Browse result page of ImmunoSPdb

The total number entries retrieved from this search are 39
IDNameSequenceLengthChiralityN-Terminal ModificationC-Terminal ModificationChemical ModificationLinear/CyclicNatureSourceTargetMechanism of ActionIn vivo/ In vitroCell LineIC-50In vivo ModelAssay TypeLethal DoseCombination TherapyPubmed IDYear of Publication
1001Vm24AAAISCVGSPECPPKCRAQGCKNGKCMNRKCKCYYC36LNoneAmidationCross linked by eight cysteines (between Cys6 and Cys26, Cys12 and Cys31, Cys16 and Cys33, and Cys21 and Cys36) (Disulphide linkage)LinearNaturalVenom of the Mexican scorpion Vaejovis mexicanus smithiBlock Kv1.3 channels with high affinity, an estimated Kd of 2.9 pMInhibits T Cell Proliferation, CD25 Expression, and Ca2+ Signaling In Vitro and Suppresses DTH Reactions In VivoBothHuman peripheral T Cells, COS-7, human embryonic kidney 293, tsA201, L929, and MEL cellsNAFemale Lewis rats (9-10 weeks of age)T cell Proliferation assaysNANA226223632012
1003Native kalata B1GLPVCGETCVGGTCNTPGCTCSWPVCTRN29LNoneNoneThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailNatural cyclotideA cyclotide isolated from Oldenlandia affinis DC. (Rubiaceae)Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroHuman peripheral Lymphocytes2.9±1.3 micromolar for Lymphocytes (PBMCs)NACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1004Native kalata B2GLPVCGETCVGGTCNTPGCTCSWPVCTRN29LNoneNoneThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailNatural cyclotideA cyclotide isolated from Oldenlandia affinis DC. (Rubiaceae)Reduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroPurified T cells2.4±0.5 micromolar for purified T cellsNACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1005kalata B1 mutants [T20K]GLPVCGETCVGGTCNTPGCKCSWPVCTRN29LAddition of CysteineThioester linkerThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailSyntheticNAReduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroHuman peripheral Lymphocytes1.9±0.6 micromolar for Lymphocytes (PBMCs)NACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1006kalata B1 mutants [T20K]GLPVCGETCVGGTCNTPGCKCSWPVCTRN29LAddition of CysteineThioester linkerThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailSyntheticNAReduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroPurified T cells2.7±0.6 micromolar for purified T cellsNACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1007kalata B1 mutants [N29K]GLPVCGETCVGGTCNTPGCTCSWPVCTRK29LAddition of CysteineThioester linkerThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailSyntheticNAReduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroHuman peripheral Lymphocytes3.2±0.6 micromolar for Lymphocytes (PBMCs)NACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1008kalata B1 mutants [N29K]GLPVCGETCVGGTCNTPGCTCSWPVCTRK29LAddition of CysteineThioester linkerThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailSyntheticNAReduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroPurified T cells2.1±0.9 micromolar for purified T cellsNACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1009kalata B1 mutants [G18K]GLPVCGETCVGGTCNTPKCTCSWPVCTRN29LAddition of CysteineThioester linkerThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailSyntheticNAReduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroHuman peripheral Lymphocytes4.4±0.5 micromolar for Lymphocytes (PBMCs)NACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1010kalata B1 mutants [G18K]GLPVCGETCVGGTCNTPKCTCSWPVCTRN29LAddition of CysteineThioester linkerThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)Cyclic (head to tailSyntheticNAReduction of the IL-2 surface receptor CD25 expression (79%±10 after 24 hrs and 46%±18 after 36 hrs), also reduces TNF-α expression (23%±11)Suppress T-cell polyfunctionality and arrest the proliferation of immune-competent cells through inhibiting IL-2 biology at more than one site as IL-2) surface receptor as well as IL-2 cytokine secretion and IL-2 gene expression.In vitroPurified T cells3.2±1.8 micromolar for purified T cellsNACell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
1011OSK1 (α-KTx3.7)GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge C1-C4, C2-C5 and C3-C6)LinearNaturalVenom of the central Asian scorpion Orthochirus scrobiculosusKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.60±0.04 nM for Kv1.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1012OSK1 (α-KTx3.7)GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1C4, C2-C5 and C3-C6)LinearNaturalVenom of the central Asian scorpion Orthochirus scrobiculosusKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells5.40±1.89 nM for Kv1.2C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1013OSK1 (α-KTx3.7)GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C-C4, C2-C5 and C3-C6)LinearNaturalVenom of the central Asian scorpion Orthochirus scrobiculosusKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.014±0.001 nM for Kv1.3C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1014OSK1 (α-KTx3.7)GVIINVKCKISRQCLEPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge C1-C4, C2-C5 and C3-C6)LinearNaturalVenom of the central Asian scorpion Orthochirus scrobiculosusKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells225±10 nM for Kca 3.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1015[K16 ,D20 ]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.40± 0.01 nM for Kv1.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1016[K16 ,D20 ]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells2.96±0.01 nM for Kv1.2C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1017[K16 ,D20 ]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.003± 0.0011 nM for Kv1.3C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1018[K16 ,D20 ]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells228±92 nM for Kca 3.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel2.5 (μg/kg of mice)NA155882512005
1019[K16 ]-OSK1GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.63±0.05 nM for Kv1.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel3 (μg/kg of mice)NA155882512005
1020[K16 ]-OSK1GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells5.23±0.22 nM for Kv1.2C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel3 (μg/kg of mice)NA155882512005
1021[K16 ]-OSK1GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.067±0.006 nM for Kv1.3C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel3 (μg/kg of mice)NA155882512005
1022[K16 ]-OSK1GVIINVKCKISRQCLKPCKKAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells151±21 nM for Kca 3.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel3 (μg/kg of mice)NA155882512005
1023[D20 ]-OSK1GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells2.95±0.24 nM for Kv1.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel4.5 (μg/kg of mice)NA155882512005
1024[D20 ]-OSK1GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells77.8± 9.2 nM for Kv1.2C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel4.5 (μg/kg of mice)NA155882512005
1025[D20 ]-OSK1GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.037±0.007 nM for Kv1.3C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel4.5 (μg/kg of mice)NA155882512005
1026[D20 ]-OSK1GVIINVKCKISRQCLEPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells716±10 nM for Kca 3.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel4.5 (μg/kg of mice)NA155882512005
1027[P12 ,K16 , D20]-OSK1GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells3.18± 0.11 nM for Kv1.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel7.5 (μg/kg of mice)NA155882512005
1028[P12 ,K16 , D20]-OSK1GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells196±9 nM for Kv1.2C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel7.5 (μg/kg of mice)NA155882512005
1029[P12 ,K16 , D20]-OSK1GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.059±0.003 nM for Kv1.3C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel7.5 (μg/kg of mice)NA155882512005
1030[P12 ,K16 , D20]-OSK1GVIINVKCKISPQCLKPCKDAGMRFGKCMNGKCHCTPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2 and Kv 1.3 channel and also Ca2+ -activated KCa 3.1 channelPotent blocker of three different Kv channel types and a moderate blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells2600±400 nM for Kca 3.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel7.5 (μg/kg of mice)NA155882512005
1031[K16,D20,Y36]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channelBlocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells34.4±0.3 nM for Kv1.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel9 (μg/kg of mice)NA155882512005
1032[K16,D20,Y36]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channelBlocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells232±11 nM for Kv1.2C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel9 (μg/kg of mice)NA155882512005
1033[K16,D20,Y36]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channelBlocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells0.122± 0.007 nM for Kv1.3C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel9 (μg/kg of mice)NA155882512005
1034[K16,D20,Y36]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channelBlocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells1500±500 nM for Kv1.7C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel9 (μg/kg of mice)NA155882512005
1035[K16,D20,Y36]-OSK1GVIINVKCKISRQCLKPCKDAGMRFGKCMNGKCHCYPK38LNoneNoneThree- Disulphide-bridge (C1-C4, C2-C5 and C3-C6)LinearSyntheticNAKv 1.1, Kv 1.2, Kv 1.3 and Kv 1.7 channel and also Ca2+ -activated KCa 3.1 channelBlocker of four different Kv channel types and also blocker of Ca2+ -activated KCa 3.1 channelBothL929 and MEL (murine erythroleukaemia), COS-7 cells, tsA cell line, LTK-cells (lacking leucocyte tyrosine kinase), CHL (Chinese-hamster lung) cells, HEK-293 (human embryonic kidney) cells885±18 nM for Kca 3.1C57/BL6 miceNeurotoxicity of peptide, Pharmacological activity on various K+ (Potassium) channel9 (μg/kg of mice)NA155882512005
1051Vm24AAAISCVGSPECPPKCRAQGCKNGKCMNRKCKCYYC36LNoneAmidationFour Disulfide bridges (between Cys6 and Cys26, Cys12 and Cys31, Cys16 and Cys33, and Cys21 and Cys36)LinearNaturalvenom of the Mexican scorpion Vaejovis mexicanus smithiK+ channelRemarkable blocking potency and selectivity for Kv1.3 channelsBothMononuclear cells from human peripheral venous blood90% inhibition achieved at 100pMMouse modelLethality testNo toxicity for 50 to 200 μg of protein per mouse (20 g body weight)NA225401872012
1063Kalata B1GLPVCGETCVGGTCNTPGCTCSWPVCTRN29LNoneNoneThree cystine knot Disulfide connectivity (CI-CIV, CII-CV and CIII-CVI)CyclicNaturalFrom Oldenlandia affinis Plant ExtractNAInhibits the growth of the Lymphocytes in a cytostatic fashionIn vitroHuman Peripheral Blood Mononuclear Cells3.9±0.5 micromolar for antiproliferative effect on PBMCNACell Proliferation assay, Cell division assay14 micromolar of the peptide are cytotoxic to the cellsNA222727972012
1125Iberiotoxin (Venom peptide)XFTDVDCSVSKECWSVCKDLFGVDRGKCMGKKCRCYQ37LNoneNoneX=Pyroglutamic acid and disulfile linkage at Disulfide bridges: Cys7 - Cys28, Cys13 - Cys33, Cys17 - Cys35LinearNaturalButhus tamulus (scorpion)Blocker of several BK channelsBloackion channelsBothNANANANANANA243331932014
1126Kalata B1 (Cyclotide)GLPVCGETCVGGTCNTPGCTCSWPVCTRN29LNoneNoneThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)CyclicNaturalOldenlandia affinis (plant)IL-2Antiproliferative, IL2-dependent mechanismBothNANANANANANA243331932014
1128Magatoxin (Venom peptide)IINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH39LNoneNonedisulfide bridges between Cys 7-Cys29, Cys13-Cys34 and Cys17-Cys36LinearNaturalCentruroides margaritatus (scorpion)K+ channelPotassium channel blockerIn vivoNANANANANANA243331932014