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 |
1064 | Antamanide | VPPAFFPPFF | 10 | L | None | None | None | Cyclic | Natural | Isolated from the poisonous mushroom Amanita phalloides | Peptidyl-prolyl cis-trans isomerase CyP-D | Inhibit mitochondrial permeability transition pore | Both | HeLa Cells | NA | C57BL/6 mice | Cell Viability assay, Ca2+ retention capacity assay | NA | NA | 21297983 | 2011 |