Search results for "Metzincin"

showing 2 items of 2 documents

Functional and structural insights into astacin metallopeptidases

2012

The astacins are a family of multi-domain metallopeptidases with manifold functions in metabolism. They are either secreted or membrane-anchored and are regulated by being synthesized as inactive zymogens and also by colocalizing protein inhibitors. The distinct family members consist of N-terminal signal peptides and pro-segments, zincdependent catalytic domains, further downstream extracellular domains, transmembrane anchors, and cytosolic domains. The catalytic domains of four astacins and the zymogen of one of these have been structurally characterized and shown to comprise compact ~200-residue zinc-dependent moieties divided into an N-terminal and a C-terminal sub-domain by an active-s…

MetzincinSignal peptideStereochemistryMolecular Sequence DataClinical BiochemistryTolloidMatrix metalloproteinaseBiologyBiochemistryEvolution Molecular03 medical and health sciencesEnzyme activatorBone morphogenetic proteinsZymogenAnimalsHumansProtease InhibitorsAmino Acid SequenceTyrosineMolecular BiologyPeptide sequence030304 developmental biologyEnzyme Precursors0303 health sciences030302 biochemistry & molecular biologyMetalloendopeptidasesMeprinTransmembrane protein3. Good healthEnzyme ActivationBiochemistryAstacinCatalytic domainsbchm
researchProduct

A Primary Evaluation of Potential Small-Molecule Inhibitors of the Astacin Metalloproteinase Ovastacin, a Novel Drug Target in Female Infertility Tre…

2020

Abstract Despite huge progress in hormonal therapy and improved in vitro fertilization methods, the success rates in infertility treatment are still limited. A recently discovered mechanism revealed the interplay between the plasma protein fetuin‐B and the cortical granule‐based proteinase ovastacin to be a novel key mechanism in the regulation of fertilization. Upon sperm–egg fusion, cleavage of a distinct zona pellucida component by ovastacin destroys the sperm receptor, enhances zona robustness, and eventually provides a definitive block against polyspermy. An untimely onset of this zona hardening prior to fertilization would consequently result in infertility. Physiologically, this proc…

Models Molecularmedicine.medical_treatmentHydroxamic Acids01 natural sciencesBiochemistryMiceHuman fertilizationIn vitro fertilizationDrug DiscoveryGeneral Pharmacology Toxicology and PharmaceuticsAminesZona pellucidametzincinseducation.field_of_studyMolecular StructureCommunicationFemale infertilitySperm receptorPolyspermyCell biologymedicine.anatomical_structureastacinsHydroxamateMolecular MedicineFemalemetalloproteinaseinfertilityInfertility FemaleInfertilityendocrine systemCortical granuleBiologySmall Molecule LibrariesStructure-Activity RelationshipmedicineAnimalseducationPharmacologyIn vitro fertilisationDose-Response Relationship Drugurogenital system010405 organic chemistryOrganic Chemistryin vitro fertilizationmedicine.diseaseovastacinCommunications0104 chemical sciences010404 medicinal & biomolecular chemistryBiocatalysisMetalloproteasesChemMedChem
researchProduct