Crystallization and structure determination of glycosylated...

Details Crystallization and structure determination of glycosylated... Crystallization and structure determination of glycosylated...

2005-01-25

2009-10-13

Steadman, David J (Department: 1656)

Chemistry: molecular biology and microbiology

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

Hydrolase

C436S004000

Reexamination Certificate

active

07601528

ABSTRACT:
An inhibitor bound form of human beta secretase, also known as memapsin 2 and BACE, particularly in a glycosylated form as expressed in Chinese hamster ovary (CHO), HEK293 cells, or in insect cells as part of a Baculovirus expression system has been crystallized, and the three dimensional x-ray crystal structure has been solved to 3.2 Å resolution. The x-ray crystal structure is useful for solving the structure of other molecules or molecular complexes, and designing inhibitors of human beta secretase activity.

REFERENCES:
patent: 5744346 (1998-04-01), Chrysler et al.
patent: 5942400 (1999-08-01), Anderson et al.
patent: 6221645 (2001-04-01), Chrysler et al.
patent: 6225103 (2001-05-01), Keolsch et al.
patent: 6245884 (2001-06-01), Hook
patent: 6258386 (2001-07-01), Xia et al.
patent: 6268158 (2001-07-01), Pantoliano et al.
patent: 6291223 (2001-09-01), Christie et al.
patent: 6297021 (2001-10-01), Nienaber et al.
patent: 6329163 (2001-12-01), Anderson et al.
patent: 6420534 (2002-07-01), Gurney et al.
patent: 6440698 (2002-08-01), Gurney et al.
patent: 6545127 (2003-04-01), Tang et al.
patent: 7217556 (2007-05-01), Benson et al.
patent: 7384773 (2008-06-01), Benson et al.
patent: 7442537 (2008-10-01), Benson et al.
patent: 7524668 (2009-04-01), Benson et al.
patent: 2001/0016324 (2001-08-01), Gurney et al.
patent: 2001/0018208 (2001-08-01), Gurney et al.
patent: 2001/0021391 (2001-09-01), Gurney et al.
patent: 2002/0037315 (2002-03-01), Gurney et al.
patent: 2002/0049303 (2002-04-01), Tang et al.
patent: 2002/0055459 (2002-05-01), Chopra et al.
patent: 2002/0064819 (2002-05-01), Gurney et al.
patent: 2002/0081634 (2002-06-01), Gurney et al.
patent: 2002/0115600 (2002-08-01), Koelsch et al.
patent: 2003/0095958 (2003-05-01), Bhisetti et al.
patent: 2004/0014194 (2004-01-01), Beyer et al.
patent: 2006/0136141 (2006-06-01), Benson et al.
patent: WO 01/17369 (2000-03-01), None
patent: WO 01/00663 (2001-01-01), None
patent: WO 01/00685 (2001-01-01), None
patent: WO 01/23533 (2001-04-01), None
patent: WO 01/49097 (2001-07-01), None
patent: WO 01/49098 (2001-07-01), None
patent: WO 01/50829 (2001-07-01), None
patent: WO 02/25276 (2002-03-01), None
patent: WO 02/053594 (2002-07-01), None
patent: WO 03/012089 (2003-02-01), None
Branden et al., “Introduction to Protein Structure Second Edition”, Garland Publishing Inc., New York, 1999, pp. 374-375.
Drenth, “Principles of X-ray Crystallography,” Springer, New York, 1999, p. 1.
Kierzek et al., Biophys Chem 91:1-20, 2001.
McPherson et al., Eur. J. Biochem. 189:1-23, 1990.
Hong et al., Science 290 :150-153, 2000.
“Crystallization of Nucleic Acids and Proteins, A Practical Approach”, 2nd Ed., Ducruix and Giege, Oxford University Press, New York, 1999, p. 394.
Bartlett et al., “Caveata: program to facilitate the structure-derived design of biologically active molecules,”Molecular Recognition: Chemical and Biological Problems, Royal Society of Chemistry, Special Pub No. 78:182-196 (1989).
Benson et al., “An enzyme-substrate complex involved in bacterial cell wall biosynthesis,”Nat Struct Biol. Aug. 1995;2(8):644-53.
Berman et al., “The Protein Data Bank,”Nucleic Acids Res. Jan. 1, 2000;28(1):235-42.
Blundell et al.,Protein Crystallography, Academic Press, New York, NY; title page, publication page, and table of contents only, 8 pages (1976).
Böhm, “The computer program LUDI: a new method for the de novo design of enzyme inhibitors,”J Comput Aided Mol Des. Feb. 1992;6(1 ):61-78.
Collaborative Computational Project, No. 4, “TheCCP4suite: programs for protein crystallography”Acta Cryst. 1994;D50:760-3.
Eisen et al., “Hook: a program for finding novel molecular architectures that satisfy the chemical and steric requirements of a macromolecule binding site,”Proteins: Struct. Funct. Genei. Jul. 1994;19(3): 199-221.
Ermolieff et al., “Proteolytic activation of recombinant pro-memapsin 2 (pro-beta-secretase) studied with new fluorogenic substrates,”Biochemistry. Oct. 10, 2000;39(40): 12450-6.
Fairlie et al., “Conformational selection of inhibitors and substrates by proteolytic enzymes: implications for drug design and polypeptide processing,”J Med Chem. Apr. 6, 2000;43(7): 1271-81.
Finzel, “Lore: exploiting database of known structures,”Meth. Enzymol. 1997:277(B):230-42.
Gillet et al., “Sprout: a program for structure generation.”J Comput Aided Mol Des. Apr. 1993;7(2): 127-53.
Goodford, “A computational procedure for determining energetically favorable binding sites on biologically important macromolecules,”J Med Chem. Jul. 1985;28(7):849-57.
Goodsell et al., “Automated docking of substrates to proteins by simulated annealing,”Proteins: Struct. Funct. Genet. 1990;8(3): 195-202.
Haniu et al., “Characterization of Alzheimer's beta -secretase protein BACE. A pepsin family member with unusual properties,”J Biol Chem. Jul. 14, 2000;275(28):21099-106.
Hendrickson et al., “Selenomethionyl proteins produced for analysis by multi-wavelength anomalous diffraction (MAD): a vehicle for direct determination three-dimensional structure,”EMBO J. May 1990;9(5): 1665-72.
Hong et al, “Structure of the protease domain of memapsin 2 (β-secretase) complexed with inhibitor,”Science, Oct. 6, 2000,290(5489). 150-3.
Huang et al., “A 3D-structural model of memapsin 2 protease generated from theoretical study,”Acta PharmacolS in. Jan. 2001;22(1):50-56.
Hussain et al., “Identification of a novel aspartic protease (Asp 2) as β-secretase,”Mol Cell Neurosci. Dec. 1999;14(6):419-27.
Jiang et al., “Protein hydration observed by X-ray diffraction. Solvation properties of penicillopepsin and neuraminidase crystal structures,”J Mol Biol. Oct. 14, 1994;243(1): 100-15.
Kang et al., “The precursor of Alzheimer's disease amyloid A4 protein resembles a cell-surface receptor,”Nature. Feb. 19, 1987;325(6106):733-6.
Kitaguchi et al., “Novel precursor of Alzheimer's disease amyloid protein shows protease inhibitory activity,”Nature. Feb. 11, 1988 ;331(6156):530-2.
Kuntz et al., “A geometric approach to macromolecule-ligand interactions,”J Mol Biol. Oct. 25, 1982;161(2):269-88.
Lattman, “Use of the rotation and translation functions,”Methods Enzymol. 1985;115:55-77.
Lauri et al., “Caveat program to facilitate the design of organic molecules,”J Comput Aided Mol Des. Feb. 1994;8(1):51-66.
Lin et al., “Human aspartic protease memapsin 2 cleaves the β-secretase site of β-amyloid precursor protein,”Proc Natl Acad SciU S A. Feb. 15, 2000;97(4): 1456-60.
Mallender et al., “Characterization of recombinant, soluble beta-secretase from an insect cell expression system,”Mol Pharmacol. Mar. 2001;59(3):619-26.
Martin, “3D database searching in drug design,”J Med Chem. Jun. 12, 1992;35(12):2145-54.
Meng et al., “Automated docking with grid-based energy evaluation,”J. Comp. Chem, May 1992;13(4):505-524.
Miranker et al., “Functionality maps of binding sites: a multiple copy simultaneous search method,”Proteins: Struct. Funct. Genet. 1991 ;11(1):29-34.
National Institutes of Health, “Blast 2 Sequences,” [online] United States; retrieved Aug. 29, 2001 from the Internet: <URL:http:/http://www.ncbi.nlm.nih.gov/gorf/bl2.html>, 1 pg.
Navaza, “AMoRe: an automated package for molecular replacement,”Acta Cryst. 1994;A50:157-163.
Nishibata et al., “Automatic creation of drug candidate structures based on receptor structure. Starting point for artificial lead generation.”Tetrahedron,1991;47(43):8985-90.
Noren et al., “A general method for site-specific incorporation of unnatural amino acids into proteins,”Science. Apr. 14, 1989;244(4901): 182-8.
Park et al., “Molecular Characterization of

Affiliated with

Also associated with

Rating

Crystallization and structure determination of glycosylated... does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Crystallization and structure determination of glycosylated..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Crystallization and structure determination of glycosylated... will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-4132140