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Journal Articles - UP - MSI

Permanent URI for this collectionhttps://repository.unesco.gov.ph/handle/123456789/50

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2022 - 20232

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AGROVOC Keyword: search.filters.agrovoc.peptidesAuthor: search.filters.author.Concepcion, Gisela

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    Somatostatin venom analogs evolved by fish-hunting cone snails: From prey capture behavior to identifying drug leads
    Ramiro, Iris Bea L.; Bjørn-Yoshimoto, Walden E.; Imperial, Julita S.; Gajewiak, Joanna; Salcedo, Paula Flórez; Watkins, Maren; Taylor, Dylan; Resager, William; Ueberheide, Beatrix; Bräuner-Osborne, Hans; Whitby, Frank G.; Hill, Christopher P.; Martin, Laurent F.; Patwardhan, Amol; Concepcion, Gisela; Olivera, Baldomero M.; Safavi-Hemami, Helena (American Association for the Advancement of Science, 2022-03-25)
    Somatostatin (SS) is a peptide hormone with diverse physiological roles. By investigating a deep-water clade of fish-hunting cone snails, we show that predator-prey evolution has generated a diverse set of SS analogs, each optimized to elicit specific systemic physiological effects in prey. The increased metabolic stability, distinct SS receptor activation profiles, and chemical diversity of the venom analogs make them suitable leads for therapeutic application, including pain, cancer, and endocrine disorders. Our findings not only establish the existence of SS-like peptides in animal venoms but also serve as a model for the synergy gained from combining molecular phylogenetics and behavioral observations to optimize the discovery of natural products with biomedical potential.
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    On-resin synthesis of the somatostatin venom analog Consomatin Ro1
    de Boda, Ramoncito Luis; Acyatan, Zildjian; Concepcion, Gisela; Villaraza, Aaron Joseph (Philippine-American Academy of Science and Engineering, 2023-08-29)
    Consomatin Ro1 is a disulfide-containing peptide derived from the venom of the cone snail Conus rolani with a sequence that is similar to the vertebrate peptide hormone somatostatin. It has been shown to preferentially activate human somatostatin receptor subtypes 1 and 4, and to exhibit antinociceptive and antihyperalgesic properties making it an interesting peptide to study and develop as a chemical probe or an analgesic drug. Here, we describe the synthesis of Consomatin Ro1 using an onresin approach wherein the disulfide bond is formed while the peptide is still attached to the resin. This was achieved by selectively removing the methoxytrityl protecting group of Cys residues with a weak acidic mixture, and treating the resulting thiol-containing peptidyl resin with the mild oxidant Nchlorosuccinimide. The strategy yielded a considerably higher amount of the peptide when compared with the previously reported in-solution disulfide formation method.
    This work was funded by the Department of Science and Technology through Project 1. Anti-Pain and AntiNeurodegeneration Drug Candidates: Discovery and Development under the Discovery and Development of Health Products - Marine Component (Phase II) program. The authors would like to thank the Philippine Council for Health Research and Development for monitoring the research project.