Browse result page of ImmunoSPdb

The total number entries retrieved from this search are 52
IDNameSequenceLengthChiralityN-Terminal ModificationC-Terminal ModificationChemical ModificationLinear/CyclicNatureSourceTargetMechanism of ActionIn vivo/ In vitroCell LineIC-50In vivo ModelAssay TypeLethal DoseCombination TherapyPubmed IDYear of Publication
1002Cyclosporin A (CsA)cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFungusReduction of the IL-2 surface receptor CD25 expression (76%±11 after 24 hrs and 62%±7.3 after 36 hrs), also reduces TNF-α expression (23%±1.8)Inhibits the production of IL-2In vitroHuman peripheral Lymphocytes and purified T cellsNANoneCell Proliferation assay, Ca2+ release assay, Cytokines release assayNANA238408032013
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
1036Cyclosporin Acyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFrom fungus Trichoderma polysporumInhibit IL-2 production by activated CD4+ T-cellsInhibiting the calcineurin pathwayBothPeripheral blood mononuclear cells (PBMCs)61.8 nM for CD4+ T cell activation of IL-2 productionC57/B6 miceMIC assay, Immunosuppression and toxicity testNANA185998252008
1037Colutellin AVISIIPV7LNoneNoneNoneCyclicNaturalEndophytic fungus Colletotrichum dematiumInhibit IL-2 production by activated CD4+ T-cellsInhibiting the calcineurin pathwayBothPeripheral blood mononuclear cells (PBMCs)167.3±0.38 nM for CD4+ T cell activation of IL-2 productionC57/B6 miceMIC assay, Immunosuppression and toxicity testMIC of 3.6 mg/ml (48 h) against Botrytis cinerea and Sclerotinia sclerotiorum.NA185998252008
1044Cyclosporin Acyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFrom fungus Trichoderma polysporumCa2+-dependent permeability transitionInhibit the Ca2+ dependent permeability transitionIn vivoNANAMale Sprague-Dawley ratNANANA24707341989
1045Cyclolinopeptide A (CLA)VPPFFLIIL9LNoneNoneNoneCyclicNaturalisolated from linseed oilCyclophilin A, IL-1α, IL-2it binds to cyclophilin A and inhibits the action of Interleukin-1-alpha and Interleukin-2BothSRBC (Sheep red blood cells)dose combinations: 0.1 mg/ml of CLA and 0.25 mM of MTX exhibited suppressive, synergistic action12-week-old BALB/c female miceSecondary humoral immune responseNAMethotrexate (MTX) 218395482011
1046CLA analogue1LVPPFFLII9LNoneNoneEthylene bridge (-CH2-CH2-) between phenylalanine nitrogensCyclicSyntheticAnalog of cyclolinopeptide A (CLA)NANABothSRBC (Sheep red blood cells)NA12-week-old BALB/c female miceSecondary humoral immune responseNANA218395482011
1047CLA analogue2LVPPffLII9MixNoneNoneEthylene bridge (-CH2-CH2-) between phenylalanine nitrogensCyclicSyntheticAnalog of cyclolinopeptide A (CLA)NANABothSRBC (Sheep red blood cells)NA12-week-old BALB/c female miceSecondary humoral immune responseNANA218395482011
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
1064AntamanideVPPAFFPPFF10LNoneNoneNoneCyclicNaturalIsolated from the poisonous mushroom Amanita phalloidesPeptidyl-prolyl cis-trans isomerase CyP-DInhibit mitochondrial permeability transition poreBothHeLa CellsNAC57BL/6 miceCell Viability assay, Ca2+ retention capacity assayNANA212979832011
1065Cyclolinopeptide A (CLA)VPPFFLIIL9LNoneNoneNoneCyclicSyntheticNANAInhibition of the action of interleukin-1 and interleukin-2BothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1066AntamanideVPPAFFPPFF10LNoneNoneNoneCyclicNaturalIsolated from the mushroom Amanita phalloidesNANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1067Cycloamanide A (CyA A)VFFAGP6LNoneNoneNoneCyclicNaturalIsolated from the mushroom Amanita phalloidesNANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1068[D-Phe3]CyA AVFfAGP6MixNoneNoneNoneCyclicSyntheticNANANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1069Cycloamanide B (CyA B)FFFPIPS7LNoneNoneNoneCyclicNaturalIsolated from the mushroom Amanita phalloidesNANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1070[D-Ser]CyA BFFFPIPs7MixNoneNoneNoneCyclicSyntheticNANANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1071Cycloamanide CLPMLGFLV8LNoneNoneR and S sulfoxide on methionineCyclicNaturalIsolated from the mushroom Amanita phalloidesNANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1072Cycloamanide DLPMLGFLP8LNoneNoneR and S sulfoxide on methionineCyclicNaturalIsolated from the mushroom Amanita phalloidesNANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1073Retro-[D-Phe3]CyA AfFVPGA6MixNoneNoneNoneCyclicSyntheticNANANot investigatedBothSRBC (sheep red blood cells)NACBA/Iiw mice 8-10 weeksHumoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) testNANA84417061992
1089Cyclosporin A (CyA)cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFungiIL-1, IL-8, TNF-αInhibits the expression of cytokine genes; lower the activity of T cells and their immune responseIn vitroMurine KC line PAM 212,human squamous carcinoma line COLO-164.5micromolarNAThymocyte co-stimulator assayNANA81482711994
1090Cyclosporin A (CyA)cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFungiIL-1, lL-8, TNF-αInhibits the expression of cytokine genes; lower the activity of T cells and their immune responseIn vitroNormal human KCs2micromolarNAThymocyte co-stimulator assayNANA81482711994
1111Collutellin AVISIIPV7LNoneNoneNoneCyclicNaturalColletotrichum dematium (fungus)IL-2Reduces IL2 productionIn vitroC57/B6 mice spleen cells167.3+/-0.38 nMC57/B6 miceNANANA243331932014
1112AntamidesVPPAFFPPFF10LNoneNoneNoneCyclicNaturalAmanita phalloides spp. (fungus)NAInhibition of mitochondrial permeability transition poresBothfibroblasts NAC57BL/6 miceNANANA243331932014
1113Cyclosporin Acyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalTolypocladium inflatum (fungus)CalcineurinInhibition of calcineurin by complex with cyclophilinsBothMurine KC line PAM 212,human squamous carcinoma line COLO-16NASprague Dawley ratsNANANA243331932014
1114Didemnin A/Bnot available0LNoneNoneNoneCyclicNaturalTrididemnum solidum (tunicate)eEFA1 and PPT-1Blocks protein and RNA synthesis, binds to eEFA1 and PPT-1In vivoNANANANANANA243331932014
1115FK506 (tracrolimus) Ascomycin (pimecrolimus,SDZ ASM 981)not available0LNoneNoneNoneCyclicNaturalStreptomyces tsukubaensis (bacteria)CalcineurinInhibition of calcineurin by complex with FK binding proteinsBothNANANANANANA243331932014
1116Homophyminesnot available0LNoneNoneNoneCyclicNaturalHomophymia spp. (marine sponge)NAAntiproliferative, mechanism unknownIn vitroNANANANANANA243331932014
1117Geodiamolides Hnot available0LNoneNoneNoneCyclicNaturalGeodia corticostylifera (marine sponge)Actin filamentsDisorganization of actin filamentsIn vitroNANANANANANA243331932014
1118Hymenistatin Inot available0LNoneNoneNoneCyclicNaturalHymeniucidon spp. (marine sponge)NAModulation of the IL2 cell response (comparable with rapamycin)In vivoNANANANANANA243331932014
1119Jasplakinolidenot available0LNoneNoneNoneCyclicNaturalJaspis splendens (marine sponge)ActinActin stabilization, induces actin polymerizationIn vitroNANANANANANA243331932014
1120Sirolimus (rapamycin), everolimus (and derivatives)not available0LNoneNoneNoneCyclicNaturalStreptomyces hygroscopius (bacteria)mTORInhibition of mTORBothNANANANANANA243331932014
1122Curcacycline B (Orbitide)LGSPILLGI9LNoneNoneNoneCyclicNaturalJatropha curcas (plant)PPIasePPIase inhbitiorIn vitroNANANANANANA243331932014
1123Cycloleonurinin (Orbitide)GPTQYPPYYlTP13MixNoneNoneNoneCyclicNaturalLeonurus heterophyllus (plant)NANot knownIn vitroNANANANANANA243331932014
1124Cyclolinopeptide A/B (Orbitide)IMLIPPFFV9LNoneNoneNoneCyclicNaturalLinum usitatissimum (plant)CalcineurinCYPA binding and calcineurin inhibitionIn vivoNANANANANANA243331932014
1126Kalata B1 (Cyclotide)GLPVCGETCVGGTCNTPGCTCSWPVCTRN29LNoneNoneThree Disulfide linkage (CI-CIV, CII-CV and CIII-CVI)CyclicNaturalOldenlandia affinis (plant)IL-2Antiproliferative, IL2-dependent mechanismBothNANANANANANA243331932014
1134Thalassospiramide Anot available0LNoneNoneNoneCyclicNaturalα-proteobacterium (strain CNJ-328)IL-5Inhibition of IL-5In vitrolymphocytes10 micromolarNANANANA173738042007
1135Thalassospiramide Bnot available0LNoneNoneNoneCyclicNaturalα-proteobacterium (strain CNJ-328)IL-5Inhibition of IL-6In vitrolymphocytes5 micromolarNANANANA173738042007
1139Cyclosporin A (CsA)cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFungusNAInhibits virus-induced polykaryocyte formation and the production of infectious measles virusIn vitroVero cells (Persistently infected Vero cells (448-PI-Vero))5micromolarNANANANA115098812001
1145Cyclosporin A (CsA)cyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFungusNANot AvailableIn vivoNANAEight- to 12-week-old male Lewis.lW (RTI.u) and Lewis.lA (RTI.')ratsGraft transplation assayNANA106664822000
1173Cyclosporin Acyclo[Abu-Sar-N(Me)Leu-Val-N(Me)Leu-Ala-D-Ala-N(Me)Leu-N(Me)Leu-N(Me)Val-N(Me)Bmt(E)]11MixNoneNoneBmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylatedCyclicNaturalFungusNANot AvailableIn vivoNANACBA/Ca and (CBA/Ca X C57BL6)F1 micePlaque-forming cell (PFC) assayNANA61594101980
1202A1HS1II-Sta-PYVPL8LNoneNoneSta = (3S, 4S) -4- amino-3-hydroxy-6-methyl-heptanoic acid(C8H17NO3)CyclicSyntheticNALymphocytes, MacrophagesInfluence of phagocytic function of macrophages, and the retarding effect of the proliferation of LymphocytesBothSpleen LymphocyteNABALB / C miceDelayed-type hypersensitivity (DTH) test, Lymphocyte Proliferation test, MTTNACN 101289499 B2010
1203A3HS1IIPPYV-Sta-L8LNoneNoneSta = StatineCyclicSyntheticNALymphocytes, MacrophagesInfluence of phagocytic function of macrophages, and the retarding effect of the proliferation of LymphocytesBothSpleen LymphocyteNABALB / C miceDelayed-type hypersensitivity (DTH) test, Lymphocyte Proliferation test, MTTNACN 101289498 B2010
1204A4HS1II-Sta-Sta-YVPL8LNoneNoneSta = StatineCyclicSyntheticNALymphocytes, MacrophagesInfluence of phagocytic function of macrophages, and the retarding effect of the proliferation of LymphocytesBothSpleen LymphocyteNABALB / C miceDelayed-type hypersensitivity (DTH) test, Lymphocyte Proliferation test, MTTNACN 101289497 A2008