TABLE 1

Studies of receptor structure and function by construction of chimeric G-protein-coupled receptors

Donated Region Probe
Family Parent GPCR Donor GPCR NT TMS Loops CT Ligand Binding Downstream Signaling Receptor Internalization Reference
I α1-AR β2-AR + + Cotecchia et al. (1990)
I α1A-AR α1B-AR + + Chen et al. (1996)
I α1A-AR α1D-AR + + Hamaguchi et al. (1996)
I α1A-AR α1D-AR + + Hamaguchi et al. (1998)
I α1A-AR α1B-AR + + Vazquez-Prado et al. (2000)
I α1A-AR α1B-AR + + Lapinsh et al. (2001)
I α1A-AR α1D-AR + + + + Shinoura et al. (2002)
I α1B-AR β2-AR + + + + Cotecchia et al. (1992)
I α1B-AR α1A-AR + + + Zhao et al. (1996)
I α2-AR mAChR3 + + + + + + Maggio et al. (1993)
I α2-AR β2-AR + + + + + + Kobilka et al. (1988)
I α2A-AR β2-AR, 5-HT1A + + Eason and Liggett (1995)
I α2AAR β2-AR, 5-HT1A + + + + + Eason and Liggett (1996)
I α2A-AR β2-AR, 5-HT1A + + + + + Jewell-Motz et al. (1997)
I α2A-AR Adenosine A1 + + + + + + Saunders et al. (1998)
I α2A-AR β2-AR, 5-HT1A + + + + Jewell-Motz et al. (1998)
I α2A-AR α2C-AR + + + Jewell-Motz et al. (2000)
I β1-AR β2-AR + + + Frielle et al. (1988)
I β1-AR β2-AR + + + + Rousseau et al. (1996)
I β1-AR β2-AR + + + + Kikkawa et al. (1998)
I β1-AR β2-AR + + + + + + Shiina et al. (2000)
I β1-AR β2-AR + + + + + Sugimoto et al. (2002)
I β2-AR β1-AR + + Marullo et al. (1990)
I β2-AR β1-AR + + + Parker et al. (1995)
I β2-AR β1-AR + + + Green et al. (1996)
I β2-AR VR2 + + + + Oakley et al. (1999)
I β2-AR α2A-AR + + + Zhao et al. (1998)
I β2-AR Histamine H2 + + + + Wang et al. (2000)
I β2-AR Angiotensin II + + + Anborgh et al. (2000)
I β2-AR VR2 + + + Tohgo et al. (2003)
I β3-AR β2-AR + + + Nantel et al. (1993)
I β3-AR β2-AR + + + Liggett et al. (1993)
I β3-AR β2-AR + + + + + + Guan et al. (1995)
I β3-AR β2-AR + + + + Jockers et al. (1996)
I β3-AR β2-AR + + + Mostafapour et al. (1996)
I Angiotensin I Angiotensin II + + + + + Feng and Karnik (1999)
I Angiotensin II α1B-AR, β2-AR + + + + Conchon et al. (1997)
I FSH LH + + + Dias et al. (1994)
I FSH LH + + + Vischer et al. (2003)
I GnRH TSH + + + Heding et al. (1998)
I GnRH TSH + + + Hanyaloglu et al. (2001)
I 5-HT1B 5-HT2A + + Oksenberg et al. (1995)
I 5-HT1B 5-HT2D + + + Wurch et al. (1998)
I 5-HT1B 5-HT2E + + Parker et al. (1996)
I 5-HT2 5-HT1c + + + Choudhary et al. (1992)
I 5-HT2 Thrombin + + Vouret-Craviari et al. (1995)
I 5-HT2A 5-HT2C + + + + Alberts et al. (2003)
I 5-HT3A 5-HT3A + + Boyd et al. (2003)
I 5-HT3A 5-HT3B + + Kelley et al. (2003)
I LH FSH + + + Braun et al. (1991)
I LH FSH + + + Hirsch et al. (1996)
I LH FSH + + + Kudo et al. (1996)
I LH FSH + + + Osuga et al. (1997)
I mAChR1 mAChR2 + + + Kubo et al. (1988)
I mAChR1 β2-AR + + + Wong et al. (1990)
I mAChR1 mAChR2 + + + Lai et al. (1992)
I mAChR2 mAChR3 + + + Wess et al. (1989)
I mAChR2 mAChR3 + + Wess et al. (1990a)
I mAChR2 mAChR3 + + + + + Wess et al. (1990b)
I mAChR2 mAChR5 + + + Wess et al. (1992)
I mAChR2 mAChR5 + + Wess and Pittel (1994)
I mAChR3 mAChR2 + + Felder et al. (1992)
I mAChR3 α2C-AR + + + + + Maggio et al. (1999)
I mAChR3 mAChR2 + + + Bluml et al. (1994)
I Rhodopsin β2-AR + + Marin et al. (2000)
I Rhodopsin mGlu1/6 + + + Yamashita et al. (2001)
I Thrombin Substance P + + + Trejo et al. (1998)
I Thrombin Substance P + + + Sambrano and Coughlin (1999)
I Thrombin Substance P + + + Trejo and Coughlin (1999)
I TSH LH + + + + Nagayama et al. (1990)
I TSH LH + + + + Nagayama et al. (1991)
I TSH LH + + + + Nagayama et al. (1991)
I TSH LH + + + + Akamizu et al. (1993)
I TSH LH + + + + Nagayama et al. (1994)
II Glucagon Dopamine D4 + + + + Cypess et al. (1999)
II Dopamine D1 Dopamine D2 + + + MacKenzie et al. (1993)
II Dopamine D1 Dopamine D2 + + + + + Kozell et al. (1994)
II Dopamine D1 Dopamine D2 + + + + Kozell and Neve (1997)
II Dopamine D2 Dopamine D3 + + Robinson et al. (1994)
II Dopamine D2 Dopamine D3 + + + Robinson and Caron (1996)
II Dopamine D2 Dopamine D3 + + + Lachowicz and Sibley (1997)
II Dopamine D2 Dopamine D3 + + + Scarselli et al. (2001)
II Dopamine D2 Dopamine D3 + + Ilani et al. (2002)
II Dopamine D2 Dopamine D4 + + + Shih et al. (1997)
II Dopamine D2 mAChR1 + + + England et al. (1991)
II Dopamine D2 Thrombin + + Verrall et al. (1997)
II Dopamine D3 Dopamine D1 + + Alberts et al. (1998)
II Dopamine D3 Dopamine D2 + + + McAllister et al. (1993)
II Dopamine D3 Dopamine D2 + + + Van Leeuwen et al. (1995)
II Dopamine D4 Glucagon + + + Kazmi et al. (2000)
II VPAC1 VPAC2 + + + Juarranz et al. (1999)
II VPAC1 VPAC2 + + + Langer et al. (2002)
II VPAC2 PAC1 + + + McCulloch et al. (2000)
II VPAC2 PAC1 + + + McCulloch et al. (2001)
III mGluR1 mGluR3 + + Gomeza et al. (1996)
III Orphan Ca2+, mGluR1 + + + Brauner-Osborne et al. (2001)
III GABAB 1 GABAB 2 + + + Calver et al. (2001)
III GABAB 1 GABAB 2 + + + + + + Galvez et al. (2001)
III GABAB 2 mGluR1 + + Malitschek et al. (1999)
III GABAB 2 GABAB 1 + + + Margeta-Mitrovic et al. (2001)a
III GABAB 2 GABAB 1 + + + Margeta-Mitrovic et al. (2001)b
III GABAB 2 GABAB 1 + + + Robbins et al. (2001)
III GABAB 2 GABAB 1 + + + Havlickova et al. (2002)
III mGluR1 Ca2+ + + Hammerland et al. (1999)
III mGluR2 mGluR4/8 + + Havlickova et al. (2003)
III mGluR3 mGluR1c + + + + Pin et al. (1994)
III mGluR3 mGluR1 + + + Flor et al. (1996)
III VR1a VRR1 + + + + + Gupte et al. (2004)
V Fizzled-1 β2-AR + + + + + Liu et al. (2001)
V Fizzled-1 β2-AR + + + + + + DeCostanzo et al. (2002)
V Fizzled-1 β2-AR + + + + Li et al. (2004)
V Fizzled-2 β2-AR + + + + + Liu et al. (1999)
V Fizzled-2 β2-AR + + + + + Ahumada et al. (2002)
V Fizzled-2 β2-AR + + + + Ishitani et al. (2003)
V Fizzled-7 Fizzled-5 + + + + + Swain et al. (2001)

  • CT, C terminus; NT, N terminus; mAChR muscarinic acetylcholine receptor; GnRH, gonadotropin-releasing hormone; TSH, thyroid-stimulating hormone; mGluR, metabotropic glutamate receptor.