Table 2.

Cell surface receptors whose signaling is modulated by IQGAP, and implications in physiology and pathology

ReceptorInteraction in cellsaDirect bindingbBinding site on IQGAP1Signaling outcomePhysiological and/or pathological implicationsReferencec
IQGAP1 
Receptor tyrosine kinases 
Axl Yes Yes IQ Inhibits Axl activation and signaling to Akt n.d. Gorisse et al., 2018  
EGFR Yes Yes IQ Promotes EGFR activation and signaling to ERK, Akt, STAT, and GTPases Drives tumorigenesis McNulty et al., 2011  
FGFR1 Yes Yes n.d. Stimulates N-WASP and B-Raf; promotes cell motility n.d. Benseñor et al., 2007  
HER2 Yes Yes IQ Sustains active HER2; induces resistance to trastuzumab Promotes breast tumorigenesis White et al., 2011  
IGF-1R n.d. n.d. IQd n.d. n.d. Salvi et al., 2022  
IR Yes Yes IQ Increases IR signaling to Akt and ERK Regulates glucose homeostasis; may contribute to diabetes Chawla et al., 2017  
MET Yes Yes n.d. Inhibits MET signaling; promotes Tyr phosphorylation of IQGAP1 Influences HGF/MET-induced tumorigenesis Hedman et al., 2020  
PDGFR-β Yes n.d. n.d. Modulates focal adhesion assembly and cell motility Coordinates vascular repair Kohno et al., 2013  
VEGFR2 Yes Yes n.d. Loosens cell adhesion and increases cell migration; stimulates angiogenesis and neurogenesis Contributes to macular degeneration and cancer development Yamaoka-Tojo et al., 2004  
G protein–coupled receptors 
CXCR2 Yes Yes CHD May inhibit chemotaxis n.d. Neel et al., 2011  
CXCR4 Yes n.d. n.d. Increases receptor trafficking, ERK activation, and cell migration n.d. Bamidele et al., 2015  
DOR1 n.d. n.d. n.d. Increases receptor trafficking and ERK activation n.d. Bamidele et al., 2015  
DP1 Yes n.d. n.d. Regulates DP1 trafficking; increases ERK activation n.d. Fréchette et al., 2021  
ET-1R n.d. n.d. n.d. Modulates GTPase activation; enhances cell migration, invasion, and metastasis May promote ovarian carcinogenesis Chellini et al., 2019  
GPR161 Yes n.d. n.d. Enhances cell migration and proliferation May contribute to breast cancer Feigin et al., 2014  
KISS1R Yes n.d. n.d. Stimulates EGFR transactivation n.d. Cvetkovic et al., 2013  
LGR4 Yes n.d. GRD Increases canonical and non-canonical Wnt signaling n.d. Carmon et al., 2014  
LGR5 Yes n.d. GRD and C-terminus Reduces IQGAP1 phosphorylation; increases Rac1 and actin binding n.d. Carmon et al., 2017  
LPA1 Yes n.d. n.d. Increases cell migration and invasion n.d. Alemayehu et al., 2013  
M3-mAChR n.d. n.d. n.d. Increases active Rac1; may couple M3-mAChR to actin cytoskeleton n.d. Ruiz-Velasco et al., 2002  
MOR1 n.d. n.d. n.d. Stimulates Rac1 and ERK activation n.d. Civciristov et al., 2019  
Receptor serine/threonine kinases 
TGFβR2 Yes Yes aa 1503–1657 Promotes TGFβR2 degradation; inhibits TGFβR2 signaling May constrain liver and bladder tumor growth Liu et al., 2013  
Glutamate-gated ion channels 
AMPAR (GluR4) Yes n.d. N-terminal May regulate cell surface targeting of GluR4 May participate in cognitive physiology and pathology Nuriya et al., 2005  
NMDAR (NR2A, NR2B) Yes n.d. n.d. Promotes cell surface targeting of NR2A; stimulates ERK signaling Gao et al., 2011  
Adhesion receptors 
β1-integrin Yes n.d. n.d. Couples β1-integrin to Rac1, RhoA, and Arf6 GTPases n.d. Nakajima et al., 2005  
β3-integrin Yes Yes n.d. Promotes cortical actin arrangements Controls vascular barrier protection Bhattacharya et al., 2012  
CD44 Yes n.d. n.d. Links CD44 to the cytoskeleton and ERK signaling Increases ovarian tumor cell migration Bourguignon et al., 2005  
E-cadherin Yes Yes RGCT Dissociates adherens junctions n.d. Kuroda et al., 1998  
N-cadherin Yes n.d. n.d Stimulates ERK1/2 signaling; regulates cell-cell adhesion Participates in fear memory and spermatogenesis Lui et al., 2005  
VE-cadherin Yes n.d. n.d. Destabilizes adherens junctions n.d. Yamaoka-Tojo et al., 2006  
T cell receptors 
OX40 Yes n.d. C-terminal Restrains OX40 cosignaling May coordinate inflammation Okuyama et al., 2020  
TCR n.d. n.d. n.d. Negatively regulates TCR-mediated signaling Gorman et al., 2012  
Receptor protein tyrosine phosphatases 
PTPμ Yes Yes n.d. Regulates GTPase-dependent functions of IQGAP1 and neurite outgrowth n.d. Phillips-Mason et al., 2006  
IQGAP2 
DP1 n.d. n.d. n.d. Inhibits ERK n.d. Fréchette et al., 2021  
IFN-α receptor n.d. n.d. n.d. Activates NF-κB-mediated gene expression May have antiviral actions Brisac et al., 2016  
LGR4 Yes n.d. n.d. n.d. n.d. Carmon et al., 2014  
PAR n.d. n.d. n.d. Modulates cytoskeletal dynamics n.d. Schmidt et al., 2003  
VEGFR2 n.d. n.d. n.d. Stimulates VEGF production, which activates VEGFR2 signaling to Akt Increases angiogenesis in breast cancer Kumar et al., 2022  
IQGAP3 
DP1 n.d. n.d. n.d. Activates ERK n.d. Fréchette et al., 2021  
EGFR n.d. n.d. n.d. Stimulates EGFR activation and signaling to ERK n.d. Yang et al., 2014  
FGFR1 n.d. n.d. n.d. Activates ERK May coordinate embryonic development Fang et al., 2015  
LGR4 Yes n.d. n.d. Enhances RSPO/LGR4 signaling to Wnt/β-catenin n.d. Carmon et al., 2014  
NGFR n.d. n.d. n.d. Triggers formation of cell extensions n.d. Caro-Gonzalez et al., 2012  
ReceptorInteraction in cellsaDirect bindingbBinding site on IQGAP1Signaling outcomePhysiological and/or pathological implicationsReferencec
IQGAP1 
Receptor tyrosine kinases 
Axl Yes Yes IQ Inhibits Axl activation and signaling to Akt n.d. Gorisse et al., 2018  
EGFR Yes Yes IQ Promotes EGFR activation and signaling to ERK, Akt, STAT, and GTPases Drives tumorigenesis McNulty et al., 2011  
FGFR1 Yes Yes n.d. Stimulates N-WASP and B-Raf; promotes cell motility n.d. Benseñor et al., 2007  
HER2 Yes Yes IQ Sustains active HER2; induces resistance to trastuzumab Promotes breast tumorigenesis White et al., 2011  
IGF-1R n.d. n.d. IQd n.d. n.d. Salvi et al., 2022  
IR Yes Yes IQ Increases IR signaling to Akt and ERK Regulates glucose homeostasis; may contribute to diabetes Chawla et al., 2017  
MET Yes Yes n.d. Inhibits MET signaling; promotes Tyr phosphorylation of IQGAP1 Influences HGF/MET-induced tumorigenesis Hedman et al., 2020  
PDGFR-β Yes n.d. n.d. Modulates focal adhesion assembly and cell motility Coordinates vascular repair Kohno et al., 2013  
VEGFR2 Yes Yes n.d. Loosens cell adhesion and increases cell migration; stimulates angiogenesis and neurogenesis Contributes to macular degeneration and cancer development Yamaoka-Tojo et al., 2004  
G protein–coupled receptors 
CXCR2 Yes Yes CHD May inhibit chemotaxis n.d. Neel et al., 2011  
CXCR4 Yes n.d. n.d. Increases receptor trafficking, ERK activation, and cell migration n.d. Bamidele et al., 2015  
DOR1 n.d. n.d. n.d. Increases receptor trafficking and ERK activation n.d. Bamidele et al., 2015  
DP1 Yes n.d. n.d. Regulates DP1 trafficking; increases ERK activation n.d. Fréchette et al., 2021  
ET-1R n.d. n.d. n.d. Modulates GTPase activation; enhances cell migration, invasion, and metastasis May promote ovarian carcinogenesis Chellini et al., 2019  
GPR161 Yes n.d. n.d. Enhances cell migration and proliferation May contribute to breast cancer Feigin et al., 2014  
KISS1R Yes n.d. n.d. Stimulates EGFR transactivation n.d. Cvetkovic et al., 2013  
LGR4 Yes n.d. GRD Increases canonical and non-canonical Wnt signaling n.d. Carmon et al., 2014  
LGR5 Yes n.d. GRD and C-terminus Reduces IQGAP1 phosphorylation; increases Rac1 and actin binding n.d. Carmon et al., 2017  
LPA1 Yes n.d. n.d. Increases cell migration and invasion n.d. Alemayehu et al., 2013  
M3-mAChR n.d. n.d. n.d. Increases active Rac1; may couple M3-mAChR to actin cytoskeleton n.d. Ruiz-Velasco et al., 2002  
MOR1 n.d. n.d. n.d. Stimulates Rac1 and ERK activation n.d. Civciristov et al., 2019  
Receptor serine/threonine kinases 
TGFβR2 Yes Yes aa 1503–1657 Promotes TGFβR2 degradation; inhibits TGFβR2 signaling May constrain liver and bladder tumor growth Liu et al., 2013  
Glutamate-gated ion channels 
AMPAR (GluR4) Yes n.d. N-terminal May regulate cell surface targeting of GluR4 May participate in cognitive physiology and pathology Nuriya et al., 2005  
NMDAR (NR2A, NR2B) Yes n.d. n.d. Promotes cell surface targeting of NR2A; stimulates ERK signaling Gao et al., 2011  
Adhesion receptors 
β1-integrin Yes n.d. n.d. Couples β1-integrin to Rac1, RhoA, and Arf6 GTPases n.d. Nakajima et al., 2005  
β3-integrin Yes Yes n.d. Promotes cortical actin arrangements Controls vascular barrier protection Bhattacharya et al., 2012  
CD44 Yes n.d. n.d. Links CD44 to the cytoskeleton and ERK signaling Increases ovarian tumor cell migration Bourguignon et al., 2005  
E-cadherin Yes Yes RGCT Dissociates adherens junctions n.d. Kuroda et al., 1998  
N-cadherin Yes n.d. n.d Stimulates ERK1/2 signaling; regulates cell-cell adhesion Participates in fear memory and spermatogenesis Lui et al., 2005  
VE-cadherin Yes n.d. n.d. Destabilizes adherens junctions n.d. Yamaoka-Tojo et al., 2006  
T cell receptors 
OX40 Yes n.d. C-terminal Restrains OX40 cosignaling May coordinate inflammation Okuyama et al., 2020  
TCR n.d. n.d. n.d. Negatively regulates TCR-mediated signaling Gorman et al., 2012  
Receptor protein tyrosine phosphatases 
PTPμ Yes Yes n.d. Regulates GTPase-dependent functions of IQGAP1 and neurite outgrowth n.d. Phillips-Mason et al., 2006  
IQGAP2 
DP1 n.d. n.d. n.d. Inhibits ERK n.d. Fréchette et al., 2021  
IFN-α receptor n.d. n.d. n.d. Activates NF-κB-mediated gene expression May have antiviral actions Brisac et al., 2016  
LGR4 Yes n.d. n.d. n.d. n.d. Carmon et al., 2014  
PAR n.d. n.d. n.d. Modulates cytoskeletal dynamics n.d. Schmidt et al., 2003  
VEGFR2 n.d. n.d. n.d. Stimulates VEGF production, which activates VEGFR2 signaling to Akt Increases angiogenesis in breast cancer Kumar et al., 2022  
IQGAP3 
DP1 n.d. n.d. n.d. Activates ERK n.d. Fréchette et al., 2021  
EGFR n.d. n.d. n.d. Stimulates EGFR activation and signaling to ERK n.d. Yang et al., 2014  
FGFR1 n.d. n.d. n.d. Activates ERK May coordinate embryonic development Fang et al., 2015  
LGR4 Yes n.d. n.d. Enhances RSPO/LGR4 signaling to Wnt/β-catenin n.d. Carmon et al., 2014  
NGFR n.d. n.d. n.d. Triggers formation of cell extensions n.d. Caro-Gonzalez et al., 2012  

Abbreviations: aa, amino acids; n.d., not determined.

a

Interaction in cells was demonstrated by co-immunoprecipitation or pull-down from cell lysates, or by colocalization or proximity ligation assay in intact cells.

b

Direct binding was demonstrated using pure proteins.

c

Only the initial publication is cited here.

d

Interaction was suggested from in silico molecular docking analysis only.

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