| 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 |
| 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 |
| 1130 | CKS-17 | LQNRRGLDLLFLKEGGLC | 18 | L | None | None | None | Linear | Protein Derived | murine leukemia virus (MLV) | TNF-α | Significantly reduces the mRNA levels of IL-17C, TNF-α, IL-6 and CXCL2 | Both | Acute allergic contact dermatitis model and TPA toxic eczema model | NA | C57BL/6 mice and BALB/CJ mice | NA | NA | NA | 24245569 | 2013 |
| 1142 | RDP1258 | RNleNleNleRNleNleNleGY | 22 | L | None | Amidation | None | Linear | Protein Derived | NA | TNF-α | Enhanced expression of splenic heme oxygenase 1 (HO-1). Decreased expression of tumor necrosis factor a (TNF-α) mRNA; and an increased level of inducible nitric oxide synthase (iNOS) mRNA. | In vivo | NA | 20 micromolar | Eight- to 12-week-old male Lewis.lW (RTI.u) and Lewis.lA (RTI.')rats | Graft transplation assay | NA | NA | 10666482 | 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 |
| 1540 | Peptide A | CTLDLNTPVDKTSN | 14 | L | None | None | None | Linear | Protein Derived | Complement receptor 5a | TNF-α | Slightly stimulates T cells | Both | Splenocytes, Dendritic Cells | NA | C57BL6/J | Cytometric bead assay | NA | NA | 23400302 | 2013 |
