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Volumn 291, Issue 1, 2016, Pages 303-317

Non-equivalence of key positively charged residues of the free fatty acid 2 receptor in the recognition and function of agonist versus antagonist ligands

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATION ANALYSIS; AMINO ACIDS; ARGININE; BINS; CARBOXYLATION; DISEASES; FUNCTIONS; LIGANDS;

EID: 84952941040     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M115.687939     Document Type: Article
Times cited : (42)

References (53)
  • 2
    • 84914145315 scopus 로고    scopus 로고
    • From microbe to man: The role of microbial short chain fatty acid metabolites in host cell biology
    • Natarajan, N., and Pluznick, J. L. (2014) From microbe to man: the role of microbial short chain fatty acid metabolites in host cell biology. Am. J. Physiol. Cell Physiol. 307, C979-C985
    • (2014) Am. J. Physiol. Cell Physiol , vol.307 , pp. C979-C985
    • Natarajan, N.1    Pluznick, J.L.2
  • 4
    • 58149095589 scopus 로고    scopus 로고
    • International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1,-2, and -3: Pharmacology and pathophysiological functions
    • Stoddart, L. A., Smith, N. J., and Milligan, G. (2008) International Union of Pharmacology. LXXI. Free fatty acid receptors FFA1, -2, and -3: pharmacology and pathophysiological functions. Pharmacol. Rev. 60, 405-417
    • (2008) Pharmacol. Rev , vol.60 , pp. 405-417
    • Stoddart, L.A.1    Smith, N.J.2    Milligan, G.3
  • 5
    • 69249214021 scopus 로고    scopus 로고
    • Agonism and allosterism: The pharmacology of the free fatty acid receptors FFA2 and FFA3
    • Milligan, G., Stoddart, L. A., and Smith, N. J. (2009) Agonism and allosterism: the pharmacology of the free fatty acid receptors FFA2 and FFA3. Br. J. Pharmacol. 158, 146-153
    • (2009) Br. J. Pharmacol , vol.158 , pp. 146-153
    • Milligan, G.1    Stoddart, L.A.2    Smith, N.J.3
  • 6
    • 84873932325 scopus 로고    scopus 로고
    • Short chain fatty acids and their receptors: New metabolic targets
    • Layden, B. T., Angueira, A. R., Brodsky, M., Durai, V., and Lowe, W. L., Jr. (2013) Short chain fatty acids and their receptors: new metabolic targets. Transl. Res. 161, 131-140
    • (2013) Transl. Res , vol.161 , pp. 131-140
    • Layden, B.T.1    Angueira, A.R.2    Brodsky, M.3    Durai, V.4    Lowe, W.L.5
  • 7
    • 84901846320 scopus 로고    scopus 로고
    • G-proteincoupled receptors for free fatty acids: Nutritional and therapeutic targets
    • Milligan, G., Ulven, T., Murdoch, H., and Hudson, B. D. (2014) G-proteincoupled receptors for free fatty acids: nutritional and therapeutic targets. Br. J. Nutr. 111, S3-S7
    • (2014) Br. J. Nutr , vol.111 , pp. S3-S7
    • Milligan, G.1    Ulven, T.2    Murdoch, H.3    Hudson, B.D.4
  • 8
    • 77957055780 scopus 로고
    • Integrated methods for modeling G-protein coupled receptors
    • Ballesteros, J. A., and Weinstein, H. (1995) Integrated methods for modeling G-protein coupled receptors. Methods Neurosci. 25, 366-428
    • (1995) Methods Neurosci , vol.25 , pp. 366-428
    • Ballesteros, J.A.1    Weinstein, H.2
  • 9
    • 57749112018 scopus 로고    scopus 로고
    • Conserved polar residues in transmembrane domains V, VI, and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids
    • Stoddart, L. A., Smith, N. J., Jenkins, L., Brown, A. J., and Milligan, G. (2008) Conserved polar residues in transmembrane domains V, VI, and VII of free fatty acid receptor 2 and free fatty acid receptor 3 are required for the binding and function of short chain fatty acids. J. Biol. Chem. 283, 32913-32924
    • (2008) J. Biol. Chem , vol.283 , pp. 32913-32924
    • Stoddart, L.A.1    Smith, N.J.2    Jenkins, L.3    Brown, A.J.4    Milligan, G.5
  • 11
    • 79953216793 scopus 로고    scopus 로고
    • Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: Identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3
    • Schmidt, J., Smith, N. J., Christiansen, E., Tikhonova, I. G., Grundmann, M., Hudson, B. D., Ward, R. J., Drewke, C., Milligan, G., Kostenis, E., and Ulven, T. (2011) Selective orthosteric free fatty acid receptor 2 (FFA2) agonists: identification of the structural and chemical requirements for selective activation of FFA2 versus FFA3. J. Biol. Chem. 286, 10628-10640
    • (2011) J. Biol. Chem , vol.286 , pp. 10628-10640
    • Schmidt, J.1    Smith, N.J.2    Christiansen, E.3    Tikhonova, I.G.4    Grundmann, M.5    Hudson, B.D.6    Ward, R.J.7    Drewke, C.8    Milligan, G.9    Kostenis, E.10    Ulven, T.11
  • 13
    • 84870361150 scopus 로고    scopus 로고
    • Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3
    • Hudson, B. D., Tikhonova, I. G., Pandey, S. K., Ulven, T., and Milligan, G. (2012) Extracellular ionic locks determine variation in constitutive activity and ligand potency between species orthologs of the free fatty acid receptors FFA2 and FFA3. J. Biol. Chem. 287, 41195-41209
    • (2012) J. Biol. Chem , vol.287 , pp. 41195-41209
    • Hudson, B.D.1    Tikhonova, I.G.2    Pandey, S.K.3    Ulven, T.4    Milligan, G.5
  • 14
    • 84874395887 scopus 로고    scopus 로고
    • Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets
    • Ulven, T. (2012) Short-chain free fatty acid receptors FFA2/GPR43 and FFA3/GPR41 as new potential therapeutic targets. Front. Endocrinol. 3, 111
    • (2012) Front. Endocrinol , vol.3 , pp. 111
    • Ulven, T.1
  • 15
    • 84876712334 scopus 로고    scopus 로고
    • The therapeutic potential of allosteric ligands for free fatty acid-sensitive GPCRs
    • Hudson, B. D., Ulven, T., and Milligan, G. (2013) The therapeutic potential of allosteric ligands for free fatty acid-sensitive GPCRs. Curr. Top. Med. Chem. 13, 14-25
    • (2013) Curr. Top. Med. Chem , vol.13 , pp. 14-25
    • Hudson, B.D.1    Ulven, T.2    Milligan, G.3
  • 20
    • 84930629051 scopus 로고    scopus 로고
    • Oxalyl chloride as a practical carbon monoxide source for carbonylation reactions
    • Hansen, S. V., and Ulven, T. (2015) Oxalyl chloride as a practical carbon monoxide source for carbonylation reactions. Org. Lett. 17, 2832-2835
    • (2015) Org. Lett , vol.17 , pp. 2832-2835
    • Hansen, S.V.1    Ulven, T.2
  • 21
    • 80052811601 scopus 로고    scopus 로고
    • Using the Flp-InTM T-RexTM system to regulate GPCR expression
    • Ward, R. J., Alvarez-Curto, E., and Milligan, G. (2011) Using the Flp-InTM T-RexTM system to regulate GPCR expression. Methods Mol. Biol. 746, 21-37
    • (2011) Methods Mol. Biol , vol.746 , pp. 21-37
    • Ward, R.J.1    Alvarez-Curto, E.2    Milligan, G.3
  • 22
    • 84904512037 scopus 로고    scopus 로고
    • The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/ GPR120)
    • Hudson, B. D., Shimpukade, B., Milligan, G., and Ulven, T. (2014) The molecular basis of ligand interaction at free fatty acid receptor 4 (FFA4/ GPR120). J. Biol. Chem. 289, 20345-20358
    • (2014) J. Biol. Chem , vol.289 , pp. 20345-20358
    • Hudson, B.D.1    Shimpukade, B.2    Milligan, G.3    Ulven, T.4
  • 24
    • 80054811622 scopus 로고    scopus 로고
    • Heteromultimerization of cannabinoid CB(1) receptor and orexin OX(1) receptor generates a unique complex in which both protomers are regulated by orexin A
    • Ward, R. J., Pediani, J. D., and Milligan, G. (2011) Heteromultimerization of cannabinoid CB(1) receptor and orexin OX(1) receptor generates a unique complex in which both protomers are regulated by orexin A. J. Biol. Chem. 286, 37414-37428
    • (2011) J. Biol. Chem , vol.286 , pp. 37414-37428
    • Ward, R.J.1    Pediani, J.D.2    Milligan, G.3
  • 25
    • 77954917965 scopus 로고    scopus 로고
    • Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogeneous time-resolved FRET
    • Alvarez-Curto, E., Ward, R. J., Pediani, J. D., and Milligan, G. (2010) Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogeneous time-resolved FRET. J. Biol. Chem. 285, 23318-23330
    • (2010) J. Biol. Chem , vol.285 , pp. 23318-23330
    • Alvarez-Curto, E.1    Ward, R.J.2    Pediani, J.D.3    Milligan, G.4
  • 26
    • 0037305047 scopus 로고    scopus 로고
    • Principles: Extending the utility of [35S] GTPγS binding assays
    • Milligan, G. (2003) Principles: extending the utility of [35S]GTPγS binding assays. Trends Pharmacol. Sci. 24, 87-90
    • (2003) Trends Pharmacol. Sci , vol.24 , pp. 87-90
    • Milligan, G.1
  • 27
    • 67650392033 scopus 로고    scopus 로고
    • [35S] GTPγS binding in G protein-coupled receptor assays
    • Cooper, T., McMurchie, E. J., and Leifert, W. R. (2009) [35S]GTPγS binding in G protein-coupled receptor assays. Methods Mol. Biol. 552, 143-151
    • (2009) Methods Mol. Biol , vol.552 , pp. 143-151
    • Cooper, T.1    McMurchie, E.J.2    Leifert, W.R.3
  • 29
    • 33749358578 scopus 로고    scopus 로고
    • Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinicM3receptor
    • Dowling, M. R., and Charlton, S. J. (2006) Quantifying the association and dissociation rates of unlabelled antagonists at the muscarinicM3receptor. Br. J. Pharmacol. 148, 927-937
    • (2006) Br. J. Pharmacol , vol.148 , pp. 927-937
    • Dowling, M.R.1    Charlton, S.J.2
  • 30
    • 84859059730 scopus 로고    scopus 로고
    • Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists
    • Sykes, D. A., and Charlton, S. J. (2012) Slow receptor dissociation is not a key factor in the duration of action of inhaled long-acting β2-adrenoceptor agonists. Br. J. Pharmacol. 165, 2672-2683
    • (2012) Br. J. Pharmacol , vol.165 , pp. 2672-2683
    • Sykes, D.A.1    Charlton, S.J.2
  • 32
    • 74549125386 scopus 로고    scopus 로고
    • SeaView version 4: A multiplatform graphical user interface for sequence alignment and phylogenetic tree building
    • Gouy, M., Guindon, S., and Gascuel, O. (2010) SeaView version 4: a multiplatform graphical user interface for sequence alignment and phylogenetic tree building. Mol. Biol. Evol. 27, 221-224
    • (2010) Mol. Biol. Evol , vol.27 , pp. 221-224
    • Gouy, M.1    Guindon, S.2    Gascuel, O.3
  • 33
    • 79951476387 scopus 로고    scopus 로고
    • PROPKA3: Consistent treatment of internal and surface residues in empirical pKa predictions
    • Olsson, M. H., Søndergaard, C. R., Rostkowski, M., and Jensen, J. H. (2011) PROPKA3: consistent treatment of internal and surface residues in empirical pKa predictions. J. Chem. Theor. Comput. 7, 525-537
    • (2011) J. Chem. Theor. Comput , vol.7 , pp. 525-537
    • Olsson, M.H.1    Søndergaard, C.R.2    Rostkowski, M.3    Jensen, J.H.4
  • 34
    • 84930865710 scopus 로고    scopus 로고
    • Schrödinger Suite 2013-2 Protein Preparation Wizard 2013-2, Schrödinger, LLC, New York
    • Schrödinger Suite 2013-2 Protein Preparation Wizard 2013-2 (2013) Epik version 2.4, Schrödinger, LLC, New York
    • (2013) Epik Version 2.4
  • 36
    • 79960606839 scopus 로고    scopus 로고
    • A ligand's view of target similarity: Chemogenomic binding site-directed techniques for drug discovery
    • Garland, S. L., and Gloriam, D. E. (2011) A ligand's view of target similarity: chemogenomic binding site-directed techniques for drug discovery. Curr. Top. Med. Chem. 11, 1872-1881
    • (2011) Curr. Top. Med. Chem , vol.11 , pp. 1872-1881
    • Garland, S.L.1    Gloriam, D.E.2
  • 37
    • 84930868579 scopus 로고    scopus 로고
    • GPCR crystal structures: Medicinal chemistry in the pocket
    • Shonberg, J., Kling, R. C., Gmeiner, P., and Löber, S. (2015) GPCR crystal structures: medicinal chemistry in the pocket. Bioorg. Med. Chem. 23, 3880-3906
    • (2015) Bioorg. Med. Chem , vol.23 , pp. 3880-3906
    • Shonberg, J.1    Kling, R.C.2    Gmeiner, P.3    Löber, S.4
  • 38
    • 84934441026 scopus 로고    scopus 로고
    • From three-dimensional GPCR structure to rational ligand discovery
    • Kooistra, A. J., Leurs, R., de Esch, I. J., and de Graaf, C. (2014) From three-dimensional GPCR structure to rational ligand discovery. Adv. Exp. Med. Biol. 796, 129-157
    • (2014) Adv. Exp. Med. Biol , vol.796 , pp. 129-157
    • Kooistra, A.J.1    Leurs, R.2    De Esch, I.J.3    De Graaf, C.4
  • 39
    • 84871812592 scopus 로고    scopus 로고
    • GPCR activation: A mutagenic spotlight on crystal structures
    • Hulme, E. C. (2013) GPCR activation: a mutagenic spotlight on crystal structures. Trends Pharmacol. Sci. 34, 67-84
    • (2013) Trends Pharmacol. Sci , vol.34 , pp. 67-84
    • Hulme, E.C.1
  • 41
    • 84864541097 scopus 로고    scopus 로고
    • G protein-coupled receptors for energy metabolites as new therapeutic targets
    • Blad, C. C., Tang, C., and Offermanns, S. (2012) G protein-coupled receptors for energy metabolites as new therapeutic targets. Nat. Rev. Drug Discov. 11, 603-619
    • (2012) Nat. Rev. Drug Discov , vol.11 , pp. 603-619
    • Blad, C.C.1    Tang, C.2    Offermanns, S.3
  • 42
    • 80955180014 scopus 로고    scopus 로고
    • Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders
    • Hara, T., Hirasawa, A., Ichimura, A., Kimura, I., and Tsujimoto, G. (2011) Free fatty acid receptors FFAR1 and GPR120 as novel therapeutic targets for metabolic disorders. J. Pharm. Sci. 100, 3594-3601
    • (2011) J. Pharm. Sci , vol.100 , pp. 3594-3601
    • Hara, T.1    Hirasawa, A.2    Ichimura, A.3    Kimura, I.4    Tsujimoto, G.5
  • 43
    • 80052684905 scopus 로고    scopus 로고
    • Experimental challenges to targeting poorly characterized GPCRs: Uncovering the therapeutic potential for free fatty acid receptors
    • Hudson, B. D., Smith, N. J., and Milligan, G. (2011) Experimental challenges to targeting poorly characterized GPCRs: uncovering the therapeutic potential for free fatty acid receptors. Adv. Pharmacol. 62, 175-218
    • (2011) Adv. Pharmacol , vol.62 , pp. 175-218
    • Hudson, B.D.1    Smith, N.J.2    Milligan, G.3
  • 44
    • 84987837271 scopus 로고    scopus 로고
    • Treatment of type 2 diabetes by free fatty acid receptor agonists
    • Watterson, K. R., Hudson, B. D., Ulven, T., and Milligan, G. (2014) Treatment of type 2 diabetes by free fatty acid receptor agonists. Front. Endocrinol. 5, 137
    • (2014) Front. Endocrinol , vol.5 , pp. 137
    • Watterson, K.R.1    Hudson, B.D.2    Ulven, T.3    Milligan, G.4
  • 45
    • 84880620577 scopus 로고    scopus 로고
    • Short-chain fatty acids activate GPR41 and GPR43 on intestinal epithelial cells to promote inflammatory responses in mice
    • Kim, M. H., Kang, S. G., Park, J. H., Yanagisawa, M., and Kim, C. H. (2013) Short-chain fatty acids activate GPR41 and GPR43 on intestinal epithelial cells to promote inflammatory responses in mice. Gastroenterology 145, 396-406
    • (2013) Gastroenterology , vol.145 , pp. 396-406
    • Kim, M.H.1    Kang, S.G.2    Park, J.H.3    Yanagisawa, M.4    Kim, C.H.5
  • 46
    • 80054980812 scopus 로고    scopus 로고
    • Regulation of inflammation by short chain fatty acids
    • Vinolo, M. A., Rodrigues, H. G., Nachbar, R. T., and Curi, R. (2011) Regulation of inflammation by short chain fatty acids. Nutrients 3, 858-876
    • (2011) Nutrients , vol.3 , pp. 858-876
    • Vinolo, M.A.1    Rodrigues, H.G.2    Nachbar, R.T.3    Curi, R.4
  • 51
    • 84937760413 scopus 로고    scopus 로고
    • Tiotropium Respimat®: A review of its use in asthma poorly controlled with inhaled corticosteroids and long-acting β2-adrenergic agonists
    • McKeage, K. (2015) Tiotropium Respimat®: a review of its use in asthma poorly controlled with inhaled corticosteroids and long-acting β2-adrenergic agonists. Drugs 75, 809-816
    • (2015) Drugs , vol.75 , pp. 809-816
    • McKeage, K.1
  • 52
    • 84879925936 scopus 로고    scopus 로고
    • Molecular determinants of drug-receptor binding kinetics
    • Pan, A. C., Borhani, D. W., Dror, R. O., and Shaw, D. E. (2013) Molecular determinants of drug-receptor binding kinetics. Drug Discov. Today 18, 667-673
    • (2013) Drug Discov. Today , vol.18 , pp. 667-673
    • Pan, A.C.1    Borhani, D.W.2    Dror, R.O.3    Shaw, D.E.4
  • 53
    • 84876018174 scopus 로고    scopus 로고
    • GPR43/FFA2: Physiopathological relevance and therapeutic prospects
    • Bindels, L. B., Dewulf, E. M., and Delzenne, N. M. (2013) GPR43/FFA2: physiopathological relevance and therapeutic prospects. Trends Pharmacol. Sci. 34, 226-232
    • (2013) Trends Pharmacol. Sci , vol.34 , pp. 226-232
    • Bindels, L.B.1    Dewulf, E.M.2    Delzenne, N.M.3


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