2p2c
From Proteopedia
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[[Image:2p2c.gif|left|200px]] | [[Image:2p2c.gif|left|200px]] | ||
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'''Inhibition of caspase-2 by a designed ankyrin repeat protein (DARPin)''' | '''Inhibition of caspase-2 by a designed ankyrin repeat protein (DARPin)''' | ||
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[[Category: Gruetter, M G.]] | [[Category: Gruetter, M G.]] | ||
[[Category: Voser, HRoschitzki.]] | [[Category: Voser, HRoschitzki.]] | ||
| - | [[Category: | + | [[Category: Apoptosis]] |
| - | [[Category: | + | [[Category: Caspase]] |
| - | [[Category: | + | [[Category: Caspase-2]] |
| - | [[Category: | + | [[Category: Designed ankyrin repeat protein]] |
| - | [[Category: | + | [[Category: Inhibition]] |
| - | [[Category: | + | [[Category: Protein design]] |
| - | [[Category: | + | [[Category: Protein library]] |
| - | [[Category: | + | [[Category: Ribosome display]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 12:11:39 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 09:11, 4 May 2008
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 Page seeded by OCA on Sun May 4 12:11:39 2008
