| 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 |
| 1036 | Cyclosporin A | 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 | From fungus Trichoderma polysporum | Inhibit IL-2 production by activated CD4+ T-cells | Inhibiting the calcineurin pathway | Both | Peripheral blood mononuclear cells (PBMCs) | 61.8 nM for CD4+ T cell activation of IL-2 production | C57/B6 mice | MIC assay, Immunosuppression and toxicity test | NA | NA | 18599825 | 2008 |
| 1037 | Colutellin A | VISIIPV | 7 | L | None | None | None | Cyclic | Natural | Endophytic fungus Colletotrichum dematium | Inhibit IL-2 production by activated CD4+ T-cells | Inhibiting the calcineurin pathway | Both | Peripheral blood mononuclear cells (PBMCs) | 167.3±0.38 nM for CD4+ T cell activation of IL-2 production | C57/B6 mice | MIC assay, Immunosuppression and toxicity test | MIC of 3.6 mg/ml (48 h) against Botrytis cinerea and Sclerotinia sclerotiorum. | NA | 18599825 | 2008 |
| 1041 | Trauma induced immunosuppressive glycopeptide (TP) | not available | 0 | NA | NA | NA | NA | NA | Natural | From arterial blood of burn or trauma patient | neutrophils, T and B Lymphocytes | Through stimulation of PGE2 biosynthesis and through a non-cyclooxygenasepathway. | In vitro | Mitomycin-treated stimulator Lymphocytes | NA | NA | Mixed Lymphocyte culture assay and TP-induced PGE2 biosynthesis assay | NA | NA | 2965105 | 1988 |
| 1044 | Cyclosporin A | 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 | From fungus Trichoderma polysporum | Ca2+-dependent permeability transition | Inhibit the Ca2+ dependent permeability transition | In vivo | NA | NA | Male Sprague-Dawley rat | NA | NA | NA | 2470734 | 1989 |
| 1045 | Cyclolinopeptide A (CLA) | VPPFFLIIL | 9 | L | None | None | None | Cyclic | Natural | isolated from linseed oil | Cyclophilin A, IL-1α, IL-2 | it binds to cyclophilin A and inhibits the action of Interleukin-1-alpha and Interleukin-2 | Both | SRBC (Sheep red blood cells) | dose combinations: 0.1 mg/ml of CLA and 0.25 mM of MTX exhibited suppressive, synergistic action | 12-week-old BALB/c female mice | Secondary humoral immune response | NA | Methotrexate (MTX) | 21839548 | 2011 |
| 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 |
| 1088 | ISU-peptide | LQARILAVERYLKDQQL | 17 | L | None | None | None | Linear | Protein Derived | HIV-1 isolate HXB2 | IL-2 | HIV env 583-599 conjugated to a carrier protein to inhibit the cytopathic effect of HIV-1. This inhibition of vims replication may be due to blocking of a secondary receptor, to inhibition of target cell proliferation preventing virus replication or to both effects | Both | Murine CTL-6, human T-cell lines MT4, Molt4/clone 8 | NA | Balb/c mice | Lymphocyte Proliferation assays, cytopathogenicity assay | NA | NA | 7986401 | 1994 |
| 1089 | Cyclosporin 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)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungi | IL-1, IL-8, TNF-α | Inhibits the expression of cytokine genes; lower the activity of T cells and their immune response | In vitro | Murine KC line PAM 212,human squamous carcinoma line COLO-16 | 4.5micromolar | NA | Thymocyte co-stimulator assay | NA | NA | 8148271 | 1994 |
| 1090 | Cyclosporin 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)] | 11 | Mix | None | None | Bmt = butenyl-methyl-threonine, Abu = L-alpha-aminobutyric acid, Sar = sarcosine, N(Me) = Amino acid is N-methylated | Cyclic | Natural | Fungi | IL-1, lL-8, TNF-α | Inhibits the expression of cytokine genes; lower the activity of T cells and their immune response | In vitro | Normal human KCs | 2micromolar | NA | Thymocyte co-stimulator assay | NA | NA | 8148271 | 1994 |
| 1091 | Transforming growth factor beta 1 (TGFβ1) | not available | 0 | L | None | None | None | Linear | Protein Derived | Human melanoma cell line | IL-7 | The immunosuppressive peptide TGFβ1 was inhibited in a human melanoma cell line transduced with IL-7 | Both | M- 14 and M-24 | NA | Congenitally athymic (nu/nu) BALB/c mice | TGFβ1 bioassay | NA | NA | 8260705 | 1993 |
| 1111 | Collutellin A | VISIIPV | 7 | L | None | None | None | Cyclic | Natural | Colletotrichum dematium (fungus) | IL-2 | Reduces IL2 production | In vitro | C57/B6 mice spleen cells | 167.3+/-0.38 nM | C57/B6 mice | NA | NA | NA | 24333193 | 2014 |
| 1117 | Geodiamolides H | not available | 0 | L | None | None | None | Cyclic | Natural | Geodia corticostylifera (marine sponge) | Actin filaments | Disorganization of actin filaments | In vitro | NA | NA | NA | NA | NA | NA | 24333193 | 2014 |
| 1126 | Kalata B1 (Cyclotide) | GLPVCGETCVGGTCNTPGCTCSWPVCTRN | 29 | L | None | None | Three Disulfide linkage (CI-CIV, CII-CV and CIII-CVI) | Cyclic | Natural | Oldenlandia affinis (plant) | IL-2 | Antiproliferative, IL2-dependent mechanism | Both | NA | NA | NA | NA | NA | NA | 24333193 | 2014 |
| 1131 | core peptide (CP) | GLRILLLKV | 9 | L | None | None | None | Linear | Protein Derived | T-cell antigen receptor alpha-chain transmembrane region | IL-2 | Inhibits IL-2 production | In vitro | Alanine scan, LK antigen-presenting cells | NA | NA | Antigen presentation assay, CTLL assay | NA | NA | 23066996 | 2013 |
| 1134 | Thalassospiramide A | not available | 0 | L | None | None | None | Cyclic | Natural | α-proteobacterium (strain CNJ-328) | IL-5 | Inhibition of IL-5 | In vitro | lymphocytes | 10 micromolar | NA | NA | NA | NA | 17373804 | 2007 |
| 1135 | Thalassospiramide B | not available | 0 | L | None | None | None | Cyclic | Natural | α-proteobacterium (strain CNJ-328) | IL-5 | Inhibition of IL-6 | In vitro | lymphocytes | 5 micromolar | NA | NA | NA | NA | 17373804 | 2007 |
| 1141 | Glycodelin-A | MLCLLLTLGVALVCGVPAMDIPQTKQDLELPKLAGTWHSMAMATNNISLMATLKAPLRVHITSLLPTPEDNLEIVLHRWENNSCVEKKVLGEKTENPKKFKINYTVANEATLLDTDYDNFLFLCLQDTTTPIQSMMCQYLARVLVEDDEIMQGFIRAFRPLPRHLWYLLDLKQMEEPCRF | 180 | L | None | None | None | Linear | Protein Derived | NA | IL-2 | Glycodelin-A interrupts the production of interleukin-2 (IL-2) by lymphocytes and inhibits the IL-2 activation of natural killer cells | In vitro | Cervical tissue | NA | NA | NA | NA | NA | 11063647 | 2000 |
| 1180 | Immunosuppressive epitope of retroviral plSE | not available | 17 | L | None | None | None | Linear | Protein Derived | Retroviral protein pl5E | IL-2, TNF-α, protein kinase-C | Inhibits human mitogen and alloantigen-stimulated lymphocyte proliferation, natural killer cell activity, interleukin 1-mediated monocyte tumor killing, interleukin 2 production, immunoglobulin synthesis, TNF-α mRNA expression and protein kinase C activity | Both | U937, P2, JLS-V5 | NA | BALB/c mice (Female, 12- week-old) | NA | NA | NA | 7511054 | 1994 |
| 1201 | 11R-VEET | RRRRRRRRRRRMAGPHPVIVITGPHEE | 27 | L | None | None | None | Linear | Synthetic | NA | T cells, Transcription of IL-2 gene | Suppressive agent of NFAT activation | Both | Jurkat | NA | BALB/c mouse, H-2d mouse, C3H/HeN mouse H-2k | NA | NA | NA | US 7659249 B2 | 2010 |
| 1533 | MOG peptide | MEVGWYRSPFSRVVHLYRNGK | 21 | L | None | None | None | Linear | Protein Derived | Myelin oligodendrocyte glycoprotein | IL-10, TGF-β | Not Available | In vivo | NLDC-145 for DEC205 and GL117 for b-galactosidase | NA | C57/Bl6 mice, 2D2 mice or BALB/c mice | Proliferation assay | NA | NA | 23945139 | 2013 |
| 1534 | Preproinsulin-1 L7-24 peptide | FLPLLALLALWEPKPTQA | 18 | L | None | None | None | Linear | Protein Derived | Preproinsulin | IL-4, IL-10, TGF-β | Induces regulatory T cells | In vivo | NA | NA | NOD/Shi/Kbe mice | Quantikine immunoassay kit | NA | NA | 20359955 | 2010 |
| 1535 | MOG35-55 | MEVGWYRSPFSRVVHLYRNGK | 21 | L | None | None | None | Linear | Protein Derived | Myelin oligodendrocyte glycoprotein | IL-10, TGF-β1, FoxP3 | Not Available | Both | splenocytes | NA | C57BL/6 mice | Proliferation assay | NA | NA | 23077616 | 2012 |
| 1536 | MSP1 peptide | ISVLKSRLLKRKKYI | 15 | L | None | None | None | Linear | Protein Derived | merozoite surface protein 1 (MSP1) | IL-10 | Not Available | Both | CTLL-2 cells, B5 CD4 T cell hybridoma | NA | BALB/c mice | NA | NA | NA | 23006847 | 2012 |
| 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 |
| 1538 | ApoB peptide | CIEIGLEGKGFEPTLEALFGK | 21 | L | None | None | None | Linear | Protein Derived | Apolipoprotein B100 (ApoB) | IL-10, TGF-β | Induced T-cell proliferation and expansion of regulatory T cells | Both | Splenocytes, Dendritic Cells | NA | C57BL6/J | Cytometric bead assay | NA | NA | 23400302 | 2013 |
| 1539 | HSP60 peptide | CAELKKQSKPVT | 12 | L | None | None | None | Linear | Protein Derived | Heat shock protein 60 (HSP60) | IL-10, TGF-β | Induced T-cell proliferation and expansion of regulatory T cells | Both | Splenocytes, Dendritic Cells | NA | C57BL6/J | Cytometric bead assay | NA | NA | 23400302 | 2013 |
| 1541 | MOG35-55 peptide | MEVGWYRSPFSRVVHLYRNGK | 21 | L | None | None | None | Linear | Protein Derived | Myelin oligodendrocyte glycoprotein | IL-10 | Not Available | Both | Spleen cells | NA | C57BL/6 and IL-10-/-(B6.129P2-Il10tmlCgn/J) mice | Proliferation assay | NA | NA | 20624940 | 2010 |
| 1542 | Cry j 1 peptide (61-75) | GATRDRPLWIIFSGN | 15 | L | None | None | None | Linear | Protein Derived | Cry j 1 protein | IL-10 | Production of CD4+CD25+ Treg cells | In vitro | Heparinized venous blood | NA | NA | CFSE-based proliferation assay, ELISPOT assay | NA | NA | 21597299 | 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 |
