Key Publications
Papers by AIRMID Founders on K+ channels in lymphocytes and their inhibitors

 

   Rangaraju S, Chi V, Pennington MW, Chandy KG. Kv1.3 potassium channels as a therapeutic target in multiple sclerosis. Expert Opin Ther Targets. 13:909-24, 2009.

   Bodendiek SB, Mahieux C, Hänsel W, Wulff H. 4-Phenoxybutoxy-substituted heterocycles--a structure-activity relationship study of blockers of the lymphocyte potassium channel Kv1.3. Eur J Med Chem. 44:1838-52, 2009.

    Pennington MW, Beeton C, Galea CA, Smith BJ, Chi V, Monaghan KP, Garcia A, Rangaraju S, Giuffrida A, Plank D, Crossley G, Nugent D, Khaytin I, Lefievre Y, Peshenko I, Dixon C, Chauhan S, Orzel A, Inoue T, Hu X, Moore RV, Norton RS, Chandy KG. Engineering a stable and selective peptide blocker of the Kv1.3 channel in T lymphocytes. Mol Pharmacol. 75:762-73, 2009.

    Stokely ME, Garg P, Bhat MA, Koulen P. Transient 5-(4-phenylbutoxy)psoralen (PAP-1) treatment dissociates developing pathologies in autoimmune optic neuritis into two distinct pathology profiles. J Neurosci Res. 86:2111-24, 2008.

   Pereira LE, Villinger F, Wulff H, Sankaranarayanan A, Raman G, Ansari AA. Pharmacokinetics, toxicity, and functional studies of the selective Kv1.3 channel blocker 5-(4-phenoxybutoxy)psoralen in rhesus macaques. Exp Biol Med 232:1338-54, 2007.

   Azam P, Sankaranarayanan A, Homerick D, Griffey S, Wulff H. Targeting effector memory T cells with the small molecule Kv1.3 blocker PAP-1 suppresses allergic contact dermatitis. J Invest Dermatol. 2007 Jun;127(6):1419-29.

   Mullen KM, Rozycka M, Rus H, Hu L, Cudrici C, Zafranskaia E, Pennington MW, Johns DC, Judge SI, Calabresi PA. Potassium channels Kv1.3 and Kv1.5 are expressed on blood-derived dendritic cells in the central nervous system. Ann Neurol. 60:118-127, 2006.

   Schmitz A, Sankaranarayanan A, Azam P, Schmidt-Lassen K, Homerick D, Hänsel W, Wulff H. Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases. Mol Pharmacol 68:1254-70, 2005.

   Schmitz A, Sankaranarayanan A, Azam P, Schmidt-Lassen K, Homerick D, Hänsel W, Wulff H. Design of PAP-1, a selective small molecule Kv1.3 blocker, for the suppression of effector memory T cells in autoimmune diseases. Mol Pharmacol. 68(5):1254-70, 2005.

   Beeton C, Chandy KG. Potassium channels, memory T cells, and multiple sclerosis. Neuroscientist. 11:550-562, 2005.

    Devaux J, Beeton C, Beraud E, Crest M Ion channels and demyelination: basis of a treatment of experimental autoimmune encephalomyelitis (EAE) by potassium channel blockers. Rev Neurol (Paris). 160:S16-27, 2004.

    Baell JB, Gable RW, Harvey AJ, Toovey N, Herzog T, Hansel W, Wulff H. Khellinone derivatives as blockers of the voltage-gated potassium channel Kv1.3: synthesis and immunosuppressive activity. J Med Chem. 47:2326-2336, 2004.

    Vennekamp J, Wulff H, Beeton C, Calabresi PA, Grissmer S, Hansel W, Chandy KG. Kv1.3-blocking 5-phenylalkoxypsoralens: a new class of immunomodulators. Mol Pharmacol. 65:1364-1374, 2004.

    Beeton C, Wulff H, Singh S, Botsko S, Crossley G, Gutman GA, Cahalan MD, Pennington M, Chandy KG A novel fluorescent toxin to detect and investigate Kv1.3 channel up-regulation in chronically activated T lymphocytes. J Biol Chem. 278:9928-9937, 2003.

    Lanigan MD, Kalman K, Lefievre Y, Pennington MW, Chandy KG, Norton RS. Mutating a critical lysine in ShK toxin alters its binding configuration in the pore-vestibule region of the voltage-gated potassium channel, Kv1.3. Biochemistry.41:11963-11971, 2002.

    Baell JB, Harvey AJ, Norton RS. Design and synthesis of type-III mimetics of ShK toxin. Design and synthesis of type-III mimetics of ShK toxin. J Comput Aided Mol Des. 16:245-262, 2002.

    Cahalan, M.D., H. Wulff, and K.G. Chandy. Molecular properties and physiological roles of ion channels in T lymphocytes. Journal of Clinical Immunology 21:235-252, 2001.

    Fanger, C., H. Rauer, A.L. Neben, M.J. Miller, H. Rauer, H. Wulff, J.C. Rosa, C.R. Ganellin, K.G. Chandy, and M.D. Cahalan. Calcium-activated potassium channels sustain calcium signaling in T lymphocytes; Selective blockers and manipulated expression levels. Journal of Biological Chemistry 276:12249-12256, 2001.

    Lanigan MD, Tudor JE, Pennington MW, Norton RS. A helical capping motif in ShK toxin and its role in helix stabilization. Biopolymers. 58:422-436, 2001.

    Wulff H, Gutman GA, Cahalan MD, Chandy KG. Delineation of the clotrimazole/TRAM-34 binding site on the intermediate conductance calcium-activated potassium channel, IKCa1. J Biol Chem. 276:32040-32045, 2001.

   Chandy KG, Cahalan M, Pennington M, Norton RS, Wulff H, Gutman GA. Potassium channels in T lymphocytes: toxins to therapeutic immunosuppressants. Toxicon. 39:1269-1276, 2001.

   Rauer H, Lanigan MD, Pennington MW, Aiyar J, Ghanshani S, Cahalan MD, Norton RS, Chandy KG Structure-guided transformation of charybdotoxin yields an analog that selectively targets Ca2+-activated over voltage-gated K+ channels. J Biol Chem. 275:1201-1208, 2000.

   Strauss U, Wissel K, Jung S, Wulff H, Hansel W, Zhu J, Rolfs A, Mix E. K(+) channel-blocking alkoxypsoralens inhibit the immune response of encephalitogenic T line cells and lymphocytes from Lewis rats challenged for experimental autoimmune encephalomyelitis. Immunopharmacology, 48:51-63, 2000.

   Fanger CM, Neben AL, Cahalan MD Differential Ca2+ influx, KCa channel activity, and Ca2+ clearance distinguish Th1 and Th2 lymphocytes. J Immunol. 164:1153-1160, 2000.

   Rauer H, Pennington M, Cahalan M, Chandy KG. Structural conservation of the pores of calcium-activated and voltage-gated potassium channels determined by a sea anemone toxin. J Biol Chem. 274:21885-21892, 1999.

    Hanson DC, Nguyen A, Mather RJ, Rauer H, Koch K, Burgess LE, Rizzi JP, Donovan CB, Bruns MJ, Canniff PC, Cunningham AC, Verdries KA, Mena E, Kath JC, Gutman GA, Cahalan MD, Grissmer S, Chandy KG. UK-78,282, a novel piperidine compound that potently blocks the Kv1.3 voltage-gated potassium channel and inhibits human T cell activation. Br J Pharmacol. 126:1707-1716, 1999.

    Pennington MW, Lanigan MD, Kalman K, Mahnir VM, Rauer H, McVaugh CT, Behm D, Donaldson D, Chandy KG, Kem WR, Norton RS. Role of disulfide bonds in the structure and potassium channel blocking activity of ShK toxin. Biochemistry. 38:14549-14558, 1999.