DOI: 10.1016/s1074-5521(00)00104-6. Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator

Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator

10.1016/s1074-5521(00)00104-6

Crossref journal-article

Elsevier BV

Chemistry & Biology (78)

Bibliography

Katz, B. A., Mackman, R., Luong, C., Radika, K., Martelli, A., Sprengeler, P. A., Wang, J., Chan, H., & Wong, L. (2000). Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator. Chemistry & Biology, 7(4), 299â312.

Authors 9

Bradley A Katz (first)
Richard Mackman (additional)
Christine Luong (additional)
Kesavan Radika (additional)
Arnold Martelli (additional)
Paul A Sprengeler (additional)
Jing Wang (additional)
Hedy Chan (additional)
Lance Wong (additional)

References 31 Referenced 71

10.1016/S0006-291X(67)80055-X / Biochem. Biophys. Res. Commun. / On the size of the active site in proteinases. I. Papain by Schechter (1967)
10.1021/jm981068g / J. Med. Chem. / Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase by Renatus (1998)
10.1021/jm970485a / J. Med. Chem. / Rational design and synthesis of novel, potent bis-phenylamidine carboxylate factor Xa inhibitors by Maduskie (1998)
10.1021/jm980227t / J. Med. Chem. / Structure-based design of benzamidine-type inhibitors of factor Xa by Gabriel (1998)
10.1074/jbc.271.47.29988 / J. Biol. Chem. / X-ray structure of active site-inhibited clotting factor Xa: implications for drug design and substrate recognition by Brandstetter (1996)
{'key': '10.1016/S1074-5521(00)00104-6_BIB6', 'first-page': '2553', 'article-title': 'Inhibition of urokinase by 4-substituted benzo[b]thiophene-2-carboxamidines: an important new class of selective synthetic urokinase inhibitor', 'volume': '53', 'author': 'Towle', 'year': '1993', 'journal-title': 'Cancer Res.'} / Cancer Res. / Inhibition of urokinase by 4-substituted benzo[b]thiophene-2-carboxamidines: an important new class of selective synthetic urokinase inhibitor by Towle (1993)
10.1016/S0065-230X(08)60028-7 / Adv. Cancer Res. / Plasminogen activators, tissue degradation, and cancer by Dano (1985)
10.1002/(SICI)1097-0215(19970703)72:1<1::AID-IJC1>3.0.CO;2-Z / Int. J. Cancer / The urokinase-type plasminogen activator system in cancer metastasis: a review by Andreasen (1997)
{'key': '10.1016/S1074-5521(00)00104-6_BIB9', 'first-page': '911', 'article-title': 'Role of urokinase (uPA) and its receptor (uPAR) in invasion and metastasis of hormone-dependent malignancies', 'volume': '12', 'author': 'Rabbani', 'year': '1998', 'journal-title': 'Int. J. Oncol.'} / Int. J. Oncol. / Role of urokinase (uPA) and its receptor (uPAR) in invasion and metastasis of hormone-dependent malignancies by Rabbani (1998)
{'key': '10.1016/S1074-5521(00)00104-6_BIB10', 'first-page': '569', 'article-title': 'The role of proteolytic enzymes in the pathology of epithelial ovarian carcinoma', 'volume': '12', 'author': 'Stack', 'year': '1998', 'journal-title': 'Int. J. Oncol.'} / Int. J. Oncol. / The role of proteolytic enzymes in the pathology of epithelial ovarian carcinoma by Stack (1998)
10.1517/14728222.3.1.109 / Emerging Therapeutic Targets / Emerging therapeutic targets in oncology: urokinase-type plasminogen activator system by Magill (1999)
10.1006/jmbi.1996.0238 / J. Mol. Biol. / The 2.3 Å crystal structure of the catalytic domain of recombinant two-chain human tissue-type plasminogen activator by Lambda (1996)
10.1016/S0969-2126(01)00203-9 / Structure / The crystal structure of the catalytic domain of human urokinase-type plaminogen activator by Spraggon (1995)
10.1006/jmbi.1999.3071 / J. Mol. Biol. / Recruiting Zn+2 to mediate potent specific inhibition of serine proteases by Katz (1999)
Perrin, D.D. (1965). Dissociation constants of organic bases in aqueous solution. Supplement to Pure and Applied Chemistry, International Union of Pure and Applied Chemistry, London, Butterworths.
10.1016/S0022-2836(77)80200-3 / J. Mol. Biol. / The Protein Data Bank: a computer-based archival file for macromolecular structures by Bernstein (1977)
10.1016/0005-2744(76)90174-1 / Biochim. Biophys. Acta / Purification of urokinase by affinity chromatography by Holmberg (1976)
Bridges, A., Littlefield, B.A., Schwartz, C.E. Urokinase Inhibitors. 23 August 1994, US Patent 5340833.
10.1055/s-1984-30929 / Synthesis / A Novel one-step synthesis of 2-methoxycarbonylthieno[2,3-b]quinolines and 3-hydroxy-2-methoxycarbonyl-2-3-dihydrothieno[2,3-b]-quinolines by Bhat (1984)
10.1016/S0040-4039(01)94745-8 / Tetrahedron Lett. / A versatile new synthesis of quinolines, thienopyridines and related fused pyridines by Meth-Cohn (1978)
10.1006/abio.1996.0238 / Anal. Biochem. / Program DYNAFIT for the analysis of enzyme kinetic data: application to HIV proteinase by Kuzmic (1996)
10.1016/0076-6879(79)63008-2 / Methods Enzymol. / Statistical analysis of enzyme kinetic data by Cleland (1979)
{'key': '10.1016/S1074-5521(00)00104-6_BIB23', 'first-page': '408', 'article-title': 'Sparse matrix sampling: a screening method for crystallization of proteins', 'volume': '25', 'author': 'Jancarik', 'year': '1991', 'journal-title': 'J. Appl. Crystallogr.'} / J. Appl. Crystallogr. / Sparse matrix sampling: a screening method for crystallization of proteins by Jancarik (1991)
10.1016/0022-2836(91)80132-E / J. Mol. Biol. / Structure of the hirugen and hirulog 1 complexes of α-thrombin by Skrzpczak-Jankun (1991)
Chmielewska, J., Lundqvist, T., Mosialou, E., Ogg, D. Modified human factor Xa. 7 February 1998, International patent WO 98/28412.
10.1002/pro.5560070405 / Protein Sci. / Crystal structure of recombinant human tissue kallikrein at 2.0 Å resolution by Katz (1998)
10.1006/jmbi.1993.1441 / J. Mol. Biol. / Structure of human des(1–45) factor Xa at 2.2 Å resolution by Padmanabhan (1993)
10.1002/pro.5560031211 / Protein Sci. / The isomorphous structures of prethrombin2, hirugen- and PPACK-thrombin: changes accompanying activation and exosite binding to thrombin by Vijayalakshmi (1994)
10.1021/bi00026a008 / Biochemistry / Novel Ki ∼ nanomolar inhibitors of serine proteases by binding or epitaxial chemistry on an enzyme surface by Katz (1995)
{'key': '10.1016/S1074-5521(00)00104-6_BIB30', 'series-title': 'Gaussian 94, Revision E.3.', 'author': 'Frisch', 'year': '1995'} / Gaussian 94, Revision E.3. by Frisch (1995)
10.1002/jcc.540030212 / J. Comp. Chem. / Optimization of equilibrium geometries and transition structures by Schlegel (1982)

Dates

Type	When
Created	23 years ago (July 25, 2002, 9:54 a.m.)
Deposited	6 years, 3 months ago (April 28, 2019, 7:20 p.m.)
Indexed	1 month ago (July 19, 2025, 11:44 p.m.)
Issued	25 years, 4 months ago (April 1, 2000)
Published	25 years, 4 months ago (April 1, 2000)
Published Print	25 years, 4 months ago (April 1, 2000)

Funders 0

None

BibTeX

@article{Katz_2000, title={Structural basis for selectivity of a small molecule, S1-binding, submicromolar inhibitor of urokinase-type plasminogen activator}, volume={7}, ISSN={1074-5521}, url={http://dx.doi.org/10.1016/s1074-5521(00)00104-6}, DOI={10.1016/s1074-5521(00)00104-6}, number={4}, journal={Chemistry & Biology}, publisher={Elsevier BV}, author={Katz, Bradley A and Mackman, Richard and Luong, Christine and Radika, Kesavan and Martelli, Arnold and Sprengeler, Paul A and Wang, Jing and Chan, Hedy and Wong, Lance}, year={2000}, month=apr, pages={299–312} }

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