8 documents found, page 1 of 1
Cyclotides from Brazilian Palicourea sessilis and Their Effects on Human Lympho...
Pinto, Meri Emili F. [UNESP]; Chan, Lai Yue; Koehbach, Johannes; Devi, Seema; Gründemann, Carsten; Gruber, Christian W.; Gomes, MarioMade available in DSpace on 2021-06-25T11:10:52Z (GMT). No. of bitstreams: 0 Previous issue date: 2021-01-22; Cyclotides are plant-derived peptides found within five families of flowering plants (Violaceae, Rubiaceae, Fabaceae, Solanaceae, and Poaceae) that have a cyclic backbone and six conserved cysteine residues linked by disulfide bonds. Their presence within the Violaceae species seems ubiquitous, yet not ...
Cell membrane composition drives selectivity and toxicity of designed cyclic he...
Philippe, Grégoire J.-B.; Gaspar, Diana; Sheng, Caibin; Huang, Yen-Hua; Benfield, Aurélie H.; Condon, Nicholas D.; Weidmann, Joachim; Lawrence, NicoleThe tumor suppressor protein p53 is inactive in a large number of cancers, including some forms of sarcoma, breast cancer, and leukemia, due to overexpression of its intrinsic inhibitors MDM2 and MDMX. Reactivation of p53 tumor suppressor activity, via disruption of interactions between MDM2/X and p53 in the cytosol, is a promising strategy to treat cancer. Peptides able to bind MDM2 and/or MDMX were shown to p...
Characterization of Tachyplesin peptides and their cyclized analogues to improv...
Vernen, Felicitas; Harvey, Peta J.; Dias, Susana; Veiga, Ana Salomé; Huang, Yen-Hua; Craik, David J.; Lawrence, Nicole; Troeira Henriques, SóniaTachyplesin I, II and III are host defense peptides from horseshoe crab species with antimicrobial and anticancer activities. They have an amphipathic β-hairpin structure, are highly positively-charged and differ by only one or two amino acid residues. In this study, we compared the structure and activity of the three tachyplesin peptides alongside their backbone cyclized analogues. We assessed the peptide stru...
Mechanisms of bacterial membrane permeabilization by crotalicidin Ctn and its f...
Peinado, Clara Pérez; Dias, Susana; Domingues, Marco André Manso; Benfield, Aurélie H.; Freire, João Miguel; Rádis-Baptista, Gandhi; Gaspar, DianaCrotalicidin (Ctn), a cathelicidin-related peptide from the venom of a South American rattlesnake, possesses potent antimicrobial, antitumor, and antifungal properties. Previously, we have shown that its C-terminal fragment, Ctn(15-34), retains the antimicrobial and antitumor activities but is less toxic to healthy cells and has improved serum stability. Here, we investigated the mechanisms of action of Ctn and...
Design and characterization of novel antimicrobial peptides, R-BP100 and RW-BP1...
Torcato, Inês M.; Huang, Yen-Hua; Franquelim, Henri G.; Gaspar, Diana; Craik, David J.; Castanho, Miguel A. R. B.; Henriques, Sónia TroeiraBP100 is a short cationic antimicrobial peptide with a mechanism of action dependent on peptide–lipid interactions and microbial surface charge neutralization. Although active against Gram-negative bacteria, BP100 is inactive against Gram-positive bacteria. In this study we report two newly designed BP100 analogues, RW-BP100 and R-BP100 that have the Tyr residue replaced with a Trp and/or the Lys residues repla...
The antimicrobial activity of sub3 is dependent on membrane binding and cell-pe...
Torcato, Inês M.; Huang, Yen-Hua; Franquelim, Henri G.; Gaspar, Diana D.; Craik, David J.; Castanho, Miguel A. R. B.; Henriques, Sónia TroeiraBecause of their high activity against microorganisms and low cytotoxicity, cationic antimicrobial peptides (AMPs) have been explored as the next generation of antibiotics. Although they have common structural features, the modes of action of AMPs are extensively debated, and a single mechanism does not explain the activity of all AMPs reported so far. Here we investigated the mechanism of action of Sub3, an AM...
Structural and functional analysis of human liver-expressed antimicrobial pepti...
Henriques, Sónia Troeira; Tan, Chia Chia; Craik, David J.; Clark, Richard J.Human liver-expressed antimicrobial peptide 2 (LEAP-2) is a cationic antimicrobial peptide (CAMP) believed to have a protective role against bacterial infection. Little is known about the structure–activity relationships of LEAP-2 or its mechanism of ction. In this study we describe the structure of LEAP-2, analyze its interaction with model membranes, and relate them to the antimicrobial activity of the peptid...
Cyclotides as templates in drug design
Henriques, Sónia Troeira; Craik, David J.Cyclotides are remarkably stable proteins from plants that have a range of pharmaceutical and agricultural applications based on both their various bioactivities and their potential for use as stable protein-engineering templates. This article discusses literature on pharmaceutically relevant activities of cyclotides, including anti-HIV, antimicrobial and cytotoxic activities, and evaluates their potential ther...