Table 1.
Summary of work published in engineered cyclotides with novel biological activities leading to therapeutic and bioimaging applications.
| Cyclotide | Biological activity | Loop Mlodified | Application | Ref. |
|---|---|---|---|---|
| Möbius subfamily | ||||
| Kalata B1 | VEGF-A antagonist 2 | 2, 3, 5 & 6 | Anti-angiogenic, potential anti-cancer activity | (41) |
| Kalata B1 | Dengue NS2B-NS3 Protease inhibitor | 2 & 5 | Anti-viral for Dengue virus infections | (108) |
| Kalata B1 | Bradikynin B1 receptor antagonist | 6 | Chronic and inflammatory pain | (45) |
| Kalata B1 | Melanocortin 4 receptor Agonist | 6 | Obesity | (44) |
| Kalata B1 | Neuropilin-1/2 antagonist | 5 & 6 | Inhibition of endothelial cell migration and angiogenesis | (109) |
| Kalata B1 | Immunomodulator | 5 & 6 | Protecting against multiple sclerosis | (110) |
| Kalata B1 | Immunomodulator | 4 | Protecting against multiple Sclerosis | (111) |
| Trypsin inhibitor subfamily | ||||
| MCoTI-I | CXCR4 antagonist | 6 | Anti-metastatic and anti-HIV PET-CT imaging | (24–26) |
| MCoTI-I | p53-Hdm2/HdmX Antagonist | 6 | Anti-tumor by activation of p53 pathway | (27) |
| MCoTI-II | FMDV 3C protease Inhibitor | 1 | Antiviral for foot-and-mouth disease | (43) |
| MCoTI-II | β-Tryptase inhibitor | 3, 5 & 6 | Inflammation disorders | (49) |
| MCoTI-II | β-Tryptase inhibitor Human elastase inhibitor | 1 | Inflammation disorders | (42) |
| MCoTI-II | CTLA-4 antagonist | 1,3 & 6 | Immunotherapy for cancer | (54) |
| MCoTI-II | Tryptase inhibitor | 1 | Anticancer | (81) |
| MCoTI-II | VEGF receptor agonist | 6 | Wound healing and cardiovascular damage | (87) |
| MCoTI-I | α-Synuclein-induced cytotoxicity inhibitor | 6 | Parkinson’s disease Validate phenotypic screening of genetically-encoded cyclotide libraries | (40) |
| MCoTI-II | BCR-Abl kinase Inhibitor | 1 & 6 | Chronic myeloid leukemia Attempt to graft both a cell penetrating peptide and kinase inhibitor | (112) |
| MCoTI-I | MAS1 receptor agonist | 6 | Lung cancer and myocardial infarction | (113) |
| MCoTI-II | SET antagonist | 6 | Potential anticancer | (50) |
| MCoTI-II | FXIIa and FXa inhibitors | 1 & 6 | Antithrombotic and cardiovascular disease | (114) |
| MCoTI-II | Thrombospondin-1 (TSP-1) agonist | 6 | Microvascular endothelial cell migration inhibition Anti-angiogenesis | (85) |
| MCoTI-II | Antiangiogenic | 5 & 6 | Anti-cancer | (103) |