4b72: Difference between revisions

Revision as of 12:52, 30 June 2013

Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in BrainAminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain

FunctionFunction

[BACE1_HUMAN] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.^[1] ^[2]

About this StructureAbout this Structure

4b72 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

ReferenceReference

^{[xtra 1]}

↑ Ginman T, Viklund J, Malmstrom J, Blid J, Emond R, Forsblom R, Johansson A, Kers A, Lake F, Sehgelmeble F, Sterky KJ, Bergh M, Lindgren A, Johansson P, Jeppsson F, Falting J, Gravenfors Y, Rahm F. Core Refinement toward Permeable beta-Secretase (BACE-1) Inhibitors with Low hERG Activity. J Med Chem. 2013 Jun 13;56(11):4181-205. doi: 10.1021/jm3011349. Epub 2013 May, 20. PMID:23126626 doi:10.1021/jm3011349

↑ Lin X, Koelsch G, Wu S, Downs D, Dashti A, Tang J. Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein. Proc Natl Acad Sci U S A. 2000 Feb 15;97(4):1456-60. PMID:10677483
↑ Okada H, Zhang W, Peterhoff C, Hwang JC, Nixon RA, Ryu SH, Kim TW. Proteomic identification of sorting nexin 6 as a negative regulator of BACE1-mediated APP processing. FASEB J. 2010 Aug;24(8):2783-94. doi: 10.1096/fj.09-146357. Epub 2010 Mar 30. PMID:20354142 doi:10.1096/fj.09-146357

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OCA

[3] Ginman T, Viklund J, Malmstrom J, Blid J, Emond R, Forsblom R, Johansson A, Kers A, Lake F, Sehgelmeble F, Sterky KJ, Bergh M, Lindgren A, Johansson P, Jeppsson F, Falting J, Gravenfors Y, Rahm F. Core Refinement toward Permeable beta-Secretase (BACE-1) Inhibitors with Low hERG Activity. J Med Chem. 2013 Jun 13;56(11):4181-205. doi: 10.1021/jm3011349. Epub 2013 May, 20. PMID:23126626 doi:10.1021/jm3011349

[1] Lin X, Koelsch G, Wu S, Downs D, Dashti A, Tang J. Human aspartic protease memapsin 2 cleaves the beta-secretase site of beta-amyloid precursor protein. Proc Natl Acad Sci U S A. 2000 Feb 15;97(4):1456-60. PMID:10677483

[2] Okada H, Zhang W, Peterhoff C, Hwang JC, Nixon RA, Ryu SH, Kim TW. Proteomic identification of sorting nexin 6 as a negative regulator of BACE1-mediated APP processing. FASEB J. 2010 Aug;24(8):2783-94. doi: 10.1096/fj.09-146357. Epub 2010 Mar 30. PMID:20354142 doi:10.1096/fj.09-146357

[1]

[2]

[xtra 1]

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+{{STRUCTURE_4b72|  PDB=4b72  |  SCENE=  }}
+===Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain===
+{{ABSTRACT_PUBMED_23126626}}
-The entry 4b72 is ON HOLD  until Paper Publication
+==Function==
+[[http://www.uniprot.org/uniprot/BACE1_HUMAN BACE1_HUMAN]] Responsible for the proteolytic processing of the amyloid precursor protein (APP). Cleaves at the N-terminus of the A-beta peptide sequence, between residues 671 and 672 of APP, leads to the generation and extracellular release of beta-cleaved soluble APP, and a corresponding cell-associated C-terminal fragment which is later released by gamma-secretase.<ref>PMID:10677483</ref> <ref>PMID:20354142</ref>
-Authors: Gravenfors, Y., Blid, J., Ginman, T., Karlstrom, S., Kihlstrom, J., Kolmodin, K., Lindstrom, J., Berg, S., Kieseritzky, F., Slivo, C., Swahn, B., Viklund, J., Olsson, L., Johansson, P., Eketjall, S., Falting, J., Jeppsson, F., Stromberg, K., Janson, J., Rahm, F.
+==About this Structure==
+[[4b72]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4B72 OCA].
-Description: Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab-lowering in Brain
+==Reference==
+<ref group="xtra">PMID:023126626</ref><references group="xtra"/><references/>
+[[Category: Homo sapiens]]
+[[Category: Memapsin 2]]
+[[Category: Berg, S.]]
+[[Category: Blid, J.]]
+[[Category: Eketjall, S.]]
+[[Category: Falting, J.]]
+[[Category: Ginman, T.]]
+[[Category: Gravenfors, Y.]]
+[[Category: Janson, J.]]
+[[Category: Jeppsson, F.]]
+[[Category: Johansson, P.]]
+[[Category: Karlstrom, S.]]
+[[Category: Kieseritzky, F.]]
+[[Category: Kihlstrom, J.]]
+[[Category: Kolmodin, K.]]
+[[Category: Lindstrom, J.]]
+[[Category: Olsson, L.]]
+[[Category: Rahm, F.]]
+[[Category: Slivo, C.]]
+[[Category: Stromberg, K.]]
+[[Category: Swahn, B.]]
+[[Category: Viklund, J.]]
+[[Category: Hydrolase]]
+[[Category: Hydrolase inhibitor]]
+[[Category: Lead generation]]
+[[Category: Structure-based drug design]]

4b72: Difference between revisions

Revision as of 12:52, 30 June 2013

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Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in BrainAminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain

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4b72: Difference between revisions

Revision as of 12:52, 30 June 2013

Aminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in BrainAminoimidazoles as BACE-1 Inhibitors: From De Novo Design to Ab- lowering in Brain

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About this StructureAbout this Structure

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