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2zkm

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2zkm, resolution 1.62Å ()
Sites:
Ligands:
Gene: PLC beta 2 (Homo sapiens)
Activity: Phosphoinositide phospholipase C, with EC number 3.1.4.11
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



Crystal Structure of Phospholipase C Beta 2

Publication Abstract from PubMed

Phospholipase C (PLC) isozymes are directly activated by heterotrimeric G proteins and Ras-like GTPases to hydrolyze phosphatidylinositol 4,5-bisphosphate into the second messengers diacylglycerol and inositol 1,4,5-trisphosphate. Although PLCs play central roles in myriad signaling cascades, the molecular details of their activation remain poorly understood. As described here, the crystal structure of PLC-beta2 illustrates occlusion of the active site by a loop separating the two halves of the catalytic TIM barrel. Removal of this insertion constitutively activates PLC-beta2 without ablating its capacity to be further stimulated by classical G protein modulators. Similar regulation occurs in other PLC members, and a general mechanism of interfacial activation at membranes is presented that provides a unifying framework for PLC activation by diverse stimuli.

General and versatile autoinhibition of PLC isozymes., Hicks SN, Jezyk MR, Gershburg S, Seifert JP, Harden TK, Sondek J, Mol Cell. 2008 Aug 8;31(3):383-94. PMID:18691970

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

About this Structure

2zkm is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

  • Hicks SN, Jezyk MR, Gershburg S, Seifert JP, Harden TK, Sondek J. General and versatile autoinhibition of PLC isozymes. Mol Cell. 2008 Aug 8;31(3):383-94. PMID:18691970 doi:10.1016/j.molcel.2008.06.018
  • Jezyk MR, Snyder JT, Gershberg S, Worthylake DK, Harden TK, Sondek J. Crystal structure of Rac1 bound to its effector phospholipase C-beta2. Nat Struct Mol Biol. 2006 Dec;13(12):1135-40. Epub 2006 Nov 19. PMID:17115053 doi:10.1038/nsmb1175

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