Protein kinase C

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Template:STRUCTURE 3gpe

Protein kinase C (PKC) phosphorylate serine or threonine residues in proteins. They act in signal transduction pathways. Conventional PKC (CPKC) - a, b1, b2, g – are activated by diacylglycerol (DAG), Ca+2 and a phospholipid. Novel PKC (NPKC) – d, e, eta, theta – are activated by DAG. Atypical (APKC) do not require DAG or Ca+2 for activation. PKC consists of regulatory domain hinged to a catalytic domain. The regulatory domain contains the C1 region which binds DAG and phorbol esters and the C2 domain which is a Ca+2 sensor. PKC contains Pleckstrin Homology (PH) domain which binds phosphatidylinositol lipids (PTDINS). The PH domain is found in proteins involved in intracellular signaling.

3D structures of protein kinase C

Conventional PKCs

PKC-a

1dsy, 3rdj – rCPKC-a C2 domain – rat

3rdl - rCPKC-a C2 domain + Pb

3gpe - rCPKC-a C2 domain + Ca + PTDINS

2eli – hCPKC-a C1 domain – human – NMR

3iw4 - hCPKC-a kinase domain + inhibitor

PKC-b

1a25 – rCPKC-b C2 domain

PKC-b2

2i0e - hCPKC-b2 catalytic domain

3pfq - rCPKC-b2 (mutant)

PKC-g

2uzp - hCPKC-g C2 domain

2e73 - hCPKC-g C1 domain - NMR

1tbn, 1tbo - rCPKC-g C2 domain – NMR

Novel PKC

PKC-d

1ptq – mNPKC-d C2 domain – mouse

1ptr - mNPKC-d C2 domain + phorbol-acetate

1bdy - rNPKC-d C2 domain

1yrk – hNPKC-d C2 domain + peptide

2yuu - hNPKC-d C1 domain - NMR

2coa - hNPKC-d PH domain – NMR

PKC-e

1gmi – rNPKC-e C2 domain

PKC-t

2enj - hNPKC-t C2 domain – NMR

2enn, 2enz - hNPKC-t C1 domain – NMR

1xjd – hNPKC-t + saurosporine

2jed - hNPKC-t kinase domain + inhibitor

PKC-eta

2fk9 – hNPKC-eta C2 domain

Atypical PKC

PKC-i

1vd2 – hAPKC-i PB1 domain – NMR

1zrz - hAPKC-i catalytic domain

3a8w, 3a8x - hAPKC-i kinase domain

1wmh - hAPKC-i PB1 domain + PAR6 alpha

PKC-nu

2d9z – hPKC-nu PH domain - NMR