메뉴 건너뛰기




Volumn 4, Issue 6, 2016, Pages

A selective GPR40 (FFAR1) agonist LY2881835 provides immediate and durable glucose control in rodent models of type 2 diabetes

Author keywords

FFAR1; GPCR; GPR40; hyperglycemia; insulin; type 2 diabetes

Indexed keywords

ANTIDIABETIC AGENT; BETA ARRESTIN; G PROTEIN COUPLED RECEPTOR 40; LY2881835; STREPTOZOCIN; UNCLASSIFIED DRUG;

EID: 85026612809     PISSN: None     EISSN: 20521707     Source Type: Journal    
DOI: 10.1002/prp2.278     Document Type: Article
Times cited : (19)

References (23)
  • 1
    • 70350561694 scopus 로고    scopus 로고
    • Deletion of GPR40 impairs glucose-induced insulin secretion in vivo in mice without affecting intracellular fuel metabolism in islets
    • Alquier T, Peyot ML, Latour MG, Kebede M, Sorensen CM, et al. (2009). Deletion of GPR40 impairs glucose-induced insulin secretion in vivo in mice without affecting intracellular fuel metabolism in islets. Diabetes 58: 2607–2615.
    • (2009) Diabetes , vol.58 , pp. 2607-2615
    • Alquier, T.1    Peyot, M.L.2    Latour, M.G.3    Kebede, M.4    Sorensen, C.M.5
  • 2
    • 84857032603 scopus 로고    scopus 로고
    • GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes
    • Araki T, Hirayama M, Hiroi S, Kaku K (2012). GPR40-induced insulin secretion by the novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Diabetes Obes Metab 14: 271–278.
    • (2012) Diabetes Obes Metab , vol.14 , pp. 271-278
    • Araki, T.1    Hirayama, M.2    Hiroi, S.3    Kaku, K.4
  • 3
    • 0037838892 scopus 로고    scopus 로고
    • The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids
    • Briscoe C, Tadayyon M, Andrews J, Benson W, Chambers J, Eilert M, et al. (2003). The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem 278: 11303–11311.
    • (2003) J Biol Chem , vol.278 , pp. 11303-11311
    • Briscoe, C.1    Tadayyon, M.2    Andrews, J.3    Benson, W.4    Chambers, J.5    Eilert, M.6
  • 4
    • 33745607930 scopus 로고    scopus 로고
    • Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules
    • Briscoe C, Peat A, McKeown S, Corbett D, Goetz A, Littleton T, et al. (2006). Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol 148: 619–628.
    • (2006) Br J Pharmacol , vol.148 , pp. 619-628
    • Briscoe, C.1    Peat, A.2    McKeown, S.3    Corbett, D.4    Goetz, A.5    Littleton, T.6
  • 5
    • 11844275233 scopus 로고    scopus 로고
    • A family of fatty acid binding receptors
    • Brown A, Jupe S, Briscoe C (2005). A family of fatty acid binding receptors. DNA Cell Biol 24: 54–61.
    • (2005) DNA Cell Biol , vol.24 , pp. 54-61
    • Brown, A.1    Jupe, S.2    Briscoe, C.3
  • 6
    • 84866357145 scopus 로고    scopus 로고
    • Discovery of AM-1638: a potent and orally bioavailable GPR40/FFA1 full agonist ACS Med
    • Brown S, Dransfield P, Vimolratana M, Jiao X, Zhu L, Pattaropong V, et al. (2012). Discovery of AM-1638: a potent and orally bioavailable GPR40/FFA1 full agonist ACS Med. Chem Lett 3: 726–730.
    • (2012) Chem Lett , vol.3 , pp. 726-730
    • Brown, S.1    Dransfield, P.2    Vimolratana, M.3    Jiao, X.4    Zhu, L.5    Pattaropong, V.6
  • 7
    • 84859625938 scopus 로고    scopus 로고
    • TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomized, double-blind, placebo controlled trial
    • Burant C, Viswanathan P, Marcinak J, Cao C, Vakilynejad M, Xie B, et al. (2012). TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomized, double-blind, placebo controlled trial. Lancet 379: 1403–1411.
    • (2012) Lancet , vol.379 , pp. 1403-1411
    • Burant, C.1    Viswanathan, P.2    Marcinak, J.3    Cao, C.4    Vakilynejad, M.5    Xie, B.6
  • 8
    • 56749163623 scopus 로고    scopus 로고
    • Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes
    • Christiansen E, Urban C, Merten N, Liebscher K, Karlsen KK, Hamacher A, et al. (2008). Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. J Med Chem 51: 7061–7064.
    • (2008) J Med Chem , vol.51 , pp. 7061-7064
    • Christiansen, E.1    Urban, C.2    Merten, N.3    Liebscher, K.4    Karlsen, K.K.5    Hamacher, A.6
  • 9
    • 52749098923 scopus 로고    scopus 로고
    • Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion
    • Edfalk S, Steneberg P, Edlund H (2008). Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion. Diabetes 57: 2280–2287.
    • (2008) Diabetes , vol.57 , pp. 2280-2287
    • Edfalk, S.1    Steneberg, P.2    Edlund, H.3
  • 10
    • 30944467752 scopus 로고    scopus 로고
    • Reduction in voltage-gated K+ currents in primary cultured rat pancreatic beta-cells by linoleic acids
    • Feng D, Luo Z, Roh S, Hernandez M, Tawadros N, et al. (2006). Reduction in voltage-gated K+ currents in primary cultured rat pancreatic beta-cells by linoleic acids. Endocrinology 147: 674–682.
    • (2006) Endocrinology , vol.147 , pp. 674-682
    • Feng, D.1    Luo, Z.2    Roh, S.3    Hernandez, M.4    Tawadros, N.5
  • 12
    • 0037434991 scopus 로고    scopus 로고
    • Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40
    • Itoh Y, Kawamata Y, Harada M, Kobayashi M, Fujii R, Fukusumi S, et al. (2003). Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature 422: 173–176.
    • (2003) Nature , vol.422 , pp. 173-176
    • Itoh, Y.1    Kawamata, Y.2    Harada, M.3    Kobayashi, M.4    Fujii, R.5    Fukusumi, S.6
  • 13
    • 80555154306 scopus 로고    scopus 로고
    • AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents
    • Lin D, Zhang J, Zhuang R, Li F, Nguyen K, Chen M, et al. (2011). AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS ONE 6: e27270.
    • (2011) PLoS ONE , vol.6
    • Lin, D.1    Zhang, J.2    Zhuang, R.3    Li, F.4    Nguyen, K.5    Chen, M.6
  • 14
    • 84655170245 scopus 로고    scopus 로고
    • Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system
    • Nakamoto K, Nishinaka T, Matsumoto K, Kasuya F, Mankura M, Koyama Y, et al. (2012). Involvement of the long-chain fatty acid receptor GPR40 as a novel pain regulatory system. Brain Res 1432: 74–83.
    • (2012) Brain Res , vol.1432 , pp. 74-83
    • Nakamoto, K.1    Nishinaka, T.2    Matsumoto, K.3    Kasuya, F.4    Mankura, M.5    Koyama, Y.6
  • 15
    • 13844266013 scopus 로고    scopus 로고
    • GPR40 gene Arg211His polymorphism may contribute to the variation of insulin secretory capacity in Japanese men
    • Ogawa T, Hirose H, Miyashita K, Saito I, Saruta T (2005). GPR40 gene Arg211His polymorphism may contribute to the variation of insulin secretory capacity in Japanese men. Metab, Clin Exp 54: 296–299.
    • (2005) Metab, Clin Exp , vol.54 , pp. 296-299
    • Ogawa, T.1    Hirose, H.2    Miyashita, K.3    Saito, I.4    Saruta, T.5
  • 16
    • 0030748260 scopus 로고    scopus 로고
    • Signal transduction mechanisms in nutrient-induced insulin secretion
    • Prentki M, Tornheim K, Corkey B (1997). Signal transduction mechanisms in nutrient-induced insulin secretion. Diabetologia 40: S32–S41.
    • (1997) Diabetologia , vol.40 , pp. S32-S41
    • Prentki, M.1    Tornheim, K.2    Corkey, B.3
  • 17
    • 50949128408 scopus 로고    scopus 로고
    • Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice
    • Tan C, Feng Y, Zhou Y, Eiermann G, Petrov A, Zhou C, et al. (2008). Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice. Diabetes 57: 2211–2219.
    • (2008) Diabetes , vol.57 , pp. 2211-2219
    • Tan, C.1    Feng, Y.2    Zhou, Y.3    Eiermann, G.4    Petrov, A.5    Zhou, C.6
  • 18
    • 84882313066 scopus 로고    scopus 로고
    • Chronic treatment with Novel GPR40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion
    • Tanaka H, Yoshida S, Oshima H, Minoura H, Negoro K, Yamazaki T, et al. (2013). Chronic treatment with Novel GPR40 agonists improve whole-body glucose metabolism based on the glucose-dependent insulin secretion. J Pharmacol Exp Ther 346: 443–452.
    • (2013) J Pharmacol Exp Ther , vol.346 , pp. 443-452
    • Tanaka, H.1    Yoshida, S.2    Oshima, H.3    Minoura, H.4    Negoro, K.5    Yamazaki, T.6
  • 19
    • 33646395425 scopus 로고    scopus 로고
    • Expression of the gene for a membrane-bound fatty acid receptor in the pancreas and islet cell tumours in humans: evidence for GPR40 expression in pancreatic beta cells and implications for insulin secretion
    • Tomita T, Masuzaki H, Iwakura H, Fujikura J, Noguchi M, Tanaka T, et al. (2006). Expression of the gene for a membrane-bound fatty acid receptor in the pancreas and islet cell tumours in humans: evidence for GPR40 expression in pancreatic beta cells and implications for insulin secretion. Diabetologia 49: 962–968.
    • (2006) Diabetologia , vol.49 , pp. 962-968
    • Tomita, T.1    Masuzaki, H.2    Iwakura, H.3    Fujikura, J.4    Noguchi, M.5    Tanaka, T.6
  • 20
    • 80053138180 scopus 로고    scopus 로고
    • TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats
    • Tsujihata Y, Ito R, Suzuki M, Harada A, Negoro N, Yasuma T, et al. (2011). TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther 339: 228–237.
    • (2011) J Pharmacol Exp Ther , vol.339 , pp. 228-237
    • Tsujihata, Y.1    Ito, R.2    Suzuki, M.3    Harada, A.4    Negoro, N.5    Yasuma, T.6
  • 21
    • 51649104136 scopus 로고    scopus 로고
    • Loss-of-function mutation of the GPR40 gene associates with abnormal stimulated insulin secretion by acting on intracellular calcium mobilization
    • Vettor R, Granzotto M, De Stefani D, Trevellin E, Rossato M, et al. (2008). Loss-of-function mutation of the GPR40 gene associates with abnormal stimulated insulin secretion by acting on intracellular calcium mobilization. J Clin Endocrinol Metab 93: 3541–3550.
    • (2008) J Clin Endocrinol Metab , vol.93 , pp. 3541-3550
    • Vettor, R.1    Granzotto, M.2    De Stefani, D.3    Trevellin, E.4    Rossato, M.5
  • 22
  • 23
    • 0029797647 scopus 로고    scopus 로고
    • Regulation of insulin secretion by phospholipase C
    • Zawalich W, Zawalich K (1996). Regulation of insulin secretion by phospholipase C. Am J Physiol Endocrinol Metab 271: E409–E416.
    • (1996) Am J Physiol Endocrinol Metab , vol.271 , pp. E409-E416
    • Zawalich, W.1    Zawalich, K.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.