| 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 |
| 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 |
| 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 |
| 1047 | CLA analogue2 | LVPPffLII | 9 | Mix | None | None | Ethylene bridge (-CH2-CH2-) between phenylalanine nitrogens | Cyclic | Synthetic | Analog of cyclolinopeptide A (CLA) | NA | NA | Both | SRBC (Sheep red blood cells) | NA | 12-week-old BALB/c female mice | Secondary humoral immune response | NA | NA | 21839548 | 2011 |
| 1049 | CLA analogue4 | LVPPffLII | 9 | Mix | None | None | Ethylene bridge (-CH2-CH2-) between phenylalanine nitrogens | Linear | Synthetic | Analog of cyclolinopeptide A (CLA) | NA | NA | Both | SRBC (Sheep red blood cells) | NA | 12-week-old BALB/c female mice | Secondary humoral immune response | NA | NA | 21839548 | 2011 |
| 1068 | [D-Phe3]CyA A | VFfAGP | 6 | Mix | None | None | None | Cyclic | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1070 | [D-Ser]CyA B | FFFPIPs | 7 | Mix | None | None | None | Cyclic | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1073 | Retro-[D-Phe3]CyA A | fFVPGA | 6 | Mix | None | None | None | Cyclic | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 1074 | Retro-[D-Phe3]CyA A | fFVPGA | 6 | Mix | None | None | None | Linear | Synthetic | NA | NA | Not investigated | Both | SRBC (sheep red blood cells) | NA | CBA/Iiw mice 8-10 weeks | Humoral immune response test,PFC (plaque froming cell) test, DTH (delayed type hypersensitivity) test | NA | NA | 8441706 | 1992 |
| 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 |
| 1113 | 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 | Tolypocladium inflatum (fungus) | Calcineurin | Inhibition of calcineurin by complex with cyclophilins | Both | Murine KC line PAM 212,human squamous carcinoma line COLO-16 | NA | Sprague Dawley rats | NA | NA | NA | 24333193 | 2014 |
| 1123 | Cycloleonurinin (Orbitide) | GPTQYPPYYlTP | 13 | Mix | None | None | None | Cyclic | Natural | Leonurus heterophyllus (plant) | NA | Not known | In vitro | NA | NA | NA | NA | NA | NA | 24333193 | 2014 |
| 1139 | 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 | NA | Inhibits virus-induced polykaryocyte formation and the production of infectious measles virus | In vitro | Vero cells (Persistently infected Vero cells (448-PI-Vero)) | 5micromolar | NA | NA | NA | NA | 11509881 | 2001 |
| 1145 | 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 | NA | Not Available | In vivo | NA | NA | Eight- to 12-week-old male Lewis.lW (RTI.u) and Lewis.lA (RTI.')rats | Graft transplation assay | NA | NA | 10666482 | 2000 |
| 1159 | RDP1258 | RnlnlnLRnlnLnLGY | 16 | Mix | None | None | None | Linear | Natural | HLA/MHC molecule | NA | Not Available | Both | In silico screening (MD simulations) | 1.2±0.2 micromolar | CBA and C57BI/6 mice | Graft transplation assay | NA | NA | 9702773 | 1998 |
| 1173 | 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 | Fungus | NA | Not Available | In vivo | NA | NA | CBA/Ca and (CBA/Ca X C57BL6)F1 mice | Plaque-forming cell (PFC) assay | NA | NA | 6159410 | 1980 |
| 1211 | NA | HAwY | 4 | Mix | None | None | A-D-Glu or D-iGlu, Y-OH or a substituted amide(C1-C3) | Linear | Natural | Total tissue extracts | Bone marrow cells, Hematopoietic progenitor cells | Reduces amount of ekzokolony cells, reduce KOE-C pool sizes | Both | Hematopoietic progenitor Cells from mice | NA | Mice | NA | NA | NA | RU2123859 (C1) | 1998 |
| 1271 | Copolymer 1(Cop 1) | EKAY | 4 | Mix | None | None | None | Linear | Synthetic | NA (Random copolymer) | T-cells | Inhibits T cell proliferation in response to graft cells, preventing the secretion of cytokines like interleukin 2 (IL-2) and interferon γ (IFN-γ) | In vivo | NA | NA | BALB/c mice, Lewis rats | Skin Grafts Transplantation, Thyroid graft Transplantation | NA | Copolymer 1-related heteropolymers in combination with other immunosuppressive drugs induce a synergistic effect, This is used as copolymer or related hateropolymer | US 20060276390 A1 | 2006 |
| 1336 | None | QNRRGLDLLFwEQGGLCKALQEQQCRF | 27 | Mix | None | None | Coupled with carrier protein human serum albumin, bovine serum albumin | Linear | Protein Derived | Retrovial envelope protein | Human Monocytes | Inhibit CTLL-2 proliferation | Both | Human mononuclear cells, Murine CTLL-2 cells, Balb/3T3 cells, NIH/3T27 | NA | BALB/c and NIH/Swiss mice, Rabbits | Hummoral Immune Response assay, Monocytes O2 release assay | NA | BSA | US 4822606 | 1989 |
| 1362 | CDP2 | GE(HP)GA(HP)GPAGP(HP)GE(HP)GA(HP)GpAGp(HP)G | 25 | Mix | None | None | HP = Hydroxyproline | Linear | Protein Derived | Collagen derived | Bystander antigens | By releasing transforming growth factor β (TGF-β) | In vivo | None | NA | Rats | NA | NA | NA | US 5720955 | 1998 |
| 1468 | SEQ ID10 | rlllrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1469 | SEQ ID11 | rvllrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1470 | SEQ ID12 | rillrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1471 | SEQ ID13 | rlvrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1472 | SEQ ID14 | rlilrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1473 | SEQ ID15 | rllvrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1474 | SEQ ID16 | rllirlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1475 | SEQ ID17 | rlllrvllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1476 | SEQ ID18 | rlllrillGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1477 | SEQ ID19 | rlllrlvlGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1478 | SEQ ID20 | rlllrlilGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1479 | SEQ ID21 | rlllrllvGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1480 | SEQ ID22 | rlllrlliGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1481 | SEQ ID23 | rwllrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1482 | SEQ ID24 | rlwlrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1483 | SEQ ID25 | rllwrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1484 | SEQ ID26 | rlllrwllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1485 | SEQ ID27 | rlllrlwlGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1486 | SEQ ID28 | rlllrllwGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1487 | SEQ ID29 | ryllrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1488 | SEQ ID30 | rlylrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1489 | SEQ ID31 | rllyrlllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1490 | SEQ ID32 | rlllryllGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1491 | SEQ ID33 | rlllrlylGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1492 | SEQ ID34 | rlllrllyGy | 10 | Mix | None | None | None | Linear | Protein Derived | (HLA-B) α1-domain | Gut Associated Lymphoid Tissue (GALT) | Increased CD4+ and CD8+ T-cells | In vivo | None | NA | Rhesus macaques | NA | NA | NA | US 7094413 B2 | 2006 |
| 1495 | SEQ ID15 | rlllrlllGy | 10 | Mix | Acetylation | Amidation | None | Linear | Synthetic | NA | NA | Inhibited T-cell proliferation, various inflammatory cytokines production. | In vivo | None | 2.5-10micromolar against binding to peptides to HSC70 | C57BL6/J, Balb/c and CBA/J mice | Enzyme-linked immunosorbent assay (ELISA) | NA | LPS | US 7267822 B2 | 2007 |
| 1496 | SEQ ID16 | rvllrlllGy | 10 | Mix | Acetylation | Amidation | None | Linear | Synthetic | NA | NA | Inhibited T-cell proliferation, various inflammatory cytokines production. | In vivo | None | 2.5-10micromolar against binding to peptides to HSC71 | C57BL6/J, Balb/c and CBA/J mice | Enzyme-linked immunosorbent assay (ELISA) | NA | LPS | US 7267822 B2 | 2007 |
| 1497 | SEQ ID17 | rillrlllGy | 10 | Mix | Acetylation | Amidation | None | Linear | Synthetic | NA | NA | Inhibited T-cell proliferation, various inflammatory cytokines production. | In vivo | None | 2.5-10micromolar against binding to peptides to HSC72 | C57BL6/J, Balb/c and CBA/J mice | Enzyme-linked immunosorbent assay (ELISA) | NA | LPS | US 7267822 B2 | 2007 |
| 1498 | SEQ ID18 | rlvlrlllGy | 10 | Mix | Acetylation | Amidation | None | Linear | Synthetic | NA | NA | Inhibited T-cell proliferation, various inflammatory cytokines production. | In vivo | None | 2.5-10micromolar against binding to peptides to HSC73 | C57BL6/J, Balb/c and CBA/J mice | Enzyme-linked immunosorbent assay (ELISA) | NA | LPS | US 7267822 B2 | 2007 |
