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Structural Biological Studies of Thipeptide Biosynthesis and Engineering

Structural Biological Studies of Thipeptide Biosynthesis and Engineering
硫肽生物合成与工程的结构生物学研究
批准号：
10386793
负责人：
Satish K Nair
金额：
$30.19万
依托单位：
UNIVERSITY OF ILLINOIS AT URBANA-CHAMPAIGN
依托单位国家：
美国
项目类别：
财政年份：
2019
资助国家：
美国
项目状态：
已结题
起止时间：
2019-07-01 至 2024-04-30
来源：
https://reporter.nih.gov/project-details/10386793
关键词：
AcidsAmidesAnabolismAnti-Bacterial AgentsAntibioticsAzolesBindingBiochemicalBiologicalBiological AvailabilityC-terminalCharacteristicsClassificationClinical TrialsComplexCrystallographyDataEngineeringEnzymatic BiochemistryEnzymesGoalsHandHybridsIllinoisIn VitroKnowledgeMethodsMultienzyme ComplexesMultiprotein ComplexesNatural ProductsNatureNitrogenOxazolesPathway interactionsPeptide Leader SequencesPeptidesPharmaceutical PreparationsPlanet EarthProcessProductionPropertyReactionResearchRibosomesRouteSolubilityStructureSulfurThiazolesThioamidesVertebral columnanaloganti-cancerbioactive natural productsbioactive scaffoldcatalystcycloadditiondehydroalaninefallsglycosylationimprovedimproved functioningin vivomicrocinnoveloxazolidinepyridinereconstitutionsuccesssugarwater solubility

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中文摘要
翻译
噻唑基肽是一类具有广泛生物活性的天然产物， 包括抗癌、抗疟原虫和抗菌。虽然天然化合物 由于溶解性差，不适合药物，目前许多合成衍生物 在临床试验阶段了解将肽底物转化为 噻唑基肽将显著有助于产生具有更好的药物样活性的分子， 特性.我们试图进行生物化学和结构生物学研究， 这些酶，以帮助指导生产这些生物活性的改进版本， 化合物.
英文摘要
Thiazolyl peptides are natural products with a wide range of biological activities, including anticancer, antiplasmodial, and antibacterial. Although the natural compounds are not suitable drug because of poor solubility, many synthetic derivatives are currently in clinical trials. An understanding of the enzymes that convert peptide substrates into thiazolyl peptides will significantly aid in producing molecules with better drug-like properties. We seek to carry out biochemical, and structural biological studies on several of these enzymes to help guide the production of improved versions of these bioactive compounds.
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会议论文
Exploring Peptide Conjugates as Trojan Horse Systems for Drug Design and Discovery
Exploring Peptide Conjugates as Trojan Horse Systems for Drug Design and Discovery.
Exploring Peptide Conjugates as Trojan Horse Systems for Drug Design and Discovery
Structural Biology of Biosynthetic Enzymes
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