Design and chemical syntheses of potent matriptase-2 inhibitors based on trypsin inhibitor SFTI-1 isolated from sunflower seeds.

scientific article published on 27 May 2017

Design and chemical syntheses of potent matriptase-2 inhibitors based on trypsin inhibitor SFTI-1 isolated from sunflower seeds. is …
instance of (P31):
scholarly articleQ13442814

External links are
P356DOI10.1002/BIP.23031
P698PubMed publication ID28555756

P50authorDawid DebowskiQ56550116
Krzysztof RolkaQ58147469
Anna ŁęgowskaQ60633041
Agata Gitlin-DomagalskaQ88178581
P2093author name stringMichael Gütschow
Marit Stirnberg
Joanna Okońska
P2860cites workSunflower trypsin inhibitor 1 as a molecular scaffold for drug discoveryQ37971976
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Spliced analogues of trypsin inhibitor SFTI-1 and their application for tracing proteolysis and delivery of cargos inside the cellsQ38746354
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Sunflower trypsin inhibitor 1 derivatives as molecular scaffolds for the development of novel peptidic radiopharmaceuticalsQ39770968
Genetic upregulation of matriptase-2 reduces the aggressiveness of prostate cancer cells in vitro and in vivo and affects FAK and paxillin localisationQ39986548
Matriptase activates stromelysin (MMP-3) and promotes tumor growth and angiogenesisQ40227949
High-affinity cyclic peptide matriptase inhibitorsQ40601659
Implication of the disulfide bridge in trypsin inhibitor SFTI-1 in its interaction with serine proteinases.Q42841595
Two-step selective formation of three disulfide bridges in the synthesis of the C-terminal epidermal growth factor-like domain in human blood coagulation factor IXQ42844329
Loss of the matriptase inhibitor HAI‐2 during prostate cancer progressionQ42945644
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.Q43732256
Matriptase/MT-SP1 is required for postnatal survival, epidermal barrier function, hair follicle development, and thymic homeostasisQ44007860
Between two worlds: a comparative study on in vitro and in silico inhibition of trypsin and matriptase by redox-stable SFTI-1 variants at near physiological pH.Q45741340
Analogues of trypsin inhibitor SFTI-1 modified in the conserved P₁' position by synthetic or non-proteinogenic amino acids retain their inhibitory activityQ45794145
Examples of peptide-peptoid hybrid serine protease inhibitors based on the trypsin inhibitor SFTI-1 with complete protease resistance at the P1-P1' reactive siteQ46482047
Abbreviated nomenclature for cyclic and branched homo- and hetero-detic peptides.Q46483032
Membrane-bound serine protease matriptase-2 (Tmprss6) is an essential regulator of iron homeostasisQ46560159
Matriptase inhibition by hepatocyte growth factor activator inhibitor-1 is essential for placental developmentQ52573669
Engineering pro-angiogenic peptides using stable, disulfide-rich cyclic scaffoldsQ59286580
Ovarian carcinoma subtypes are different diseases: implications for biomarker studiesQ21563402
Matriptase-2, a membrane-bound mosaic serine proteinase predominantly expressed in human liver and showing degrading activity against extracellular matrix proteinsQ24302437
Regulation of cell surface protease matriptase by HAI2 is essential for placental development, neural tube closure and embryonic survival in miceQ24313255
Molecular mechanisms of the defective hepcidin inhibition in TMPRSS6 mutations associated with iron-refractory iron deficiency anemiaQ24314377
High-resolution structure of a potent, cyclic proteinase inhibitor from sunflower seedsQ27618903
Structure of a proteolytically resistant analogue of (NLys)5SFTI-1 in complex with trypsin: evidence for the direct participation of the Ser214 carbonyl group in serine protease-mediated proteolysisQ27689437
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reactionQ27860958
Matriptase-2 inhibits breast tumor growth and invasion and correlates with favorable prognosis for breast cancer patientsQ28306692
PyBOP®: A new peptide coupling reagent devoid of toxic by-productQ29303117
Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitorsQ29617995
Matriptase, HAT, and TMPRSS2 activate the hemagglutinin of H9N2 influenza A virusesQ30424187
Matriptase proteolytically activates influenza virus and promotes multicycle replication in the human airway epitheliumQ30426551
Molecular recognition mechanisms of thrombinQ33221756
Role of matriptase-2 (TMPRSS6) in iron metabolismQ33792112
Down-regulation of Bmp/Smad signaling by Tmprss6 is required for maintenance of systemic iron homeostasisQ33834771
Deregulated matriptase causes ras-independent multistage carcinogenesis and promotes ras-mediated malignant transformationQ33917709
The interaction of thrombin with fibrinogen. A structural basis for its specificityQ34416186
Substrate specificity of human matriptase-2.Q35026724
Improving the Selectivity of Engineered Protease Inhibitors: Optimizing the P2 Prime Residue Using a Versatile Cyclic Peptide LibraryQ35783014
Cleavage activation of the human-adapted influenza virus subtypes by matriptase reveals both subtype and strain specificitiesQ36276614
Reducing TMPRSS6 ameliorates hemochromatosis and β-thalassemia in miceQ36733512
An RNAi therapeutic targeting Tmprss6 decreases iron overload in Hfe(-/-) mice and ameliorates anemia and iron overload in murine β-thalassemia intermediaQ36849024
Exosites in the substrate specificity of blood coagulation reactionsQ36884329
Type II transmembrane serine proteases in development and diseaseQ37055730
IC50-to-Ki: a web-based tool for converting IC50 to Ki values for inhibitors of enzyme activity and ligand bindingQ37245607
Matriptase: a culprit in cancer?Q37401353
Matriptase-2 (TMPRSS6): a proteolytic regulator of iron homeostasisQ37450622
Iron-refractory iron deficiency anemia: new molecular mechanisms.Q37602503
Peptoid-Peptide hybrid backbone architectures.Q37657397
P433issue6
P577publication date2017-11-01
P1433published inBiopolymersQ15767528
P1476titleDesign and chemical syntheses of potent matriptase-2 inhibitors based on trypsin inhibitor SFTI-1 isolated from sunflower seeds
P478volume108

Reverse relations

Q93015323Antibodies raised against a Sunn bug (Eurygaster integriceps Put.) recombinant protease, rGHP3p2, can inhibit gluten-hydrolyzing activitycites workP2860

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