
Expert Opinion on Therapeutic Patents. 2010, 20:1-33  

Gerlach AC, Stoehr SJ, Castle NA.

Pharmacological removal of hERG potassium Channel Inactivation by ICA-105574

Mol Pharmacol. 2010 (Epub ahead of print, Oct 5 2009)

Su X, Castle NA, Antonio B, Roeloffs R, Thomas JB, Krafte DS, Chapman ML.

The effect of kappa-opioid receptor agonists on tetrodotoxin-resistant sodium channels in primary sensory neurons.

Anesth Analg. 2009, 109:632-40

Wulff H, Castle NA, Pardo LA.

Voltage-gated Potassium Channels as Therapeutic Drug Targets.

Nature Reviews Drug Discovery. 2009, 8: 982-1001

Michael F. Gross, Neil A. Castle, Anruo Zou, Alan D. Wickenden, Weifeng Yu, Kerry L. Spear.
Aryl sulfonamido tetralin inhibitors of the Kv1.5 ion channel
Bioorganic & Medicinal Chemistry Letters Volume 19, Issue 11, June 2009, pp. 3063-3066

Neil Castle, David Printzenhoff, Shannon Zellmer, Brett Antonio, Alan Wickenden, Christopher Silvia

Sodium Channel Inhibitor Drug Discovery Using Automated High Throughput Electrophysiology Platforms

 Combinatorial Chemistry & High Throughput Screening. 2009, 12,107-122

Grant A. McNaughton-Smith, J. Ford Burns, Jonathan W. Stocker, Gregory C. Rigdon, Christopher Creech, Susan Arrington, Tara Shelton, Lucia de Franceschi

Novel Inhibitors of the Gardos Channel for the Treatment of Sickle Cell Disease

 J. Med.Chem. 2008, 51, 976–982

Wickenden AD., Krajewski J., London B., Wagoner P.K., Wilson W.A., Clark S., Roeloffs R., McNaugton-Smith G., Rigdon G.C.

W-(6-Chloro-pyridin-3-yl)-4-difluoro-benzamide (ICA-27243): A Novel Selective KCNQ2/Q3 Potassium Channel Activator
Mol Pharmacol.2008; 73: 977-986

Krafte DS, Bannon AW.
Sodium channels and nociception; recent concepts and therapeutic opportunitites
Current Opinion in Pharmcology, 2008, 8:50-56

Kenneth I Ataga, Wally R. Smith, Laura M De Castro, Paul Swerdlow, Yogen Saunthararajah, Oswaldo Castro, Elliot Vichinsky, Abdullah Kutlar, Eugene P. Orringer, Greg C Rigdon and Jonathan W. Stocker

Efficacy and safety of the Gardos channel blocker, Senicapoc (ICA-17043), in patients with sickle cell anemia

Blood doi;10.1182/blood-2007-08-110098

Jarvis M, Honore P, Shieh C, Chapman M,Joshi S, Zhang X, Kort M, Carroll W,

Marron B, Atkinson A, Thomas J, Liu D, Krambis M, Liu Y, McGaraughty S, Chu K, Roeloffs R, Zhong C, Mikusa J, Hernandez G, Gauvin D, Wade C, Zhu C, Pai M, Scanio M, Shi L, Drizin I, Gregg R, Matulenko M, Hakeem A, Gross M, Johnson M, Marsh K, Wagoner K, Sullivan J, Falynek C, Krafte D.

A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.

PNAS published online, 2007

Gross M, Beaudoin S, McNaughton-Smith G, Amato G, Castle N, Huang C, Zou A,

Yu W.
Aryl Sulfonamido Indane Inhibitors of the Kv1.5 Ion Channel.
Bioorganic & medicinal chemistry letters, 17, 2849, 2007

Castle N.
Aquaporins as targets for drug discovery.
Drug Discovery Today 10: 485-493, 2005.

Wickenden AD, Roeloffs R, McNaughton-Smith G, Rigdon GC.
KCNQ potassium channels: drug targets for the treatment of epilepsy and pain.
Expert Opin. Ther. Patents. 14: 457-469, 2004.

Gopalakrishnan M, Buckner SA, Shieh CC, Fey T, Fabiyi A, Whiteaker KL, Davis-Taber R, Milicic I, Daza AV, Scott VE, Castle NA, Printzenhoff D, London B, Turner SC, Carroll WA, Sullivan JP, Coghlan MJ, Brune ME.
In vitro and in vivo characterization of a novel naphthylamide ATP-sensitive K+ channel opener, A-151892.
Br J Pharmacol. 143:81-90 2004.

Stocker JW, De Franceschi L, McNaughton-Smith G, Corrocher R, Beauzard Y, Brugnara C.
ICA-17043, a novel Gardos channel blocker, prevents sickled red blood cells dehydration in vitro and in vivo in SAD mice.
Blood 101(6):2412-2418, 2003

Beaudoin S, Kinsey KE, Burns JF.
Preparation of unsymmetrical sulfonylureas from N, N'-Sulfuryldiimidazoles
Journal of Organic Chemistry. 68(1):115-119, 2003

Castle NA, London DO, Creech C, Fajloun Z, Stocker JW, Sabatier JM.
Maurotoxin: a potent inhibitor of intermediate conductance Ca2+ -activated potassium channels
Molecular Pharmacology. 63:409-18, 2003

Hadley JK, Passmore GM, Tatulian L, Al-Qatari M, Ye F, Wickenden AD, Brown DA.
Stoichiometry of expressed KCNQ2/KCNQ3 potassium channels and subunit composition of native ganglionic M channels deduced from block by tetraethylammonium
Journal of Neuroscience. 23(12):5012-9, 2003

Turner SC, Carroll WA, White TK, Brune ME, Buckner SA, Gopalakrishnan M, Fabiyi A, Coghlan MJ, Scott VE, Castle NA, Daza AV, Milicic I, Sullivan JP.
Structure-activity relationship of a novel class of naphthyl amide K(ATP) channel openers
Bioorganic Medicinal Chemistry Letters. 13:1741-4, 2003

van Rhee AM.
Use of recursion forests in the sequential screening process: consensus selection by multiple recursion trees
Journal of Chemical Information and Computer Sciences. 43:941-948, 2003

Zou A, Lin Z, Humble M, Creech C, Wagoner PK, Krafte D, Jegla T, Wickenden A.
Distribution and functional properties of human KCNH8 (Elk1) potassium channels
American Journal of Physiology (Cell Physiology). 285:C1356-C1366, 2003

Wickenden AD.
Potassium channels as anti-epileptic drug targets (Invited Review)
Neuropharmacology. 43(7):1055-60, 2003

Liu Y, Liu D, Krafte DS.
Decrease of inward rectification as a mechanism for arachidonic acid-induced potentiation of hKir2.3
European Biophysics Journal. 31(7):497-503, 2003

Gopalakrishnan M, Buckner SA, Whiteaker KL, Shieh CC, Molinari EJ, Milicic I, Daza AV, Davis-Taber R, Scott VE, Sellers D, Chess-Williams R, Chapple CR, Liu Y, Liu D, Brioni JD, Sullivan JP, Williams M, Carroll WA, Coghlan MJ.
(-)-(9S)-9-(3-Bromo-4-fluorophenyl)-2,3,5,6,7, 9-hexahydrothieno[3,2-b]quinolin-8(4H) -one 1,1-dioxide (A-278637): a novel ATP-sensitive potassium channel opener efficacious in suppressing urinary bladder contractions. I. In vitro characterization
Journal of Pharmacology and Experimental Therapeutics. 303:379-386, 2003

Wickenden AD.
Potassium channels as therapeutic drug targets. (Invited review)
Pharmacology & Therapeutics.94 :157-182, 2002

Liu Y, Liu D, Heath L, Meyers DM, Krafte DS, Wagoner PK, Silvia CP, Yu W, Curran ME.
Direct activation of an inwardly rectifying potassium channel by arachidonic acid
Molecular Pharmacology. 59(5):1061-1068, 2001

Liu Y, Liu D, Printzenhoff D, Coghlan MJ, Harris R, Krafte DS.
Tenidap, a novel anti-inflammatory agent, is an opener of the inwardly rectifying K+ channel hKir2.3
European Journal of Pharmacology. 435:153-160, 2002

Wickenden A, Zou A, Wagoner PK, Jegla T.
Characterization of KCNQ5/Q3 potassium channels expressed in mammalian cells
British Journal of Pharmacology. 132: 381-384, 2001

van Rhee MA, Stocker J, Printzenhoff D, Creech C, Wagoner PK, Spear KL.
Retrospective analysis of an experimental high-throughput screening data set by recursive partitioning
Journal of Combinatorial Chemistry. 3(3):267-277, 2001

Brenner R, Jegla TJ, Wickenden A, Liu Y, Aldrich RW.
Cloning and functional characterization of novel large conductance calcium-activated potassium channel beta subunits, hKCNMB3 and hKCNMB4
Journal of Biological Chemistry. 275(9):6453-61, 2000

Packer J, Conley E, Castle N, Wray D, January C, Patmore, L.
Internet resources for exploring gene family diversity
Trends in Pharmacological Sciences. 21: 327-329, 2000

Wickenden AD, Yu W, Zou A, Jegla T, Wagoner PK.
Retigabine, a novel anti-convulsant, enhances activation of KCNQ2/Q3 potassium channels
Molecular Pharmacology. 58(3): 591-600, 2000

Castle NA.
Recent advances in the biology of small conductance calcium-activated potassium channels. (Invited Review)
Perspectives in Drug Discovery and Design. 15/16:131-154, 1999

Wickenden AD, Jegla TJ, Kaprielian R, Backx PH.
Regional contributions of Kv1.4, Kv4.2, and Kv4.3 to transient outward K+ current in rat ventricle
American Journal Physiology. 276(5-2): H1599-1607,1999

Additional Publications of Interest

Wickenden AD, McNaughton-Smith G. 

Kv7 channels as targets for the treatment of pain.  Curr Pharm Des.  2009, 15(15):  1773-98.

Brown DA, Passmore GM. 

Neural KCNQ (Kv7) channels. 

Br J Pharmacol.  2009, 156(8):  185-95.

Gribkoff VK. 

The therapeutic potential of neuronal Kv7 (KCNQ) channel modulators:  an update.  Expert Opin Ther Targets.  2008, 12(5):  565-81.

Rogawski MA, Bazil CW. 

New molecular targets for antiepileptic drugs:  alpha(2)delta, SV2A, and Kv7/KCNQ/M potassium channels.  Curr Neurol Neurosci Rep.  2008, 8(4):  345-52.

Reimann F, Cox JJ, Belfer I, Diatchenko L, et al. 

Pain perception is altered by a nucleotide polymorphism in SCN9A. 

Proc Natl Acad ci USA.  2010, 107(11):  5148-54

Dib-Hajj SD, Black JA, Waxman SG.

Voltage-gated sodium channels:  therapeutic targets for pain. 

Pain Med.  2009, 19(7):  1260-69.

Cox JJ, Riemann F, Nicholas AK, Thornton G, et al. 

A SCN9A channelopathy causes congenital inability to experience pain. 

Nature  2006, 444(7121):  894-98.

Rech JC, Eckert WA, Maher MP, Banke T, Bhattacharya A, Wickenden AD. 

Recent advances in the biology and medicinal chemistry of TRPA1. 

Future Med Chem. 2010, 2(5):  843-858.

Kremeyer B, Lopera F, Cox JJ, Momin A, et al. 

A gain-of-function mutation in TRPA1 causes familial episodic pain syndrome.  Neuron.  2010, 66:  671-680.

McGaraughty S, Chu KL, Perner RJ, DiDomenico, Kort ME, Kym PR. 

TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic and inflamed rats.  Molecular Pain.  2010, 6:14.