Intracellular Ca2+ Signaling
2004

Why Calcium?
Na+ and Cl- are sea water
Excluded to maintain low osmotic pressure
[K+]i kept high for electrical neutrality
[Ca2+]i maintained very low
Prevents precipitation of organic anions
Mg2+ helps solubilize organic anions

How cells keep [Ca]i low
All eukaryotic cells have PM Ca2+-ATPase
Excitable cells also have Na+/Ca2+ exchanger (NCX)
ER Ca2+-ATPase (against a high grad)
Mitochondrial high capacity (low affinity) pump
When [Ca]i very high (dangerous) levels (>10-5 M)
Inner mitochondrial membrane
Uses the electrochemical gradient generated during electron-transfer of oxidative-phosphorylation

Calcium Concentrations
[Ca2+]o / [Ca2+]i >104
[Ca2+]o ~10-3 M
[Ca2+]ER ~10-3 M
[Ca2+]i <10-7 M at rest

Ca2+ - a versatile signal

Ca2+ - a versatile signal
Synaptic vesicle release (ms)
Excitation-contraction coupling (ms)
Smooth muscle relaxation (ms-sec)
Excitation-transcription coupling (min-h)
Gene transcription (h)
Fertilization (h)

How Ca2+ is measured
Ratiometric dyes
Cameleons

How cells ↑ [Ca]i
Voltage-gated Ca2+ Channels
Membrane potential drives Ca2+ down its chemical gradient
Different channels in different cells
Different properties for different purposes

Ca2+ shut-off pathways
Voltage-gated Ca2+ channels inactivate
IP3 rapidly dephosphorylated
Ca2+ rapidly pumped out

Ca2+ oscillations

Intracellular Ca2+ Targets
EF hand-containing proteins
Calmodulin
C2 domain proteins
PKC
Synaptogamin

Intracellular Ca2+ Targets
EF hand proteins
Troponin C
Calmodulin
Calcineurin
Calpain
Recoverin
S100

Calmodulin (CaM)
16.8 kDa Ca2+-binding protein
Highly conserved in all eukaryotes
Up to 1% of protein
Binds 4 mol Ca2+/mol
Binding affinity ~ .25-1x106 M
Cooperativity with Hill constant ~ 2

Classical mode of CaM regulation
Relief of autoinhibition

CaMKII
Autoinhibition and
Frequency Decoder

New modes of CaM interaction

New modes of CaM interaction
New modes of CaM regulation

Intracellular Ca2+ Targets
C2 Domains
Protein kinase C
Synaptotagmin
Phospholipase A2

C2 domains -  PKC

Synaptotagmin and neurotransmitter release