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File:ShK history.png

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Description
English: Timeline of ShK development. Used in v:WikiJournal_of_Science/ShK_toxin:_history,_structure_and_therapeutic_applications_for_autoimmune_diseases.
  1. Karlsson E, Adem A, Aneiros A, Castañeda O, Harvey AL, Jolkkonen M and Sotolongo V. New toxins from marine organisms. Toxicon. 1991;29:1168.
  2. Harvey AL, Anderson AJ, Rowan EG, Marshall DL, Castañeda O and Karlsson E. Dendrotoxin-like activity isolated from sea anemones. Br. J. Pharmac. 1991;104:34P.
  3. Castañeda O, Sotolongo V, Amor AM, Stöcklin R, Anderson AJ, Harvey AL, Engström A, Wernstedt C, Karlsson E. Characterization of a potassium channel toxin from the Caribbean Sea anemone Stichodactyla helianthus. Toxicon. 1995;33:603-13.
  4. Pennington MW, Byrnes ME, Zaydenberg I, Khaytin I, de Chastonay J, Krafte DS, Hill R, Mahnir VM, Volberg WA, Gorczyca W, et al. Chemical synthesis and characterization of ShK toxin: a potent potassium channel inhibitor from a sea anemone. Int J Pept Protein Res. 1995;46:354-8.
  5. Tudor JE, Pallaghy PK, Pennington MW, Norton RS. Solution structure of ShK toxin, a novel potassium channel inhibitor from a sea anemone. Nat Struct Biol. 1996;3:317-20.
  6. Pennington MW, Mahnir VM, Krafte DS, Zaydenberg I, Byrnes ME, Khaytin I, Crowley K, Kem WR. Identification of three separate binding sites on ShK toxin, a potent inhibitor of voltage-dependent potassium channels in human T-lymphocytes and rat brain. Biochem Biophys Res Commun. 1996;219:696-701.
  7. Pennington MW, Mahnir VM, Khaytin I, Zaydenberg I, Byrnes ME, Kem WR. An essential binding surface for ShK toxin interaction with rat brain potassium channels. Biochemistry. 1996;35:16407-11.
  8. Dauplais M, Lecoq A, Song J, Cotton J, Jamin N, Gilquin B, Roumestand C, Vita C, de Medeiros CL, Rowan EG, Harvey AL, Ménez A. On the convergent evolution of animal toxins. Conservation of a diad of functional residues in potassium channel-blocking toxins with unrelated structures. J Biol Chem. 1997;272:4302-9.
  9. Kalman K, Pennington MW, Lanigan MD, Nguyen A, Rauer H, Mahnir V, Paschetto K, Kem WR, Grissmer S, Gutman GA, Christian EP, Cahalan MD, Norton RS, Chandy KG. ShK-Dap22, a potent Kv1.3-specific immunosuppressive polypeptide. J Biol Chem. 1998;273:32697-707.
  10. Tudor JE, Pennington MW, Norton RS. Ionisation behaviour and solution properties of the potassium-channel blocker ShK toxin. Eur J Biochem. 1998;251:133-41.
  11. 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. 1999;274:21885-92.
  12. 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. 1999;38:14549-58.
  13. Lanigan MD, Tudor JE, Pennington MW, Norton RS. A helical capping motif in ShK toxin and its role in helix stabilization. Biopolymers. 2001;58:422-36.
  14. Beeton C, Wulff H, Barbaria J, Clot-Faybesse O, Pennington M, Bernard D, Cahalan MD, Chandy KG, Béraud E. Selective blockade of T lymphocyte K+ channels ameliorates experimental autoimmune encephalomyelitis, a model for multiple sclerosis. Proc Natl Acad Sci U S A. 2001;98:13942-7.
  15. 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. 2002;41:11963-71.
  16. Baell JB, Harvey AJ, Norton RS. Design and synthesis of type-III mimetics of ShK toxin. J Comput Aided Mol Des. 2002;16:245-62.
  17. 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. 2003;278:9928-37.
  18. Middleton RE, Sanchez M, Linde AR, Bugianesi RM, Dai G, Felix JP, Koprak SL, Staruch MJ, Bruguera M, Cox R, Ghosh A, Hwang J, Jones S, Kohler M, Slaughter RS, McManus OB, Kaczorowski GJ, Garcia ML. Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile. Biochemistry. 2003;42:13698-707.
  19. Beeton C, Pennington MW, Wulff H, Singh S, Nugent D, Crossley G, Khaytin I, Calabresi PA, Chen CY, Gutman GA, Chandy KG. Targeting effector memory T cells with a selective peptide inhibitor of Kv1.3 channels for therapy of autoimmune diseases. Mol Pharmacol. 2005;67:1369–1381.
  20. Beeton C, Wulff H, Standifer NE, Azam P, Mullen KM, Pennington MW, Kolski-Andreaco A, Wei E, Grino A, Counts DR, Wang PH, LeeHealey CJ, S Andrews B, Sankaranarayanan A, Homerick D, Roeck WW, Tehranzadeh J, Stanhope KL, Zimin P, Havel PJ, Griffey S, Knaus HG, Nepom GT, Gutman GA, Calabresi PA, Chandy KG. Kv1.3 channels: therapeutic target for T cell-mediated autoimmune diseases. Proc. Natl Acad. Sci. US. 2006;103:17414-17418.
  21. Tsang SW, Nguyen CQ, Hall DH, Chow KL. mab-7 encodes a novel transmembrane protein that orchestrates sensory ray morphogenesis in C. elegans. Dev Biol. 2007;312:353-66.
  22. Matheu MP, Beeton C, Garcia A, Chi V, Rangaraju S, Safrina O, Monaghan K, Uemura MI, Li D, Pal S, de la Maza LM, Monuki E, Flügel A, Pennington MW, Parker I, Chandy KG, Cahalan MD. Imaging of effector memory T cells during a delayed-type hypersensitivity reaction and suppression by Kv1.3 channel block. Immunity 2008;29:602–614.
  23. 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. Pharm. 2009;75:762-773.
  24. Rangaraju S, Khoo KK, Feng ZP, Crossley G, Nugent D, Khaytin I, Chi V, Pham C, Calabresi P, Pennington MW, Norton RS, Chandy KG. Potassium channel modulation by a toxin domain in matrix metalloprotease 23. J Biol Chem. 2010, 285:9124-36.
  25. Nguyen HM, Galea CA, Schmunk G, Smith BJ, Edwards RA, Norton RS, Chandy KG. Intracellular trafficking of the KV1.3 potassium channel is regulated by the prodomain of a matrix metalloprotease. J Biol Chem. 2013;288:6451-64.
  26. Galea CA, Nguyen HM, George Chandy K, Smith BJ, Norton RS. Domain structure and function of matrix metalloprotease 23 (MMP23): role in potassium channel trafficking. Cell Mol Life Sci. 2014;71:1191-210.
  27. Moogk D, da Silva IP, Ma MW, Friedman EB, de Miera EV, Darvishian F, Scanlon P, Perez-Garcia A, Pavlick AC, Bhardwaj N, Christos PJ, Osman I, Krogsgaard M. Melanoma expression of matrix metalloproteinase-23 is associated with blunted tumor immunity and poor responses to immunotherapy. J Transl Med. 2014;12:342.
  28. Pan T, Gröger H, Schmid V, Spring J. A toxin homology domain in an astacin-like metalloproteinase of the jellyfish Podocoryne carnea with a dual role in digestion and development. Dev Genes Evol. 1998;208:259-66.
  29. Gilhar A, Bergman R, Assay B, Ullmann Y, Etzioni A. The beneficial effect of blocking Kv1.3 in the psoriasiform SCID mouse model. J Invest Dermatol. 2011;131:118-24.
  30. Tarcha EJ et al. Durable pharmacological responses from the peptide drug ShK-186, a specific Kv1.3 channel inhibitor that suppresses T cell mediators of autoimmune disease. J Pharmacol Exp Ther. 2012;342:642-653.
  31. Chi V et al. Development of a sea anemone toxin as an immunomodulator for therapy of autoimmune diseases. Toxicon 2012,59:529-546.
  32. Chang SC, Galea CA, Leung EW, Tajhya RB, Beeton C, Pennington MW, Norton RS. Expression and isotopic labelling of the potassium channel blocker ShK toxin as a thioredoxin fusion protein in bacteria. Toxicon. 2012;60:840-50.
  33. Pennington MW, Harunur Rashid M, Tajhya RB, Beeton C, Kuyucak S, Norton RS. A C-terminally amidated analogue of ShK is a potent and selective blocker of the voltage-gated potassium channel Kv1.3. FEBS Lett. 2012;586:3996-4001.
  34. Dang B, Kubota T, Mandal K, Bezanilla F, Kent SB. Native chemical ligation at Asx-Cys, Glx-Cys: chemical synthesis and high-resolution X-ray structure of ShK toxin by racemic protein crystallography. J Am Chem Soc. 2013;135:11911-9.
  35. Upadhyay SK, Eckel-Mahan KL, Mirbolooki MR, Tjong I, Griffey SM, Schmunk G, Koehne A, Halbout B, Iadonato S, Pedersen B, Borrelli E, Wang PH, Mukherjee J, Sassone-Corsi P, Chandy KG. Selective Kv1.3 channel blocker as therapeutic for obesity and insulin resistance. Proc Natl Acad Sci U S A. 2013;110:E2239-48.
  36. Lioudyno MI, Birch AM, Tanaka BS, Sokolov Y, Goldin AL, Chandy KG, Hall JE, Alkire MT. Shaker-related potassium channels in the central medial nucleus of the thalamus are important molecular targets for arousal suppression by volatile general anesthetics. J Neurosci. 2013;33:16310-22.
  37. Peng Y, Lu K, Li Z, Zhao Y, Wang Y, Hu B, Xu P, Shi X, Zhou B, Pennington M, Chandy KG, Tang Y. Blockade of Kv1.3 channels ameliorates radiation-induced brain injury. Neuro Oncol. 2014;16:528-39.
  38. Chhabra S, Chang SC, Nguyen HM, Huq R, Tanner MR, Londono LM, Estrada R, Dhawan V, Chauhan S, Upadhyay SK, Gindin M, Hotez PJ, Valenzuela JG, Mohanty B, Swarbrick JD, Wulff H, Iadonato SP, Gutman GA, Beeton C, Pennington MW, Norton RS, Chandy KG. Kv1.3 channel-blocking immunomodulatory peptides from parasitic worms: implications for autoimmune diseases. FASEB J. 2014;28:3952-64.
  39. Murray JK, et al, Pharmaceutical optimization of peptide toxins for ion channel targets: Potent, selective, and long-lived antagonists of Kv1.3. J Med Chem. 2015;58:6784-802.
  40. Chang SC, Huq R, Chhabra S, Beeton C, Pennington MW, Smith BJ, Norton RS. N-Terminally extended analogues of the K⁺ channel toxin from Stichodactyla helianthus as potent and selective blockers of the voltage-gated potassium channel Kv1.3. FEBS J. 2015;282:2247-59.
  41. Zhao R, Dai H, Mendelman N, Cuello LG, Chill JH, Goldstein SA. Designer and natural peptide toxin blockers of the KcsA potassium channel identified by phage display. Proc Natl Acad Sci U S A. 2015;112:E7013-21.
  42. Zhang H, Du M, Xie J, Liu X, Sun J, Wang W, Xin X, Possani LD, Yea K, Lerner RA. Autocrine-based selection of drugs that target ion channels from combinatorial venom peptide libraries. Angew Chem Int Ed Engl. 2016;55:9306-10.
  43. Rangaraju S, Raza SA, Pennati A, Deng Q, Dammer EB, Duong D, Pennington MW, Tansey MG, Lah JJ, Betarbet R, Seyfried NT, Levey AI. A systems pharmacology-based approach to identify novel Kv1.3 channel-dependent mechanisms in microglial activation. J Neuroinflammation. 2017;14:128.
  44. Tarcha EJ, Olsen CM, Probst P, Peckham D, Muñoz-Elías EJ, Kruger JG, Iadonato SP. Safety and pharmacodynamics of dalazatide, a Kv1.3 channel inhibitor, in the treatment of plaque psoriasis: A randomized phase 1b trial. PLoS One. 2017;12:e0180762.
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