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Table 1

From: Signaling and regulation of G protein-coupled receptors in airway smooth muscle

GPCR

References

Couples to

Functions in ASM1

Comment

5-HT

[125, 126, 213–215]

Gi2

CXN, GP

5-HT2c identified, other subtypes likely

A1 adenosine

[42, 216, 217]

Gi

CXN

Low levels suggested in human ASM

A2b adenosine

[42]

Gs3

RLXN

Mediates effects of autocrine and paracrine adenosine

A3 adenosine

[218, 219]

Gq4

unclear

 

α-1 adrenergic

[220–223]

Gq

unclear

Only response in lung or ex vivo occurs with βAR antagonist present

β2 adrenergic

[56, 185, 224, 225]

Gs

RLXN, Cyt, GI

 

BK bradykinin

[39, 226–231]

Gq

CXN

Robust activation of PLC and PLA2 in cultured ASM;putative B3 yet to be cloned

CLT1R

[232–236]

Gq

CXN, GP

CLT1R antagonists most therapeutic of all GqCR antagonists

ET-A/B

[237–242]

Gq

CXN, GP

 

EDG 1–7

[38, 243–245]

Gq, Gi, G12/13

GS, Cyt

Most subtypes exhibit promiscuity toward G proteins

EP2

[20, 246, 247]

Gs

RLXN, GI, Cyt

Indirect evidence for expression of EP1, EP3, and EP4

H1 histamine

[248, 249]

Gq

CXN, GP

Exhibits homologous and heterologous desensitization

IP Prostacyclin

[41, 250]

Gs

GI

Responsive to autocrine PGI2 induced by cytokines via COX-2 induction

m2 muscarinic

[21, 251, 252]

Gi

unclear

Mediator of acute adenylyl cyclase inhibition, chronic sensitization

m3 muscarinic

[251–256]

Gq

CXN, GP

Rapid reduction of expression in culture

NK-1/2

[257–260]

Gq

CXN, GP

 

PAR-1,2,3

[34, 261, 262]

Gq, Gi, G12/13

GS, GP

Thrombin most mitogenic GPCR agonist; subtype promiscuity towards G proteins

P2 purinergic

[218, 219]

Gq

unclear

P1 may also be expressed

TP

[41, 263–266]

Gq, Gi, G12/13 (?)

CXN, GP

Coupling specificity poorly characterized in ASM

VIP

[43, 267, 268]

Gs

GI

 
  1. 1 Abbreviations: CXN – contraction; Cyt – regulation of ASM cytokine/chemokine synthesis; GI-inhibition of ASM growth (DNA synthesis/cell proliferation); GP – potentiation of growth stimulated by polypeptide growth factors; GS – growth stimulation ; RLXN – relaxation 2 Coupling to Gi is suggested by sensitivity of signal transduction or functional effects to pertussis toxin 3 All receptors noted to couple to Gs have been shown to stimulate cAMP production in ASM. 4 Coupling of receptors to Gq is suggested by either agonist-stimulated phosphoinositide production or calcium flux.
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Respiratory Research

ISSN: 1465-993X

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