First time at Proteopedia? Click on the green links, they change the 3D image. Click and drag the molecules. Proteopedia is a 3D, interactive encyclopedia of proteins, RNA, DNA and other molecules. With a free user account, you can edit pages in Proteopedia. Visit the Main Page to learn more.
2p2c
From Proteopedia
| 2p2c, resolution 3.24Å () | |||||||||
|---|---|---|---|---|---|---|---|---|---|
| Gene: | CASP2 (Homo sapiens) | ||||||||
| Domains: | CASc, ANK | ||||||||
| 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)
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.
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
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
About this Structure
2P2C is a 18 chains structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.
Reference
- Schweizer A, Roschitzki-Voser H, Amstutz P, Briand C, Gulotti-Georgieva M, Prenosil E, Binz HK, Capitani G, Baici A, Pluckthun A, Grutter MG. Inhibition of caspase-2 by a designed ankyrin repeat protein: specificity, structure, and inhibition mechanism. Structure. 2007 May;15(5):625-36. PMID:17502107 doi:10.1016/j.str.2007.03.014
Page seeded by OCA on Mon Feb 16 16:03:46 2009
