Table 1.
Venom-derived peptide modulators of cation channels.
| Channel | Toxin | Species | IC50/Kd | Reference |
|---|---|---|---|---|
| Kir1.1 | Lq2 (α-KTx1.2) | Leiurus quinquestriatus | 410 nM | Lu and MacKinnon, 1997 |
| δ-DTX | Dendroaspis angusticeps | 150 nM | Imredy et al., 1998 | |
| Tertiapin (TPN) | Apis mellifera | 2 nM | Jin and Lu, 1998 | |
| Kir3.1/Kir3.4 | Tertiapin (TPN) | Apis mellifera | 8 nM | Jin and Lu, 1998 |
| Kv1.1 | α-DTx | Dendroaspis angusticeps | 20 nM | Grissmer et al., 1994 |
| DTx K (toxin I) | Dendroaspis polylepis | 50 nM | Robertson and Owen, 1993 | |
| α-KTx 2.2 (margatoxin) | Centruroides margaritatus | 4.2 nM | Bartok et al., 2014 | |
| α-KTx 2.5 (hongotoxin) | Centruroides limbatus | 31 pM | Koschak et al., 1998 | |
| α-KTx 3.13 | Mesobuthus eupeus | 203 pM | Gao et al., 2010 | |
| ShK | Stichodactyla helianthus | 16 pM | Kalman et al., 1998 | |
| Kv1.2 | α-DTx | Dendroaspis angusticeps | 17 nM | Grissmer et al., 1994 |
| α-KTx 1.1 (Charybdotoxin) | Leiurus quinquestriatus hebraeus | 9 nM | Takacs et al., 2009 | |
| α-KTx 10.1 (Cobatoxin-1) | Centruroides noxius | 27 nM | Jouirou et al., 2004 | |
| α-KTx 2.1 (Noxiustoxin) | Centruroides noxius | 2 nM | Grissmer et al., 1994 | |
| α-KTx 2.2 (margatoxin) | Centruroides margaritatus | 6 pM | Bartok et al., 2014 | |
| α-KTx 2.5 (hongotoxin) | Centruroides limbatus | 0.17 nM | Koschak et al., 1998 | |
| α-KTx 3.6 (mesomartoxin) | Mesobuthus martensii | 15 nM | Wang et al., 2015 | |
| α-KTx 6.4 | Pandinus imperator | 8 pM | Sarrah et al., 2003 | |
| α-KTx-6.2 (Maurotoxin) | Scorpio maurus palmatus | 0.8 nM | Ryadh et al., 2018 | |
| α-KTx-6.21 (Urotoxin) | Urodacus yaschenkoi | 160 pM | Luna-Ramírez et al., 2014 | |
| ShK | Stichodactyla helianthus | 9 nM | Kalman et al., 1998 | |
| BscTx1 | Bunodosoma caissarum | 30 pM | Orts et al., 2013 | |
| Kv1.3 | α-KTx 6.12 (Anuroctoxin) | Anuroctonus phaiodactylus | 0.73 nM | Bagdáany et al., 2005 |
| α-KTx 3.12 (Aam-KTX) | Androctonus amoreuxi | 1.1 nM | Abbas et al., 2008 | |
| α-KTx 2.1 (Noxiustoxin) | Centruroides noxius | 1 nM | Grissmer et al., 1994 | |
| α-KTx 2.2 (margatoxin) | Centruroides margaritatus | 11 pM | Bartok et al., 2014 | |
| α-KTx 2.5 (hongotoxin) | Centruroides limbatus | 86 nM | Koschak et al., 1998 | |
| α-KTx 6.15 (Hemitoxin) | Hemiscorpius lepturus | 2 nM | Najet et al., 2008 | |
| α-KTx 6.3 (Neurotoxin) | Heterometrus spinifer | 12 pM | Lebrun et al., 1997 | |
| α-KTx 3.2 (Agitoxin-2) | Leiurus quinquestriatus hebraeus | 200 pM | Garcia et al., 1994 | |
| α-KTx 12.5 (LmKTx10) | Lychas mucronatus | 28 nM | Liu et al., 2009 | |
| α-KTx 3.11 | Odonthobuthus doriae | 7.2 nM | Abdel-Mottaleb et al., 2008 | |
| α-KTx3.7 | Orthochirus scrobiculosus | 14 pM | Mouhat et al., 2005 | |
| α-KTx 23.1 (Vm24) | Vaejovis mexicanus smithi | 2.9 pM | Varga et al., 2012 | |
| ShK | Stichodactyla helianthus | 11 pM | Kalman et al., 1998 | |
| Kv1.6 | α-DTx | Dendroaspis angusticeps | 9 nM | Swanson et al., 1990 |
| α-KTx 1.1 (Charybdotoxin) | Leiurus quinquestriatus hebraeus | 22 nM | Garcia et al., 1994 | |
| α-KTx 3.2 (Agitoxin-2) | Leiurus quinquestriatus hebraeus | 37 pM | Garcia et al., 1994 | |
| ShK | Stichodactyla helianthus | 165 pM | Kalman et al., 1998 | |
| BcSTx1/BcSTx2 | Bunodosoma caissarum | 1.3 nM/7.7 nM | Orts et al., 2013 | |
| Kv2.1 | HaTx1 (Hanatoxin) | Grammostola spatulata | 42 nM | Swartz and MacKinnon, 1995 |
| JZTX-III/JZTX-XI | Chilobrachys jingzhao | 710 nM/390 nM | Tao et al., 2013, 2016 | |
| ScTx1 | Stromatopelma calceata | 12.7 nM | Escoubas et al., 2002 | |
| Kv2.2 | ScTx1 | Stromatopelma calceata | 21.4 nM | Escoubas et al., 2002 |
| Kv3.2 | ShK | Stichodactyla helianthus | 6 nM | Yan et al., 2005 |
| Kv3.4 | BDS-I/BDS-II | Anemonia sulcata | 47 nM/56 nM | Diochot et al., 1998 |
| Kv4.1 | JZTX-XII | Chilobrachys jingzhao | 363 nM | Yuan et al., 2007 |
| Kv4.2 | PaTx1/PaTx2 | Phrixotrichus auratus | 5 nM/34 nM | Diochot et al., 1999 |
| ScTx1 | Stromatopelma calceata | 1.2 nM | Escoubas et al., 2002 | |
| TsTx-Kβ (Ts8) | Tityus serrulatus | 652 nM | Pucca et al., 2016 | |
| HpTx3 (Heteropodatoxin) | Heteropoda venatoria | 67 nM | Sanguinetti et al., 1997 | |
| JZTX-V | Chilobrachys jingzhao | 604.2 nM | Zeng et al., 2007 | |
| Kv4.3 | PaTx1/PaTx2 | Phrixotrichus auratus | 28 nM/71 nM | Diochot et al., 1999 |
| SNX-482 | Hysterocrates gigas | 3 nM | Kimm and Bean, 2014 | |
| KCa1.1 | α-KTx1.1 (Charybdotoxin) | Leiurus quinquestriatus | 2.9 nM | Rauer et al., 2000 |
| α-KTx 1.3 (Iberiotoxin) | Mesobuthus tamulus | 1.7 nM | Candia et al., 1992 | |
| α-KTx 1.5 (BmTx1) | Buthus martensi Karsch | 0.6 nM | Romi-Lebrun et al., 1997 | |
| α-KTx 1.6 (BmTx2) | Buthus martensi Karsch | 0.3 nM | Romi-Lebrun et al., 1997 | |
| α-KTx 1.11 (Slotoxin) | Centruroides noxius | 1.5 nM | Garcia-Valdes et al., 2001 | |
| α-KTx 3.1 (Kaliotoxin) | Androctonus mauretanicus | 20 nM | Crest et al., 1992 | |
| α-KTx 3.5 (Kaliotoxin2) | Androctonus australis | 135 nM | Crest et al., 1992 | |
| α-KTx 12.1 (Butantoxin) / TsTX-IV | Tityus serrulatus | 50 nM | Novello et al., 1999 | |
| α-KTx (BmP09) | Buthus martensi Karsch | 27 nM | Yao et al., 2005 | |
| Natrin | Naja naja atra | 34.4 nM | Wang et al., 2005 | |
| KCa2.1 | α-KTx 5.1 (Leiurotoxin I/scyllatoxin) | Leiurus quinquestriatus hebraeus | 325 nM | Castle and Strong, 1986 |
| Tamapin | Mesobuthus tamulus | 32 nM | Pedarzani et al., 2002 | |
| Apamin | Apis mellifera | 8 nM | Hugues et al., 1982 | |
| KCa2.2 | α-KTx 5.1 (Leiurotoxin I/scyllatoxin) | Leiurus quinquestriatus hebraeus | 200 pM | Castle and Strong, 1986 |
| PO5 | Androctonus mauretanicus | 22 nM | Zerrouk et al., 1993 | |
| Tamapin | Mesobuthus tamulus | 24 pM | Pedarzani et al., 2002 | |
| Apamin | Apis mellifera | 30-200 pM | Hugues et al., 1982 | |
| TsK | Tityus serrulatus | 80 nM | Lecomte et al., 1999 | |
| KCa2.3 | α-KTx 5.1 (Leiurotoxin I/scyllatoxin) | Leiurus quinquestriatus hebraeus | 1.1 nM | Castle and Strong, 1986 |
| PO5 | Androctonus mauretanicus | 25 nM | Zerrouk et al., 1993 | |
| Tamapin | Mesobuthus tamulus | 1.7 nM | Pedarzani et al., 2002 | |
| Apamin | Apis mellifera | 10 nM | Hugues et al., 1982 | |
| TsK | Tityus serrulatus | 197 nM | Lecomte et al., 1999 | |
| KCa3.1 | α-KTx 1.1 (Charybdotoxin) | Leiurus quinquestriatus hebraeus | 5 nM | Ghanshani et al., 2000; Rauer et al., 2000 |
| α-KTx 6.2 (Maurotoxin) | Maurus palmatus | 1 nM | Castle, 2003 | |
| Margatoxin | Centruroides margaritatus | 459 nM | Garcia-Calvo et al., 1993 | |
| α-KTx 3.7 (OSK1) | Orthochirus scrobiculosus | 225 nM | Mouhat et al., 2005 | |
| ShK | Stichodactyla helianthus | 30 nM | Pennington et al., 1995 | |
| BgK | Bunodosoma granulifera | 172 nM | Cotton et al., 1997 | |
| Nav1.1 | MeuNaTxα-12 | Mesobuthus eupeus | 0.91 μM | Zhu et al., 2012 |
| MeuNaTxα-13 | Mesobuthus eupeus | 2.5 μM | Zhu et al., 2012 | |
| ATX-II | Anemonia sulcata | 6 nM | Chahine et al., 1996; Oliveira et al., 2004 | |
| Cangitoxin-II; CGTX-II | Bunodosoma cangicum | 0.165 μM | Zaharenko et al., 2012 | |
| Bc-III | Bunodosoma caissarum | 300 nM | Oliveira et al., 2004 | |
| AFT-II | Anthopleura fuscoviridis | 391 nM | Oliveira et al., 2004 | |
| GVIIJSSG | Conus geographus | 11 nM | Gajewiak et al., 2014 | |
| μ-Conotoxin BuIIIA | Conus bullatus | 0.35 μM | Wilson et al., 2011 | |
| Nav1.2 | Huwentoxin IV | Haplopelma schmidti | 150 nM | Minassian et al., 2013 |
| ATX-II | Anemonia sulcata | 41 nM | Oliveira et al., 2004 | |
| Bc-III | Bunodosoma caissarum | 1449 nM | Oliveira et al., 2004 | |
| AFT-II | Anthopleura fuscoviridis | 1998 nM | Oliveira et al., 2004 | |
| Lqh-2 | Leiurus quinquestriatus hebraeus | 1.8 nM | Chen et al., 2002 | |
| PnTx1 | Phoneutria nigriventer | 33.7 nM | Silva et al., 2012 | |
| Phrixotoxin 3 (PaurTx3) | Phrixotrichus auratus | 0.6 nM | Bosmans et al., 2006 | |
| ProTx-III | Thrixopelma pruriens | 0.3 μM | Cardoso et al., 2015 | |
| Hainantoxin-IV | Ornithoctonus hainana | 36 nM | Liu et al., 2003 | |
| GrTx1 | Grammostola rosea | 0.23 μM | Redaelli et al., 2010 | |
| GVIIJSSG | Conus geographus | 11 nM | Gajewiak et al., 2014 | |
| μ-conotoxin TIIIA | Conus tulipa | 0.045 μM | Wilson et al., 2011 | |
| μ-conotoxin SIIIA | Conus striatus | 0.05 μM | Wilson et al., 2011 | |
| μ-conotoxin KIIIA | Conus kinoshitai | 0.003 μM | Wilson et al., 2011 | |
| μ-conotoxin MIIIA | Conus magus | 0.45 μM | Wilson et al., 2011 | |
| μ-conotoxin BuIIIA | Conus bullatus | 0.012 μM | Wilson et al., 2011 | |
| Nav1.3 | AFT-II | Anthopleura fuscoviridis | 460 nM | Oliveira et al., 2004 |
| ATX-II | Anemonia sulcata | 759 nM | Oliveira et al., 2004 | |
| Bc-III | Bunodosoma caissarum | 1458 nM | Oliveira et al., 2004 | |
| ProTx-III | Thrixopelma pruriens | 0.9 μM | Cardoso et al., 2015 | |
| Hainantoxin-IV | Ornithoctonus hainana | 375 nM | Liu et al., 2003 | |
| GrTx1 | Grammostola rosea spider | 0.77 μM | Redaelli et al., 2010 | |
| GVIIJSSG | Conus geographus | 15 nM | Gajewiak et al., 2014 | |
| μ-conotoxin BuIIIA | Conus bullatus | 0.35 μM | Wilson et al., 2011 | |
| Nav1.4 | AFT-II | Anthopleura fuscoviridis | 31 nM | Oliveira et al., 2004 |
| ATX-II | Anemonia sulcata | 109 nM | Oliveira et al., 2004 | |
| Bc-III | Bunodosoma caissarum | 821 nM | Oliveira et al., 2004 | |
| MrVIB (μO-Conotoxin) | Conus marmoreus | 222 nM | Zorn et al., 2006 | |
| MfVIA (μO-Conotoxin) | Conus magnificus | 81 nM | Vetter et al., 2012 | |
| GrTx1 | Grammostola rosea | 1.3 μM | Redaelli et al., 2010 | |
| GVIIJSSG | Conus geographus | 47 nM | Gajewiak et al., 2014 | |
| μ-conotoxin TIIIA | Conus tulipa | 0.005 μM | Wilson et al., 2011 | |
| μ-conotoxin SIIIA | Conus striatus | 0.13 μM | Wilson et al., 2011 | |
| μ-conotoxin MIIIA | Conus magus | 0.33 μM | Wilson et al., 2011 | |
| μ-conotoxin BuIIIA | Conus bullatus | 0.012 μM | Wilson et al., 2011 | |
| Nav1.5 | ProTx-II | Thrixopelma pruriens | 79 nM | Middleton et al., 2002 |
| ATX-II | Anemonia sulcata | 49 nM | Oliveira et al., 2004 | |
| AFT-II | Anthopleura fuscoviridis | 62.5 nM | Oliveira et al., 2004 | |
| Bc-III | Bunodosoma caissarum | 307 nM | Oliveira et al., 2004 | |
| CGTX-II | Bunodosoma cangicum | 50 nM | Zaharenko et al., 2012 | |
| Nav1.6 | ATX-II | Anemonia sulcata | 180 nM | Oliveira et al., 2004 |
| AFT-II | Anthopleura fuscoviridis | 300 nM | Oliveira et al., 2004 | |
| Bc-III | Bunodosoma caissarum | 900 nM | Oliveira et al., 2004 | |
| ProTx-II | Thrixopelma pruriens | 47 nM | Maertens et al., 2006 | |
| CGTX-II | Bunodosoma cangicum | 50 nM | Zaharenko et al., 2012 | |
| ProTx-III | Thrixopelma pruriens | 0.29 μM | Cardoso et al., 2015 | |
| GrTx1 | Grammostola rosea spider | 0.63 μM | Redaelli et al., 2010 | |
| Nav1.7 | ProTx-I | Thrixopelma pruriens | 51 nM | Middleton et al., 2002 |
| ProTx-II | Thrixopelma pruriens | 300 pM | Schmalhofer et al., 2008 | |
| ProTx-III | Thrixopelma pruriens | 2.1 nM | Cardoso et al., 2015 | |
| Lqh-2 | Leiurus quinquestriatus hebraeus | 32 nM | Chen et al., 2002 | |
| Lqh-3 | Leiurus quinquestriatus hebraeus | 13.6 nM | Chen et al., 2002 | |
| GpTx-1 | Grammostola porteri | 10 nM | Murray et al., 2015 | |
| μ-SLPTX-Ssm6a | Scolopendra subspinipes mutilans | 25 nM | Yang et al., 2013 | |
| Hainantoxin-IV | Ornithoctonus hainana | 21 nM | Liu et al., 2003 | |
| μ-TRTx-Pn3a | Pamphobeteus nigricolor | 0.9 nM | Deuis et al., 2017 | |
| GrTx1 | Grammostola rosea | 0.37 μM | Redaelli et al., 2010 | |
| GVIIJSSG | Conus geographus | 41 nM | Gajewiak et al., 2014 | |
| Huwentoxin-IV | Haplopelma schmidti | 26 nM; 0.4 nM | Xiao et al., 2008; Rahnama et al., 2017 | |
| Nav1.8 | ProTx-I | Thrixopelma pruriens | 27 nM | Middleton et al., 2002 |
| MrVIB (μO-Conotoxin) | Conus marmoreus | 102 nM | Ekberg et al., 2006 | |
| MfVIA (μO-Conotoxin) | Conus magnificus | 529 nM | Vetter et al., 2012 | |
| HSTX-I | Haemadipsa sylvestris | 2.44 μM | Wang et al., 2018 | |
| Nav1.9 | HSTX-I | Haemadipsa sylvestris | 3.30 μM | Wang et al., 2018 |
| Cav1.2 | Calciseptine | Dendroaspis polylepis polylepis | 430 nM | de Weille et al., 1991 |
| Cav2.1 | ω-conotoxin CVIB | Conus catus | 7.7 nM | Lewis et al., 2000 |
| ω-conotoxin CVIC | Conus catus | 7.6 nM | Lewis et al., 2000 | |
| ω-conotoxin MVIIC | Conus magus | 7 nM | Lewis et al., 2000 | |
| ω-agatoxin IVA | Agelenopsis aperta | 0.1 μM | Mintz et al., 1992 | |
| ω-grammotoxin SIA | Grammostola rosea | 50 nM | Lampe et al., 1993; McDonough et al., 1997 | |
| Cav2.2 | ω-agatoxin IIA | Agelenopsis aperta | 10 nM | Bindokas and Adams, 1989; Adams et al., 1990 |
| ω-agatoxin IIIA | Agelenopsis aperta | 1.4 nM | Ertel et al., 1994; Olivera et al., 1994 | |
| ω-agatoxin IIIB | Agelenopsis aperta | 140 nM | Ertel et al., 1994; Yan and Adams, 2000 | |
| ω-agatoxin IIID | Agelenopsis aperta | 35 nM | Ertel et al., 1994 | |
| ω-ctenitoxin-Pn3a/Neurotoxin Tx3–4 | Phoneutria nigriventer | 50 pM | Cordeiro Mdo et al., 1993 | |
| ω-conotoxin CVIA | Conus catus | 0.6 nM | Lewis et al., 2000 | |
| ω-conotoxin CVIB | Conus catus | 7.7 nM | Lewis et al., 2000 | |
| ω-conotoxin CVIC | Conus catus | 7.6 nM | Lewis et al., 2000 | |
| ω-conotoxin CVID | Conus catus | 0.07 nM | Lewis et al., 2000 | |
| ω-conotoxin MVIIA | Conus magus | 0.055 nM | Lewis et al., 2000 | |
| ω-conotoxin GVIA | Conus geographus | 0.04 nM | Olivera et al., 1984; Lewis et al., 2000 | |
| Cav2.3 | SNX482 | Hysterocrates gigas | 15–30 nM | Newcomb et al., 1998 |
| Cav3.1 | Kurtoxin | Parabuthus transvaalicus | 15–50 nM | Chuang et al., 1998; Sidach and Mintz, 2002 |
| ProTx1 | Thrixopelma pruriens | 200 nM | Ohkubo et al., 2010 | |
| Cav3.2 | Kurtoxin | Parabuthus transvaalicus | 25–50 nM | Chuang et al., 1998; Sidach and Mintz, 2002 |