Publications by authors named "Laura Droctove"
Article Synopsis
- Venomous animals produce Kunitz-type peptides, with mambaquaretin-1 (MQ1) being a selective antagonist for the V2 receptor, prompting researchers to explore more mamba venoms to expand the V2R-Kunitz peptide family.
- Through bio-guided screening, eight new MQs were discovered, all acting as antagonists to the V2R, revealing significant interactions within specific loops of the MQ1 peptide structure.
- The insights gained suggest that the extensive interaction sites of MQ1 contribute to its selectivity, with the variant MQ1-K39A showing promise for enhanced affinity targeting human V2R, paving the way for potential medicinal advancements.
MQ1, a snake toxin which targets with high nanomolar affinity and absolute selectivity for the type 2 vasopressin receptor (V2R), is a drug candidate for renal diseases and a molecular probe for imaging cells or organs expressing V2R. MQ1's pharmacological properties were characterized and applied to a rat model of hyponatremia. Its PK/PD parameters were determined as well as its therapeutic index.
View Article and Find Full Text PDFPolycystic kidney diseases (PKDs) are genetic disorders that can cause renal failure and death in children and adults. Lowering cAMP in cystic tissues through the inhibition of the type-2 vasopressin receptor (V2R) constitutes a validated strategy to reduce disease progression. We identified a peptide from green mamba venom that exhibits nanomolar affinity for the V2R without any activity on 155 other G-protein-coupled receptors or on 15 ionic channels.
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