2p2c
From Proteopedia
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|ACTIVITY= | |ACTIVITY= | ||
|GENE= CASP2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | |GENE= CASP2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | |DOMAIN= | ||
| + | |RELATEDENTRY=[[1pyo|1PYO]], [[1mjo|1MJO]] | ||
| + | |RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p2c FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p2c OCA], [http://www.ebi.ac.uk/pdbsum/2p2c PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2p2c RCSB]</span> | ||
}} | }} | ||
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[[Category: ribosome display]] | [[Category: ribosome display]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:27:35 2008'' |
Revision as of 01:27, 31 March 2008
| |||||||
| , resolution 3.24Å | |||||||
|---|---|---|---|---|---|---|---|
| Gene: | CASP2 (Homo sapiens) | ||||||
| Related: | 1PYO, 1MJO
| ||||||
| Resources: | FirstGlance, OCA, PDBsum, RCSB | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
Inhibition of caspase-2 by a designed ankyrin repeat protein (DARPin)
Overview
Specific and potent caspase inhibitors are indispensable for the dissection of the intricate pathways leading to apoptosis. We selected a designed ankyrin repeat protein (DARPin) from a combinatorial library that inhibits caspase-2 in vitro with a subnanomolar inhibition constant and, in contrast to the peptidic caspase inhibitors, with very high specificity for this particular caspase. The crystal structure of this inhibitor (AR_F8) in complex with caspase-2 reveals the molecular basis for the specificity and, together with kinetic analyses, the allosteric mechanism of inhibition. The structure also shows a conformation of the active site that can be exploited for the design of inhibitory compounds. AR_F8 is a specific inhibitor of an initiator caspase and has the potential to help identify the function of caspase-2 in the complex biological apoptotic signaling network.
About this Structure
2P2C is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
Inhibition of caspase-2 by a designed ankyrin repeat protein: specificity, structure, and inhibition mechanism., Schweizer A, Roschitzki-Voser H, Amstutz P, Briand C, Gulotti-Georgieva M, Prenosil E, Binz HK, Capitani G, Baici A, Pluckthun A, Grutter MG, Structure. 2007 May;15(5):625-36. PMID:17502107
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