Crystal structure of hepatocyte growth factor activator...

Details Crystal structure of hepatocyte growth factor activator... Crystal structure of hepatocyte growth factor activator...

2005-12-09

2010-06-22

Nashed, Nashaat T (Department: 1656)

Chemistry: molecular biology and microbiology

Enzyme , proenzyme; compositions thereof; process for...

Hydrolase

C435S219000, C435S212000, C435S023000

Reexamination Certificate

active

07741096

ABSTRACT:
The present disclosure provides crystals of and structural coordinates of Hepatocyte growth factor activator with and without bound pseudo-substrate or inhibitor. In a specific embodiment, a crystal structure of activated HGFA complexed with a Kunitz domain inhibitor is provided. The crystals and crystal structures are useful, for example, in the design and synthesis of inhibitors of HGFA.

REFERENCES:
patent: RE30985 (1982-06-01), Cartaya
patent: 4560655 (1985-12-01), Baker
patent: 4657866 (1987-04-01), Kumar
patent: 4767704 (1988-08-01), Cleveland et al.
patent: 4927762 (1990-05-01), Darfler
patent: 5122469 (1992-06-01), Mather et al.
patent: WO-87/00195 (1987-01-01), None
patent: WO-90/03430 (1990-04-01), None
Ganunis, R.M. et al. (1996). “Effect of the Crystallizing Agent 2-Methyl-2,4-pentanediol on the Structure of Adenine Tract DNA in Solution,”Biochemistry35(43):13729-13732.
Banner, D.W. et al. (Mar. 7, 1996). “The Crystal Structure of the Complex of Blood Coagulation Factor Vlla with Soluble Tissue Factor,”Nature380:41-46.
Barnes, D. et al. (1980). “Methods for Growth of Cultured Cells in Serum-Free Medium,”Anal. Biochem.102:255-270.
Bode, W. et al. (1997). “Comparative Analysis of Haemostatic Proteinases: Structural Aspects of Thrombin, Factor Xa, Factor IXa and Protein C,”Thromb. Haemost.78(1):501-511.
Böhm, H-J. (1992). “The Computer Program LUDI: A New Method for the de novo Design of Enzyme Inhibitors,”J. Comput. Aided Molec. Design6:61-78.
Brünger, A.T. (Jan. 30, 1992). “FreeRValue: A Novel Statistical Quantity for Assessing the Accuracy of Crystal Structures,”Nature355:472-475.
Bussolino, F. et al. (Nov. 1, 1992). “Hepatocyte Growth Factor Is a Potent Angiogenic Factor Which Stimulates Endothelial Cell Motility and Growth,”J. Cell Biol.119(3):629-641.
Cavarelli, J. et al. (Jun. 15, 1997). “The Structure ofStaphylococcus aureusEpidermolytic Toxin A, an Atypic Serine Protease, at 1.7 Å Resolution,”Structure5(5):813-824.
Denda, K. et al. (Apr. 19, 2002, e-pub. Jan. 22, 2002). “Functional Characterization of Kunitz Domains in Hepatocyte Growth Factor Activator Inhibitor Type 1,”J. Biol. Chem.277(16):14053-14059.
Dennis, M.S. et al. (Mar. 30, 2000). “Peptide Exosite Inhibitors of Factor Vlla as Anticoagulants,”Nature404:465-470.
Dennis, M.S. et al. (2001, e-pub. Jul. 11, 2001). “Selection and Characterization of a New Class of Peptide Exosite Inhibitors of Coagulation Factor Vlla,”Biochemistry40(32):9513-9521.
Eigenbrot, C. et al. (Jul. 2001). “The Factor Vll Zymogen Structure Reveals Reregistration of β Strands During Activation,”Structure9:627-636.
Friedrich, R. et al. (Jan. 18, 2002, e-pub. Nov. 5, 2001). “Catalytic Domain Structures of MT-SP1/Matriptase, a Matrix-degrading Transmembrane Serine Proteinase,”J. Biol. Chem.277(3):2160-2168.
Genbank Accession No. NP—001027539.1, gi:74027265, last updated Oct. 5, 2009, located at <http://www.ncbi.nlm.nih.gov/protein/74027265>, last visited Nov. 24, 2009, seven pages.
Gillet, V. et al. (1993). “SPROUT: A Program for Structure Generation,”J. Comput. Aided Mol. Design7:127-153.
Goodsell, D.S. et al. (1990). “Automated Docking of Substrates to Proteins by Simulated Annealing,”Proteins8:195-202.
Ham, R.G. et al. (1979). “Media and Growth Requirements,” Chapter 5in Methods in Enzymology, 58:44-93.
Hayashi, T. et al. (1998). “Inductions of Hepatocyte Growth Factor and its Activator in Rat Brain with Permanent Middle Cerebral Artery Occlusion,”Brain Res.799:311-316.
Hermoso, M. et al. (Apr. 23, 2004, e-pub. Feb. 11, 2004). “Cell Volume Regulation in Response to Hypotonicity is Impaired in HeLa Cells Expressing a Protein Kinase Cα Mutant Lacking Kinase Activity,”J. Biol. Chem.279(17):17681-17689.
Huang, C. et al. (Jul. 9, 1999). “Human Tryptases α and β/ll Are Functionally Distinct Due, in Part, to a Single Amino Acid Difference in One of the Surface Loops That Forms the Substrate-binding Cleft,”J. Biol. Chem.274(28):19670-19676.
Hubbard, S.R. (Aug. 1999). “Src Autoinhibition: Let Us Count The Ways,”Nature Struct. Biol.6(8):711-714.
Huber, R. et al. (1978). “Structural Basis of the Activation and Action of Trypsin,”Acc. Chem. Res.11:114-122.
International Search Report mailed Jul. 12, 2006, for PCT Application No. PCT/US2005/044752, filed Dec. 9, 2005, six pages.
Itoh, H. et al. (2000). “Mouse Heptocyte Growth Factor Activator Gene: Its Expression Not Only in the Liver But Also in the Gastrointestinal Tract,”Biochim. Biophys. Acta1491:295-302.
Kataoka, H. et al. (Nov. 1, 2000). “Activation of Hepatocyte Growth Factor/Scatter Factor in Colorectal Carcinoma,”Cancer Res.60:6148-6159.
Kataoka, H. et al. (2003). “Roles of Hepatocyte Growth Factor (HGF) Activator and HGF Activator Inhibitor in the Pericellular Activation of HGF/Scatter Factor,”Cancer and Metastasis Rev.22:223-236.
Kawaguchi, T. et al. (Oct. 31, 1997). “Purification and Cloning of Hepatocyte Growth Factor Activator Inhibitor Type 2, a Kunitz-type Serine Protease Inhibitor,”J. Biol. Chem.272(44):27558-27564.
Kirchhofer, D. et al. (2001, e-pub. Dec. 22, 2000). “The Tissue Factor Region That Interacts with Factor Xa in the Activation of Factor Vll,”Biochemistry40(3):675-682.
Kirchhofer, D. et al. (Sep. 19, 2003, e-pub. Jun. 18, 2003). “Tissue Expression, Protease Specificity, and Kunitz Domain Functions of Hepatocyte Growth Factor Activator Inhibitor-1B (HAI-1 B), a New Splice Variant of HAI-1,”J. Biol. Chem.278(38):36341-36349.
Kirchhofer, D. et al. (Sep. 17, 2004, e-pub. Jun. 24, 2004). “Structural and Functional Basis of the Serine Protease-like Heptocyte Growth Factor β-Chain in Met Binding and Signaling,”J. Biol. Chem.279(38):39915-39924.
Kuntz, I.D. et al. (1982). “A Geometric Approach to Macromolecule-Ligand Interactions,”J. Mol. Biol.161:269-288.
Lander, E.S. et al. (Feb. 15, 2001). “Initial Sequencing and Analysis of the Human Genome,”Nature409:860-921.
Lattman, E. (1985). “Use of the Rotation and Translation Functions,” Chapter 5in Methods in Enzymology, 115:55-77.
Lee, B. et al. (Feb. 14, 1971). “The Interpretation of Protein Structures: Estimation of Static Accessibility,”J. Mol. Biol.55(3):379-400.
Marquardt, U. et al. (2002). “The Crystal Structure of Human α1 -Tryptase Reveals a Blocked Substrate-binding Region,”J. Mol. Biol.321:491-502.
Mather, J.P. (1980). “Establishment and Characterization of Two Distinct Mouse Testicular Epithelial Cell Lines,”Biol. Reprod.23:243-252.
Mcree, D.E. (1999). “Xta/View/Xfit-A Versatile Program for Manipulating Atomic Coordinates and Electron Density,”J. Struct. Biol.125:156-165.
Meng, E.G. et al. (1992). “Automated Docking with Grid-Based Energy Evaluation,”J. Comp. Chem.13(4):505-524.
Miranker, A. et al. (1991). “Functionality Maps of Binding Sites: A Multiple Copy Simultaneous Search Method,”Proteins11:29-34.
Moriyama, T. et al. (1995). “Concomitant Expression of Hepatocyte Growth Factor (HGF), HGF Activator and cmet Genes in Human Glioma Cells in vitro,”FEBS Lett.372:78-82.
Nagata, K. et al. (2001). “Expression of Hepatocyte Growth Factor Activator and Hepatocyte Growth Factor Activator Inhibitor Type 1 in Human Hepatocellular Carcinoma,”Biochem Biophys. Res. Comm.289(1):205-211.
Navaza, J. (1994). “AMoRe: An Automated Package for Molecular Replacement,”Acta Crystallogr.A50:157-163.
Nicolaou, K.C. et al. (1994). “Calicheamicin ⊖11: A Retionally Designed Molecule with Extremely Potent and Selective DNA Cleaving Properties and Apoptosis Inducing Activity,”Agnew Chem. Intl. Ed. Engl.3

Affiliated with

Also associated with

Rating

Crystal structure of hepatocyte growth factor activator... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Crystal structure of hepatocyte growth factor activator..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Crystal structure of hepatocyte growth factor activator... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-4249484