| 1002 | Cyclosporin 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)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungus | Reduction 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-2 | In vitro | Human peripheral Lymphocytes and purified T cells | NA | None | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1003 | Native kalata B1 | GLPVCGETCVGGTCNTPGCTCSWPVCTRN | 29 | L | None | None | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Natural cyclotide | A 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 vitro | Human peripheral Lymphocytes | 2.9±1.3 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1004 | Native kalata B2 | GLPVCGETCVGGTCNTPGCTCSWPVCTRN | 29 | L | None | None | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Natural cyclotide | A 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 vitro | Purified T cells | 2.4±0.5 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1005 | kalata B1 mutants [T20K] | GLPVCGETCVGGTCNTPGCKCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | 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 vitro | Human peripheral Lymphocytes | 1.9±0.6 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1006 | kalata B1 mutants [T20K] | GLPVCGETCVGGTCNTPGCKCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | 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 vitro | Purified T cells | 2.7±0.6 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1007 | kalata B1 mutants [N29K] | GLPVCGETCVGGTCNTPGCTCSWPVCTRK | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | 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 vitro | Human peripheral Lymphocytes | 3.2±0.6 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1008 | kalata B1 mutants [N29K] | GLPVCGETCVGGTCNTPGCTCSWPVCTRK | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | 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 vitro | Purified T cells | 2.1±0.9 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1009 | kalata B1 mutants [G18K] | GLPVCGETCVGGTCNTPKCTCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | 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 vitro | Human peripheral Lymphocytes | 4.4±0.5 micromolar for Lymphocytes (PBMCs) | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1010 | kalata B1 mutants [G18K] | GLPVCGETCVGGTCNTPKCTCSWPVCTRN | 29 | L | Addition of Cysteine | Thioester linker | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic (head to tail | Synthetic | NA | 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 vitro | Purified T cells | 3.2±1.8 micromolar for purified T cells | NA | Cell Proliferation assay, Ca2+ release assay, Cytokines release assay | NA | NA | 23840803 | 2013 |
| 1053 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-1 | 0.013 nM for IL-2 when stimulation with PMA and ionomycin | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1054 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-2 | 0.016 nM for IL-4 when stimulation with PMA and ionomycin | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1055 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-3 | 0.5 nM for IL-2 production when stimulated with a-CD3 and VCAM-1 | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1056 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-4 | 0.13 nM for IL-4 production when stimulated with a-CD3 and VCAM-1 | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1057 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-5 | 4.9 nM for a-CD3/VCAM-1 induced proliferation | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1058 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-6 | 0.5 nM anti-CD3 mediated redirected cytolysis of CD8(+) T cells | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1059 | Margatoxin | TIINVKCTSPKQCLPPCKAQFGQSAGAKCMNGKCKCYPH | 39 | L | None | None | None | Linear | Synthetic | Recombinantnt was made by expressing the synthetic cDNA in Escherichia coli | Kv1.3 channel | Inhibit both Th1 and Th2 cytokine production | Both | Human peripheral blood mononuclear cells (PBMC), Purified T cells, Human monocytes, Human monocytic cell line, THP-7 | 0.5 nM anti-CD3 mediated redirected cytolysis of T cells | Mini swine model | Proliferation asaay, detection of intracellular cytokines, Antibody-dependent cellular cytotoxicity assay | NA | NA | 12747950 | 2003 |
| 1086 | Ac1-9 | ASQKRPSQR | 9 | L | Acetylation | None | None | Linear | Protein Derived | From myelin basic protein | IL-10 and IL-2 | peptide-induced regulatory cells suppress the response of naive T cells and leads to the generation of IL-10-secreting regulatory cells | Both | purified T cells | NA | Tg4 transgenic mouse | CD4 T cell Proliferation assays, Cytokine protein levels assays | NA | NA | 12538682 | 2003 |
| 1087 | MHC-binding analog (Ac1-9[4Y]) | ASQYRPSQR | 9 | L | Acetylation | None | None | Linear | Synthetic | Analog of Ac1-9 | IL-10 and IL-3 | peptide-induced regulatory cells suppress the response of naive T cells and leads to the generation of IL-10-secreting regulatory cells | Both | purified T cells | NA | Tg4 transgenic mouse | CD4 T cell Proliferation assays, Cytokine protein levels assays | NA | NA | 12538682 | 2003 |
| 1521 | RTL401 | GGGGSLVPRGSGGGG | 15 | L | None | None | None | Linear | Protein Derived | I-As/proteolipid protein | T-cells | cytokine switch in targeted T cells to produce anti-inflammatory cytokines,reduction of infiltrating mononuclear cells into CNS | In vivo | NA | NA | SJL mice | Immunoblotting, Cytokine determination by cytometric bead array, ELISA | NA | autoimmune encepha- lomyelitis | 16148160 | 2005 |
| 1524 | 119R | VAALEEANTELEVKI | 15 | L | None | None | None | Linear | Protein Derived | keratin 17 | Psoriatic T-cells and keratinocyte | Inhibition of T-cell proliferation , secretion of interferon gamma and interleukin 2 and up-regulation of interleukins 4 and 10 | In vitro | NA | NA | NA | Cytokine secretion assay, T-cell proliferation assay | NA | NA | 16713453 | 2006 |
| 1525 | 355L | ENRYCVQASQIQGLI | 15 | L | None | None | None | Linear | Protein Derived | keratin 18 | Psoriatic T-cells and keratinocyte | Inhibition of T-cell proliferation , secretion of interferon gamma and interleukin 2 and up-regulation of interleukins 4 and 11 | In vitro | NA | NA | NA | Cytokine secretion assay, T-cell proliferation assay | NA | NA | 16713453 | 2006 |
| 1537 | Analog peptide (A9) | not available | 26 | L | NA | NA | NA | Linear | Protein Derived | Type II collagen (CII) | IL-10, IL-4 | High expression of FcεRIγ(FcRγ) | Both | splenocytes or inguinal lymph node cells | NA | DBA/1 mice | Bio-plex mouse cytokine assay | NA | NA | 21590683 | 2011 |
| 1543 | MOG35-55 peptide | MEVGWYRSPFSRVVHLYRNGK | 21 | L | None | None | None | Linear | Protein Derived | Myelin oligodendrocyte glycoprotein | IL-10 | Not Available | Both | Spleen and lymph node cells | NA | C57BL/6 mice | Bio-Plex Cytokine Assay | NA | NA | 23033382 | 2012 |
| 1551 | altered peptide ligand (APL), | HSLGKQLGHPDKF | 13 | L | None | None | None | Linear | Synthetic | Subsitution of trytophan to glutamine in myelin proteolipid protein | Cross reacts with native peptide | Induces T- cells that produces Th2 (IL-4 and IL-10) and Th0 (IFN-γ and IL-10) | Both | T cell lines | NA | Female (4 to 6week-old) SJL mice | In vitro cytokine assays | NA | NA | 7584131 | 1995 |
| 1553 | 262Lys | VIVKLIPSTSSAV | 13 | L | None | None | None | Linear | Synthetic | Analog of Peptide p259-271 of the human acetylcholine receptor a-subunit | NA | Inhibited complete secretion of IL-2 and IL-4 and inhibit effeicintly IL-10 and TNF-α | Both | T cell line | NA | Female mice of the inbred strain BALBrc | Cytokine detection | NA | NA | 9627000 | 1998 |
| 1554 | 262Ser | VIVSLIPSTSSAV | 13 | L | None | None | None | Linear | Synthetic | Analog of Peptide p259-271 of the human acetylcholine receptor a-subunit | NA | Inhibited complete secretion of IL-2 and IL-4 and inhibit effeicintly IL-10 and TNF-α | Both | T cell line | NA | Female mice of the inbred strain BALBrc | Cytokine detection | NA | NA | 9627000 | 1998 |
