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Volumn 26, Issue 2, 2014, Pages 149-155

Ghrelin and motilin receptor agonists: Time to introduce bias into drug design

Author keywords

Camicinal GSK962040; Constipation; Gastroparesis; Ghrelin; Motilin; Ulimorelin

Indexed keywords

CAMICINAL; GHRELIN; MOTILIN; MOTILIN RECEPTOR AGONIST; RQ 00201894; UNCLASSIFIED DRUG;

EID: 84892640469     PISSN: 13501925     EISSN: 13652982     Source Type: Journal    
DOI: 10.1111/nmo.12300     Document Type: Review
Times cited : (25)

References (52)
  • 1
    • 0033540056 scopus 로고    scopus 로고
    • Ghrelin is a growth-hormone-releasing acylated peptide from stomach
    • Kojima M, Hosoda H, Date Y, Nakazato M, Matsuo H, Kangawa K. Ghrelin is a growth-hormone-releasing acylated peptide from stomach. Nature 1999; 402: 656-60.
    • (1999) Nature , vol.402 , pp. 656-660
    • Kojima, M.1    Hosoda, H.2    Date, Y.3    Nakazato, M.4    Matsuo, H.5    Kangawa, K.6
  • 2
    • 15544385058 scopus 로고    scopus 로고
    • Ghrelin: structure and function
    • Kojima M, Kangawa K. Ghrelin: structure and function. Physiol Rev 2005; 85: 495-522.
    • (2005) Physiol Rev , vol.85 , pp. 495-522
    • Kojima, M.1    Kangawa, K.2
  • 5
    • 84884988766 scopus 로고    scopus 로고
    • The TZP-102 Phase 2b Study Group. Phase 2b, randomized, double-blind 12-week studies of TZP-102, a ghrelin receptor agonist for diabetic gastroparesis
    • McCallum RW, Lembo A, Esfandyari T, Bhandari BR, Ejskjaer N, Cosentino C, Helton N, Mondou E et al. The TZP-102 Phase 2b Study Group. Phase 2b, randomized, double-blind 12-week studies of TZP-102, a ghrelin receptor agonist for diabetic gastroparesis. Neurogastroenterol Motil 2013; 25: e705-17.
    • (2013) Neurogastroenterol Motil , vol.25
    • McCallum, R.W.1    Lembo, A.2    Esfandyari, T.3    Bhandari, B.R.4    Ejskjaer, N.5    Cosentino, C.6    Helton, N.7    Mondou, E.8
  • 8
    • 33748916666 scopus 로고    scopus 로고
    • Evidence that stimulation of ghrelin receptors in the spinal cord initiates propulsive activity in the colon of the rat
    • 576.1
    • Shimizu Y, Chang EC, Shafton AD, Sanger GJ, Witherington J, Furness JB. Evidence that stimulation of ghrelin receptors in the spinal cord initiates propulsive activity in the colon of the rat. J Physiol 2006; 576.1: 329-38.
    • (2006) J Physiol , pp. 329-338
    • Shimizu, Y.1    Chang, E.C.2    Shafton, A.D.3    Sanger, G.J.4    Witherington, J.5    Furness, J.B.6
  • 9
    • 77951884103 scopus 로고    scopus 로고
    • Functional and in situ hybridisation evidence that preganglionic sympathetic vasoconstrictor neurons express ghrelin receptors
    • Ferens DM, Yin L, Bron R, Hunne B, Ohashi-Doi K, Kitchener PD, Sanger GJ, Witherington J et al. Functional and in situ hybridisation evidence that preganglionic sympathetic vasoconstrictor neurons express ghrelin receptors. Neuroscience 2010; 166: 671-9.
    • (2010) Neuroscience , vol.166 , pp. 671-679
    • Ferens, D.M.1    Yin, L.2    Bron, R.3    Hunne, B.4    Ohashi-Doi, K.5    Kitchener, P.D.6    Sanger, G.J.7    Witherington, J.8
  • 10
    • 0344010043 scopus 로고    scopus 로고
    • The rabbit motilin receptor: molecular characterisation and pharmacology
    • Dass NB, Hill J, Muir A, Testa T, Wise A, Sanger GJ. The rabbit motilin receptor: molecular characterisation and pharmacology. Br J Pharmacol 2003; 140: 948-54.
    • (2003) Br J Pharmacol , vol.140 , pp. 948-954
    • Dass, N.B.1    Hill, J.2    Muir, A.3    Testa, T.4    Wise, A.5    Sanger, G.J.6
  • 11
    • 84866972210 scopus 로고    scopus 로고
    • Regional- and agonist-dependent facilitation of human neurogastrointestinal functions by motilin receptor agonists
    • Broad J, Mukherjee S, Samadi M, Martin JE, Dukes GE, Sanger GJ. Regional- and agonist-dependent facilitation of human neurogastrointestinal functions by motilin receptor agonists. Br J Pharmacol 2012; 167: 763-74.
    • (2012) Br J Pharmacol , vol.167 , pp. 763-774
    • Broad, J.1    Mukherjee, S.2    Samadi, M.3    Martin, J.E.4    Dukes, G.E.5    Sanger, G.J.6
  • 13
    • 79959778996 scopus 로고    scopus 로고
    • The translational value of rodent gastrointestinal functions: a cautionary tale
    • Sanger GJ, Holbrook JD, Andrews PLR. The translational value of rodent gastrointestinal functions: a cautionary tale. Trends Pharmacol Sci 2011; 32: 402-9.
    • (2011) Trends Pharmacol Sci , vol.32 , pp. 402-409
    • Sanger, G.J.1    Holbrook, J.D.2    Andrews, P.L.R.3
  • 14
    • 40649105561 scopus 로고    scopus 로고
    • Motilin, ghrelin and related neuropeptides as targets for the treatment of GI diseases
    • Sanger GJ. Motilin, ghrelin and related neuropeptides as targets for the treatment of GI diseases. Drug Discov Today 2008; 13: 234-9.
    • (2008) Drug Discov Today , vol.13 , pp. 234-239
    • Sanger, G.J.1
  • 16
    • 84885470949 scopus 로고    scopus 로고
    • Motilin: toward a new understanding of the gastrointestinal neuropharmacology and therapeutic use of motilin receptor agonists
    • Sanger GJ, Wang Y-T, Hobson A, Broad J. Motilin: toward a new understanding of the gastrointestinal neuropharmacology and therapeutic use of motilin receptor agonists. Br J Pharmacol 2013; 170: 1349-62.
    • (2013) Br J Pharmacol , vol.170 , pp. 1349-1362
    • Sanger, G.J.1    Wang, Y.-T.2    Hobson, A.3    Broad, J.4
  • 18
    • 81355156238 scopus 로고    scopus 로고
    • Guide to receptors and channels (GRAC), 5th edn
    • Alexander SPH, Mathie A, Peters JA. Guide to receptors and channels (GRAC), 5th edn. Br J Pharmacol 2011; 164(Suppl. 1): S1-324.
    • (2011) Br J Pharmacol , vol.164 , Issue.SUPPL. 1
    • Alexander, S.P.H.1    Mathie, A.2    Peters, J.A.3
  • 19
    • 79960033349 scopus 로고    scopus 로고
    • The identification and rationale for drugs which act at the motilin receptor
    • Westaway SM, Sanger GJ. The identification and rationale for drugs which act at the motilin receptor. Prog Med Chem 2009; 48: 31-80.
    • (2009) Prog Med Chem , vol.48 , pp. 31-80
    • Westaway, S.M.1    Sanger, G.J.2
  • 20
    • 84875465813 scopus 로고    scopus 로고
    • The antibiotic azithromycin is a motilin receptor agonist in human stomach: comparison with erythromycin
    • Broad J, Sanger GJ. The antibiotic azithromycin is a motilin receptor agonist in human stomach: comparison with erythromycin. Br J Pharmacol 2013; 168: 1859-67.
    • (2013) Br J Pharmacol , vol.168 , pp. 1859-1867
    • Broad, J.1    Sanger, G.J.2
  • 21
    • 84871924869 scopus 로고    scopus 로고
    • Critical residues in the transmembrane helical bundle domains of the human motilin receptor for erythromycin binding and activity
    • Utsunomiya S, Matsuura B, Ueda T, Miyake T, Furukawa S, Kumagi T, Ikeda Y, Abe M et al. Critical residues in the transmembrane helical bundle domains of the human motilin receptor for erythromycin binding and activity. Regul Pept 2013; 180: 17-25.
    • (2013) Regul Pept , vol.180 , pp. 17-25
    • Utsunomiya, S.1    Matsuura, B.2    Ueda, T.3    Miyake, T.4    Furukawa, S.5    Kumagi, T.6    Ikeda, Y.7    Abe, M.8
  • 22
    • 33845196470 scopus 로고    scopus 로고
    • Delineation of the motilin domain involved in desensitization and internalization of the motilin receptor by using full and partial agonists
    • Mitselos A, Depoortere I, Peeters TL. Delineation of the motilin domain involved in desensitization and internalization of the motilin receptor by using full and partial agonists. Biochem Pharmacol 2007; 73: 115-24.
    • (2007) Biochem Pharmacol , vol.73 , pp. 115-124
    • Mitselos, A.1    Depoortere, I.2    Peeters, T.L.3
  • 23
    • 78751498756 scopus 로고    scopus 로고
    • Perspectives in pharmacology: functional selectivity and biased receptor signalling
    • Kenakin TP. Perspectives in pharmacology: functional selectivity and biased receptor signalling. J Pharmacol Exp Ther 2011; 336: 296-302.
    • (2011) J Pharmacol Exp Ther , vol.336 , pp. 296-302
    • Kenakin, T.P.1
  • 24
    • 33847153056 scopus 로고    scopus 로고
    • Differences between the abilities of tegaserod and motilin receptor agonists to stimulate gastric motility in vitro
    • Jarvie EM, North Laidler V, Corcoran S, Bassil A, Sanger GJ. Differences between the abilities of tegaserod and motilin receptor agonists to stimulate gastric motility in vitro. Br J Pharmacol 2007; 150: 455-62.
    • (2007) Br J Pharmacol , vol.150 , pp. 455-462
    • Jarvie, E.M.1    North Laidler, V.2    Corcoran, S.3    Bassil, A.4    Sanger, G.J.5
  • 25
    • 0034873597 scopus 로고    scopus 로고
    • What comes after macrolides and other motilin stimulants?
    • Tack J, Peeters T. What comes after macrolides and other motilin stimulants? Gut 2001; 49: 317-8.
    • (2001) Gut , vol.49 , pp. 317-318
    • Tack, J.1    Peeters, T.2
  • 26
    • 0027497367 scopus 로고
    • The treatment of idiopathic and diabetic gastroparesis with acute intravenous and chronic oral erythromycin
    • Richards RD, Davenport K, McCallum RW. The treatment of idiopathic and diabetic gastroparesis with acute intravenous and chronic oral erythromycin. Am J Gastroenterol 1993; 88: 203-7.
    • (1993) Am J Gastroenterol , vol.88 , pp. 203-207
    • Richards, R.D.1    Davenport, K.2    McCallum, R.W.3
  • 27
    • 0037224416 scopus 로고    scopus 로고
    • Erythromycin accelerates gastric emptying in a dose-response manner in healthy subjects
    • Boivin MA, Carey MC, Levy H. Erythromycin accelerates gastric emptying in a dose-response manner in healthy subjects. Pharmacotherapy 2003; 23: 5-8.
    • (2003) Pharmacotherapy , vol.23 , pp. 5-8
    • Boivin, M.A.1    Carey, M.C.2    Levy, H.3
  • 28
    • 84865487434 scopus 로고    scopus 로고
    • Abnormal initiation and conduction of slow-wave activity in gastroparesis, defined by high-resolution electrical mapping
    • O'Grady G, Angeli TR, Du P, Lahr C, Lammers WJ, Windsor JA, Abell TL, Farrugia G et al. Abnormal initiation and conduction of slow-wave activity in gastroparesis, defined by high-resolution electrical mapping. Gastroenterol 2012; 143: 589-98.
    • (2012) Gastroenterol , vol.143 , pp. 589-598
    • O'Grady, G.1    Angeli, T.R.2    Du, P.3    Lahr, C.4    Lammers, W.J.5    Windsor, J.A.6    Abell, T.L.7    Farrugia, G.8
  • 31
    • 84887814896 scopus 로고    scopus 로고
    • Functionally biased signaling properties of 7TM receptors - Opportunities for drug development for the ghrelin receptor
    • Sivertsen B, Holliday N, Madsen AN, Holst B. Functionally biased signaling properties of 7TM receptors - Opportunities for drug development for the ghrelin receptor. Br J Pharmacol 2013; 170: 1349-62.
    • (2013) Br J Pharmacol , vol.170 , pp. 1349-1362
    • Sivertsen, B.1    Holliday, N.2    Madsen, A.N.3    Holst, B.4
  • 32
    • 0038031634 scopus 로고    scopus 로고
    • Growth hormone secretagogue receptor expression in the cells of the stomach-projected afferent nerve in the rat nodose ganglion
    • Sakata I, Yamazaki M, Inoue K, Hayashi Y, Kangawa K, Sakai T. Growth hormone secretagogue receptor expression in the cells of the stomach-projected afferent nerve in the rat nodose ganglion. Neurosci Lett 2003; 342: 183-6.
    • (2003) Neurosci Lett , vol.342 , pp. 183-186
    • Sakata, I.1    Yamazaki, M.2    Inoue, K.3    Hayashi, Y.4    Kangawa, K.5    Sakai, T.6
  • 33
    • 10644280945 scopus 로고    scopus 로고
    • Ghrelin enhances gastric motility through direct stimulation of intrinsic neural pathways and capsaicin-sensitive afferent neurones in rats
    • Fukuda H, Mizuta Y, Isomoto H, Takeshima F, Ohnita K, Ohba K, Omagari K, Taniyama K et al. Ghrelin enhances gastric motility through direct stimulation of intrinsic neural pathways and capsaicin-sensitive afferent neurones in rats. Scand J Gastroenterol 2004; 12: 1209-14.
    • (2004) Scand J Gastroenterol , vol.12 , pp. 1209-1214
    • Fukuda, H.1    Mizuta, Y.2    Isomoto, H.3    Takeshima, F.4    Ohnita, K.5    Ohba, K.6    Omagari, K.7    Taniyama, K.8
  • 37
    • 80053919039 scopus 로고    scopus 로고
    • Elevated serum ghrelin levels in adult patients with cyclic vomiting syndrome
    • Hejazi RA, Lavenbarg TH, McCallum RW. Elevated serum ghrelin levels in adult patients with cyclic vomiting syndrome. Am J Gastroenterol 2011; 106: 1858-9.
    • (2011) Am J Gastroenterol , vol.106 , pp. 1858-1859
    • Hejazi, R.A.1    Lavenbarg, T.H.2    McCallum, R.W.3
  • 40
    • 84865621644 scopus 로고    scopus 로고
    • Effects of ghrelin administration during chemotherapy with advanced esophageal cancer patients: a prospective, randomized, placebo-controlled phase 2 study
    • Hiura Y, Takiguchi S, Yamamoto K, Takahashi T, Kurokawa Y, Yamasaki M, Nakajima K, Miyata H et al. Effects of ghrelin administration during chemotherapy with advanced esophageal cancer patients: a prospective, randomized, placebo-controlled phase 2 study. Cancer 2012; 118: 4785-94.
    • (2012) Cancer , vol.118 , pp. 4785-4794
    • Hiura, Y.1    Takiguchi, S.2    Yamamoto, K.3    Takahashi, T.4    Kurokawa, Y.5    Yamasaki, M.6    Nakajima, K.7    Miyata, H.8
  • 41
    • 77956316577 scopus 로고    scopus 로고
    • Safety and efficacy of ghrelin agonist TZP-101 in relieving symptoms in patients with diabetic gastroparesis: a randomized, placebo-controlled study
    • Ejskjaer N, Dimcevski G, Wo J, Hellström PM, Gormsen LC, Sarosiek I, Søfteland E, Nowak T et al. Safety and efficacy of ghrelin agonist TZP-101 in relieving symptoms in patients with diabetic gastroparesis: a randomized, placebo-controlled study. Neurogastroenterol Motil 2010; 22: 1069-81.
    • (2010) Neurogastroenterol Motil , vol.22 , pp. 1069-1081
    • Ejskjaer, N.1    Dimcevski, G.2    Wo, J.3    Hellström, P.M.4    Gormsen, L.C.5    Sarosiek, I.6    Søfteland, E.7    Nowak, T.8
  • 43
    • 84865958749 scopus 로고    scopus 로고
    • Safety/tolerability, pharmacokinetics (PK), and effect on gastric emptying(GE) with 14-days repeat oral dosing of the motilin receptor agonist, GSK962040, in healthy male and female volunteers
    • Dukes GE, Barton M, Dewit O, Stephens K, Vasist L, Young M, Richards D, Alpers D et al. Safety/tolerability, pharmacokinetics (PK), and effect on gastric emptying(GE) with 14-days repeat oral dosing of the motilin receptor agonist, GSK962040, in healthy male and female volunteers. Neurogastroenterol Motil 2010; 22(S1): 14-5.
    • (2010) Neurogastroenterol Motil , vol.22 , Issue.S1 , pp. 14-15
    • Dukes, G.E.1    Barton, M.2    Dewit, O.3    Stephens, K.4    Vasist, L.5    Young, M.6    Richards, D.7    Alpers, D.8
  • 44
    • 84862503973 scopus 로고    scopus 로고
    • A double-blind, randomized placebo-controlled phase II study of the pharmacokinetics of single doses of the motilin agonist GSK962040, in patients with type I diabetes mellitus (TIDM) and gastroparesis
    • Hellstrom PM, Tack JF, Stephens KE, Barton ME, Vasist LS, Richards DB, Williams PM, Alpers DH et al. A double-blind, randomized placebo-controlled phase II study of the pharmacokinetics of single doses of the motilin agonist GSK962040, in patients with type I diabetes mellitus (TIDM) and gastroparesis. Gastroenterol 2011; 140: S183.
    • (2011) Gastroenterol , vol.140
    • Hellstrom, P.M.1    Tack, J.F.2    Stephens, K.E.3    Barton, M.E.4    Vasist, L.S.5    Richards, D.B.6    Williams, P.M.7    Alpers, D.H.8
  • 45
    • 84873407879 scopus 로고    scopus 로고
    • The effect of GSK962040, a selective motilin agonist, on gastric emptying in critically ill patients with enteral feed intolerance
    • Chapman M, Fraser R, Nguyen N, Deane A, O'Connor S, Richards D, Hacquoil K, Vasist L et al. The effect of GSK962040, a selective motilin agonist, on gastric emptying in critically ill patients with enteral feed intolerance. Crit Care Med 2011; 39: 195.
    • (2011) Crit Care Med , vol.39 , pp. 195
    • Chapman, M.1    Fraser, R.2    Nguyen, N.3    Deane, A.4    O'Connor, S.5    Richards, D.6    Hacquoil, K.7    Vasist, L.8
  • 46
    • 84865983560 scopus 로고    scopus 로고
    • Characterization of a novel, potent, and selective small molecule motilin receptor agonist, RQ-00201894
    • Takahashi N, Koba N, Yamamoto T, Sudo M. Characterization of a novel, potent, and selective small molecule motilin receptor agonist, RQ-00201894. Gastroenterol 2010; 138(Suppl 1): S-713.
    • (2010) Gastroenterol , vol.138 , Issue.SUPPL 1
    • Takahashi, N.1    Koba, N.2    Yamamoto, T.3    Sudo, M.4
  • 47
    • 84884983158 scopus 로고    scopus 로고
    • A ghrelin agonist fails to show benefit in patients with diabetic gastroparesis: let's not throw the baby out with the bath water
    • Camilleri M, Acosta A. A ghrelin agonist fails to show benefit in patients with diabetic gastroparesis: let's not throw the baby out with the bath water. Neurogastroenterol Motil 2013; 25: 859-63.
    • (2013) Neurogastroenterol Motil , vol.25 , pp. 859-863
    • Camilleri, M.1    Acosta, A.2
  • 48
    • 38849092560 scopus 로고    scopus 로고
    • Development of drugs for gastrointestinal motor disorders: translating science to clinical need
    • Sanger GJ, Alpers D. Development of drugs for gastrointestinal motor disorders: translating science to clinical need. Neurogastroenterol Motil 2008; 20: 177-84.
    • (2008) Neurogastroenterol Motil , vol.20 , pp. 177-184
    • Sanger, G.J.1    Alpers, D.2
  • 50
    • 0033016280 scopus 로고    scopus 로고
    • Intestinal pseudo-obstruction
    • Coulie B, Camilleri M. Intestinal pseudo-obstruction. Annu Rev Med 1999; 50: 37-55.
    • (1999) Annu Rev Med , vol.50 , pp. 37-55
    • Coulie, B.1    Camilleri, M.2
  • 51
    • 84886800214 scopus 로고    scopus 로고
    • Cholinergic interactions between donepezil and prucalopride in human colon: potential to treat severe intestinal dysmotility
    • Broad J, Kung VW, Boundouki G, Aziz Q, De Maeyer JH, Knowles CH, Sanger GJ. Cholinergic interactions between donepezil and prucalopride in human colon: potential to treat severe intestinal dysmotility. Br J Pharmacol 2013; 170: 1253-61.
    • (2013) Br J Pharmacol , vol.170 , pp. 1253-1261
    • Broad, J.1    Kung, V.W.2    Boundouki, G.3    Aziz, Q.4    De, M.J.5    Knowles, C.H.6    Sanger, G.J.7
  • 52
    • 34447530948 scopus 로고    scopus 로고
    • Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism
    • Holst B, Mokrosinski J, Lang M, Brandt E, Nygaard R, Frimurer TM, Beck-Sickinger AG, Schwartz TW. Identification of an efficacy switch region in the ghrelin receptor responsible for interchange between agonism and inverse agonism. J Biol Chem 2007; 282: 15799-811.
    • (2007) J Biol Chem , vol.282 , pp. 15799-15811
    • Holst, B.1    Mokrosinski, J.2    Lang, M.3    Brandt, E.4    Nygaard, R.5    Frimurer, T.M.6    Beck-Sickinger, A.G.7    Schwartz, T.W.8


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