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C2.1 Chemical signaling

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receptor
ligand
oestradiol
progesterone
acetylcholine
second messenger
GPCR
RTK
feedback
quorum sensing
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Understanding points

C2.1.1 Receptors as proteins with binding sites for specific signalling chemicals (HL only) C2.1.2 Cell signalling by bacteria in quorum sensing (HL only) C2.1.3 Hormones, neurotransmitters, cytokines and calcium ions as examples of functional categories of signalling chemicals in animals (HL only) C2.1.4 Chemical diversity of hormones and neurotransmitters (HL only) C2.1.5 Localized and distant effects of signalling molecules (HL only) C2.1.6 Differences between transmembrane receptors in a plasma membrane and intracellular receptors in the cytoplasm or nucleus (HL only) C2.1.7 Initiation of signal transduction pathways by receptors (HL only) C2.1.8 Transmembrane receptors for neurotransmitters and changes to membrane potential (HL only) C2.1.9 Transmembrane proteins that activate G protein (HL only) C2.1.10 Mechanism of action of epinephrine (adrenaline) receptors (HL only) C2.1.11 Transmembrane receptors with tyrosine kinase activity (HL only) C2.1.12 Intracellular receptors that affect gene expression (HL only) C2.1.13 Effects of the hormones oestradiol and progesterone on target cells (HL only) C2.1.14 Regulation of cell signalling pathways by positive and negative feedback (HL only)

Receptors

Signals can be chemical or electrical
Ligand: a molecule that binds specifically to a site on a receptor
Receptor: a molecule that binds with ligands to convey signals that affect cellular activity
The specificity of receptor-ligand binding is similar to enzyme-substrate interactions

Signalling chemicals

Hormones 
Produced by endocrine glands Secreted and transported by blood vessels
Long-lasting effects Act at a distant site
Amine: melatonin Peptide: insulin Steroid: testosterone
Neurotransmitters 
Secreted by presynaptic neurons into the synaptic cleft
Short-lived effects Act at a local site
Amine: dopamine Amino acid: glutamate Ester: acetylcholine Gas: nitrous oxide
Cytokines 
Secreted by a wide range of cells
Multiple effects Act locally
e.g. erythropoietin
Ca²⁺ ions 
Increases in intracellular concentration lead to effects
Short-lived effects
e.g. Ca²⁺

Oestradiol and progesterone

Female sex hormones secreted by the ovaries
Oestradiol
Progesterone
Promotes development and maintenance of female sex characteristics
Promotes development of the endometrium for implantation
Oestradiol (ovaries) ↓ GnRH (hypothalamus) ↓ LH, FSH (anterior pituitary) ↓ Ovulation
Progesterone (ovaries) ↓ Thickening of the endometrium ↓ Preparation for implantation

Acetylcholine

Signal transduction pathway

A cascade of reactions in the cell caused by receptor-ligand binding
Second messenger: small, non-protein molecules or ions that amplify the signal
e.g. cAMP, Ca²⁺
Transmembrane receptor 
Intracellular receptor 
Location 
Plasma membrane 
Cytosol or nucleus 
Type of ligand
Polar, hydrophilic ligands that cannot cross the cell membrane 
Nonpolar, lipophilic ligands that easily cross the cell membrane 
Signal transduction
Ligand binds to extracellular domain of receptor ↓ Structural change in receptor ↓ Intracellular domain generates second messenger ↓ Activation of effectors ↓ Cellular response
Ligand diffuses through plasma membrane ↓ Ligand binds to receptor ↓ Formation of active ligand- receptor complex ↓ Binding of DNA and regulation of transcription ↓ Cellular response
e.g. GPCR, RTK
e.g. steroid hormone receptors
Transmembrane receptor signal transduction
Intracellular receptor signal transduction

G protein-coupled receptor (GPCR)

Common structure of 7 hydrophobic α-helices
Convey signals via G proteins composed of αβγ subunits
GDP-bound G protein is inactive, GTP bound G protein is active
When the ligand is no longer present, GTPase hydrolyzes GTP to GDP and inactivates the G protein, terminating the signal pathway
e.g. Epinephrine signaling:

Receptor tyrosine kinase (RTK)

Phosphorylation: transfer of phosphate group from ATP to a substrate molecule
RTKs phosphorylates tyrosine on its intracellular tails
e.g. Insulin signaling:

Feedback regulation

The end product of a pathway interacts with an earlier stage to promote or inhibit the pathway
Positive 
Negative 
End product promotes its own production
End product inhibits its own production 
e.g. LH surge during ovulatory phase of menstrual cycle
e.g. thyroxine secretion
Positive feedback
Negative feedback

Quorum sensing

Intercellular communication used for collective activation of genes in response to increased bacterial population density
e.g. bioluminescence in Vibrio fischeri: at high population density, autoinducer molecules secreted by the bacteria bind to a cytoplasmic receptor called LuxR and induce the transcription of genes encoding luciferase, which catalyzes an oxidation reaction that produces light