Research Topics
| Heike WulffSummaryAffiliation: University of California Country: USA Publications
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Publications
K+ channel expression during B cell differentiation: implications for immunomodulation and autoimmunityHeike Wulff
Department of Medical Pharmacology and Toxicology, University of California, Davis, CA 95616, USA
J Immunol 173:776-86. 2004..These changes parallel those reported for T cells. Therefore, specific Kv1.3 and IKCa1 inhibitors may have use in therapeutic manipulation of selective lymphocyte subsets in immunological disorders...
K+ channels as targets for specific immunomodulationK George Chandy
Department of Physiology and Biophysics, University of California, Irvine, CA 92697, USA
Trends Pharmacol Sci 25:280-9. 2004..3 and IKCa1 channels, and provide a rationale for the potential therapeutic use of these inhibitors in immunological disorders...- Targeting effector memory T cells with the small molecule Kv1.3 blocker PAP-1 suppresses allergic contact dermatitisPhilippe Azam
Department of Medical Pharmacology and Toxicology, University of California, Davis, California 95616, USA
J Invest Dermatol 127:1419-29. 2007..Based on these results we propose that PAP-1 could potentially be developed into a drug for the topical treatment of inflammatory skin diseases such as psoriasis... - Potassium channel block by a tripartite complex of two cationophilic ligands and a potassium ionPavel I Zimin
Department of Pharmacology, University of California, Davis, California, USA
Mol Pharmacol 78:588-99. 2010..Our study provides a new concept for potassium channel block by cationophilic ligands... - Kv1.3 channels are a therapeutic target for T cell-mediated autoimmune diseasesChristine Beeton
Department of Physiology and Biophysics, University of California, Irvine, CA 92697, USA
Proc Natl Acad Sci U S A 103:17414-9. 2006..Repeated dosing with Kv1.3 inhibitors in rats has not revealed systemic toxicity. Further development of Kv1.3 blockers for autoimmune disease therapy is warranted... - A novel fluorescent toxin to detect and investigate Kv1.3 channel up-regulation in chronically activated T lymphocytesChristine Beeton
Department of Physiology and Biophysics, University of California, Irvine, California 92697, USA
J Biol Chem 278:9928-37. 2003..3 up-regulation. ShK-F6CA might be useful for rapid and quantitative detection of Kv1.3(high) expressing cells in normal and diseased tissues, and to visualize the distribution of functional channels in intact cells... - Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseasesAlexander Schmitz
Department of Medical Pharmacology and Toxicology, Genome and Biomedical Sciences Facility, Room 3502, 451 East Health Sciences Drive, University of California, Davis, Davis, CA 95616, USA
Mol Pharmacol 68:1254-70. 2005..PAP-1 and several of its derivatives therefore constitute excellent new tools to further explore Kv1.3 as a target for immunosuppression and could potentially be developed into orally available immunomodulators... - Targeting effector memory T-cells with Kv1.3 blockersHeike Wulff
University of California, Davis, Department of Medical Pharmacology, School of Medicine, Genome and Biomedical Sciences Facility, Davis, CA 95616, USA
Curr Opin Drug Discov Devel 10:438-45. 2007..3 in autoimmune diseases, reviews the progress made in both developing peptidic and small-molecule inhibitors for this challenging target, and in validating Kv1.3 as a target for the treatment of autoimmune diseases... - AMA production in primary biliary cirrhosis is promoted by the TLR9 ligand CpG and suppressed by potassium channel blockersYuki Moritoki
Division of Rheumatology, Allergy, and Clinical Immunology and the University of California at Davis, Davis, CA 95616, USA
Hepatology 45:314-22. 2007..Conclusion: These data suggest that the hyperresponsiveness of B cells in PBC accelerates B cell-mediated autoimmunity... - Potassium channels as therapeutic targets for autoimmune disordersHeike Wulff
University of California, Davis Department of Pharmacology and Toxicology, School of Medicine, Tupper Hall, One Shields Avenue, Davis, CA 95616, USA
Curr Opin Drug Discov Devel 6:640-7. 2003..3 blockers for the therapy of T-cell mediated autoimmune diseases... - 4-Phenoxybutoxy-substituted heterocycles--a structure-activity relationship study of blockers of the lymphocyte potassium channel Kv1.3Silke B Bodendiek
Department of Pharmacology, University of California, Davis, Genome and Biomedical Sciences Facility, 451 Health Sciences Drive, Davis, CA 95616, USA
Eur J Med Chem 44:1838-52. 2009..Taken together, our results demonstrate that the psoralen system is a crucial part of the pharmacophore of phenoxyalkoxypsoralen-type Kv1.3 blockers... - Modulators of small- and intermediate-conductance calcium-activated potassium channels and their therapeutic indicationsHeike Wulff
Department of Medical Pharmacology and Toxicology, University of California, Davis, CA 95616, USA
Curr Med Chem 14:1437-57. 2007..1 as a target for the treatment of traumatic and possibly ischemic brain injury. Taken together KCa2 and KCa3.1 channels constitute attractive new targets for several diseases that currently have no effective therapies... - K+ channel modulators for the treatment of neurological disorders and autoimmune diseasesHeike Wulff
Department of Pharmacology, University of California, Davis, California 95616, USA
Chem Rev 108:1744-73. 2008 
New light on the "old" chloride channel blocker DIDSHeike Wulff
Department of Pharmacology, University of California, Davis, 451 Health Sciences Drive, Davis, California 95616, USA
ACS Chem Biol 3:399-401. 2008..The DIDS tetra- and pentamer could potentially act as tethered blockers that simultaneously obstruct both chloride pathways in the dimeric CLC proteins...- The KCa3.1 blocker TRAM-34 reduces infarction and neurological deficit in a rat model of ischemia/reperfusion strokeYi Je Chen
Department of Pharmacology, Genome and Biomedical Sciences Facility, University of California, Davis, California 95616, USA
J Cereb Blood Flow Metab 31:2363-74. 2011..Our findings suggest that KCa3.1 blockade constitutes an attractive approach for the treatment of ischemic stroke because it is still effective when initiated 12 hours after the insult... - Spiro azepane-oxazolidinones as Kv1.3 potassium channel blockers: WO2010066840Heike Wulff
University of California, Department of Pharmacology, Davis, Davis, CA 95616, USA
Expert Opin Ther Pat 20:1759-65. 2010..This article briefly summarizes the chemistry and biological data provided in the patent and then compares the new compounds to Kv1.3 blockers previously disclosed by both academia and pharmaceutical companies... - Voltage-gated potassium channels as therapeutic targetsHeike Wulff
Department of Pharmacology, University of California, Davis, 451 Health Sciences Drive, GBSF Room 3502, Davis, California 95616, USA
Nat Rev Drug Discov 8:982-1001. 2009..1 (also known as EAG1 and KCNH1) and K(V)11.1 (also known as HERG and KCNH2) channels... - Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressureAnanthakrishnan Sankaranarayanan
Department of Pharmacology, University of California, Davis, California 95616, USA
Mol Pharmacol 75:281-95. 2009..The blood pressure-lowering effect of SKA-31 suggests KCa3.1 channel activation as a new therapeutic principle for the treatment of hypertension... - Amyloid-beta protein oligomer at low nanomolar concentrations activates microglia and induces microglial neurotoxicityIzumi Maezawa
Medical Investigation of Neurodevelopmental Disorders Institute, University of California, Davis, California 95618, USA
J Biol Chem 286:3693-706. 2011..Our results suggest that AβO, generally considered a neurotoxin, may more potently cause neuronal damage indirectly by activating microglia in AD... - Endothelial Small-Conductance and Intermediate-Conductance KCa Channels: An Update on Their Pharmacology and Usefulness as Cardiovascular TargetsHeike Wulff
Department of Pharmacology, University of California, Davis, CA Cardiovascular and Renal Research, Institute of Molecular Medicine, University of Southern Denmark, Odense, Denmark Aragon Institute of Health Sciences I CS and ARAID, Zaragoza, Spain
J Cardiovasc Pharmacol 61:102-12. 2013..1 and KCa2.3 modulators and critically assess the potential of KCa activators for the treatment of diabetes and cardiovascular diseases by improving endothelium-derived hyperpolarizations... - A simple device to illustrate the Einthoven triangleBenjamin E Jin
Department of Pharmacology, University of California, Davis, 95616, USA
Adv Physiol Educ 36:319-24. 2012..Combined with traditional demonstrations with ECG machines, this equipment demonstrated its ability to help medical students obtain a solid foundation of the basic principles of electrocardiography... - Microglial KCa3.1 Channels as a Potential Therapeutic Target for Alzheimer's DiseaseIzumi Maezawa
Department of Pathology and Laboratory Medicine, University of California Davis, Davis, CA 95616, USA
Int J Alzheimers Dis 2012:868972. 2012..1 blockers are well known, and a KCa3.1 blocker has been proven safe in clinical trials. It is therefore promising to reposition old or new KCa3.1 blockers for AD preclinical and clinical trials... - Therapeutic potential of K(Ca)3.1 blockers: recent advances and promising trendsHeike Wulff
University of California, Davis, CA, USA
Expert Rev Clin Pharmacol 3:385-96. 2010..This article will review the physiology and pharmacology of K(Ca)3.1 and critically examine the available preclinical and clinical data validating K(Ca)3.1 as a therapeutic target... - Modulation of mouse Paneth cell alpha-defensin secretion by mIKCa1, a Ca2+-activated, intermediate conductance potassium channelTokiyoshi Ayabe
Department of Pathology, College of Medicine, University of California, Irvine, California 92697 4800, USA
J Biol Chem 277:3793-800. 2002..These results demonstrate that mIKCa1 is modulator of Paneth cell alpha-defensin secretion and disclose an involvement in mucosal defense of the intestinal epithelium against ingested bacterial pathogens... - Targeting effector memory T cells with a selective peptide inhibitor of Kv1.3 channels for therapy of autoimmune diseasesChristine Beeton
Department of Physiology and Biophysics, 291 Irvine Hall, Medical School, University of California-Irvine, Irvine, CA 92697-4561, USA
Mol Pharmacol 67:1369-81. 2005..ShK(L5) prevents and treats experimental autoimmune encephalomyelitis and suppresses delayed type hypersensitivity in rats. ShK(L5) might prove useful for therapy of autoimmune disorders... - A new class of blockers of the voltage-gated potassium channel Kv1.3 via modification of the 4- or 7-position of khellinoneAndrew J Harvey
The Walter and Eliza Hall Institute of Medical Research Biotechnology Centre, 4 Research Avenue, La Trobe R and D Park, Bundoora 3086, Australia
J Med Chem 49:1433-41. 2006..3 with EC50 values of 480 and 400 nM, respectively. Both compounds exhibit moderate selectivity over other Kv1-family channels and HERG, are not cytotoxic, and suppress human T cell proliferation at low micromolar concentrations... - The voltage-gated Kv1.3 K(+) channel in effector memory T cells as new target for MSHeike Wulff
Department of Physiology and Biophysics, University of California Irvine, College of Medicine, Irvine, California 92697, USA
J Clin Invest 111:1703-13. 2003..Selective targeting of Kv1.3 in T(EM) cells may therefore hold therapeutic promise for MS and other T cell-mediated autoimmune diseases... - Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosisRalf Köhler
Department of Nephrology, Benjamin Franklin Medical Center, Berlin, Germany
Circulation 108:1119-25. 2003..In a rat model of balloon catheter injury (BCI), we investigated whether alterations in expression of Ca2+-activated K+ channels (KCa) contribute to intimal hyperplasia and vascular restenosis... - The 'functional' dyad of scorpion toxin Pi1 is not itself a prerequisite for toxin binding to the voltage-gated Kv1.2 potassium channelsStephanie Mouhat
Laboratoire International Associé d Ingénierie Biomoléculaire, Boulevard Pierre Dramard, 13916 Marseille Cedex 20, France
Biochem J 377:25-36. 2004..2 channels support an unexpected key role of specific basic amino acid residues, which form a basic ring (Arg-5, Arg-12, Arg-28 and Lys-31 residues), in toxin binding... - Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulatorsJulia Vennekamp
Pharmaceutical Institute, University of Kiel, Germany
Mol Pharmacol 65:1364-74. 2004..3 blockers may be useful as immunomodulators for the therapy of autoimmune disorders... - Khellinone derivatives as blockers of the voltage-gated potassium channel Kv1.3: synthesis and immunosuppressive activityJonathan B Baell
The Walter and Eliza Hall Institute of Medical Research Biotechnology Centre, 4 Research Avenue, La Trobe R and D Park, Bundoora 3086, Australia
J Med Chem 47:2326-36. 2004..3, aryl-substituted khellinone derivatives represent attractive lead compounds for the development of more potent and selective Kv1.3 blocking immunosuppressants... - The voltage-gated potassium channel Kv1.3 is highly expressed on inflammatory infiltrates in multiple sclerosis brainHorea Rus
Department of Neurology, The Johns Hopkins University School of Medicine, 600 North Wolfe Street, Baltimore, MD 21287, USA
Proc Natl Acad Sci U S A 102:11094-9. 2005..3(high)/CCR7(-) T(EM), suggesting that a subset of cerebrospinal fluid cells existed in a primed state ready to become T(EM). These studies provide further rationale for the use of specific Kv1.3 antagonists in MS... - Potassium channel blockade by the sea anemone toxin ShK for the treatment of multiple sclerosis and other autoimmune diseasesRaymond S Norton
Walter and Eliza Hall Institute of Medical Research, Parkville 3052, Victoria, Australia
Curr Med Chem 11:3041-52. 2004..ShK and its analogs are currently undergoing further evaluation as leads in the development of new biopharmaceuticals for the treatment of multiple sclerosis and other T-cell mediated autoimmune disorders... - Protein histidine phosphatase 1 negatively regulates CD4 T cells by inhibiting the K+ channel KCa3.1Shekhar Srivastava
Department of Pharmacology, New York University School of Medicine, New York, NY 10016, USA
Proc Natl Acad Sci U S A 105:14442-6. 2008.... - The intermediate-conductance calcium-activated potassium channel KCa3.1 contributes to atherogenesis in mice and humansKazuyoshi Toyama
Department of Medicine and Cardiovascular Center, Medical College of Wisconsin, Milwaukee, Wisconsin 53226, USA
J Clin Invest 118:3025-37. 2008..These data suggest that KCa3.1 blockers represent a promising therapeutic strategy for atherosclerosis... - International Union of Pharmacology. LII. Nomenclature and molecular relationships of calcium-activated potassium channelsAguan D Wei
Department of Anatomy and Neurobiology, Washington University School of Medicine, St. Louis, MO 63110, USA
Pharmacol Rev 57:463-72. 2005 - K+ channel types targeted by synthetic OSK1, a toxin from Orthochirus scrobiculosus scorpion venomStephanie Mouhat
Laboratoire Cellpep S A, 13 15 Rue Ledru Rollin, 13015 Marseille, France
Biochem J 385:95-104. 2005..3 channel, with an IC50 value of 0.003 nM, without loss of activity on K(Ca)3.1 channel. These data suggest that OSK1 or [K16,D20]-OSK1 could serve as leads for the design and production of new immunosuppressive drugs... - Characterisation of the human voltage-gated potassium channel gene, KCNA7, a candidate gene for inherited cardiac disorders, and its exclusion as cause of progressive familial heart block I (PFHBI)Soraya Bardien-Kruger
University of Stellenbosch Medical Research Council Centre for Molecular and Cellular Biology, Department of Medical Physiology and Biochemistry, University of Stellenbosch Medical School, Tygerberg, South Africa
Eur J Hum Genet 10:36-43. 2002..As ion channel-encoding genes have been implicated in a growing number of genetic conditions, the data presented may facilitate further analysis of the role of KCNA7 and its product in the heart... - International Union of Pharmacology. XLI. Compendium of voltage-gated ion channels: potassium channelsGeorge A Gutman
Department of Microbiology and Molecular Genetics, University of California Irvine, Irvine, CA 92697, USA
Pharmacol Rev 55:583-6. 2003..The complete Compendium, including data tables for each member of the potassium channel family can be found at http://www.iuphar-db.org/iuphar-ic/...