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Items: 1 to 20 of 133

1.

S 50131 and S 51434, two novel small molecule glucokinase activators, lack chronic efficacy despite potent acute antihyperglycaemic activity in diabetic mice.

De Ceuninck F, Kargar C, Charton Y, Goldstein S, Perron-Sierra F, Ilic C, Caliez A, Rolin JO, Sadlo M, Harley E, Vinson C, Ktorza A.

Br J Pharmacol. 2013 Jul;169(5):999-1010. doi: 10.1111/bph.12172.

2.

Small molecule glucokinase activators disturb lipid homeostasis and induce fatty liver in rodents: a warning for therapeutic applications in humans.

De Ceuninck F, Kargar C, Ilic C, Caliez A, Rolin JO, Umbdenstock T, Vinson C, Combettes M, de Fanti B, Harley E, Sadlo M, Lefèvre AL, Broux O, Wierzbicki M, Fourquez JM, Perron-Sierra F, Kotschy A, Ktorza A.

Br J Pharmacol. 2013 Jan;168(2):339-53. doi: 10.1111/j.1476-5381.2012.02184.x.

3.

Glucokinase activator PSN-GK1 displays enhanced antihyperglycaemic and insulinotropic actions.

Fyfe MC, White JR, Taylor A, Chatfield R, Wargent E, Printz RL, Sulpice T, McCormack JG, Procter MJ, Reynet C, Widdowson PS, Wong-Kai-In P.

Diabetologia. 2007 Jun;50(6):1277-87. Epub 2007 Apr 6.

PMID:
17415548
4.

Treatment with exendin-4 improves the antidiabetic efficacy and reverses hepatic steatosis in glucokinase activator treated db/db mice.

Dhanesha N, Joharapurkar A, Shah G, Kshirsagar S, Patel V, Patel K, Bahekar R, Jain M.

Eur J Pharmacol. 2013 Aug 15;714(1-3):188-92. doi: 10.1016/j.ejphar.2013.06.015. Epub 2013 Jun 25.

PMID:
23810686
5.

Allosteric activators of glucokinase: potential role in diabetes therapy.

Grimsby J, Sarabu R, Corbett WL, Haynes NE, Bizzarro FT, Coffey JW, Guertin KR, Hilliard DW, Kester RF, Mahaney PE, Marcus L, Qi L, Spence CL, Tengi J, Magnuson MA, Chu CA, Dvorozniak MT, Matschinsky FM, Grippo JF.

Science. 2003 Jul 18;301(5631):370-3.

6.

Chronic glucokinase activator treatment at clinically translatable exposures gives durable glucose lowering in two animal models of type 2 diabetes.

Baker DJ, Wilkinson GP, Atkinson AM, Jones HB, Coghlan M, Charles AD, Leighton B.

Br J Pharmacol. 2014 Apr;171(7):1642-54.

7.

Research and development of glucokinase activators for diabetes therapy: theoretical and practical aspects.

Matschinsky FM, Zelent B, Doliba NM, Kaestner KH, Vanderkooi JM, Grimsby J, Berthel SJ, Sarabu R.

Handb Exp Pharmacol. 2011;(203):357-401. doi: 10.1007/978-3-642-17214-4_15. Review.

PMID:
21484579
8.

Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.

Xu J, Lin S, Myers RW, Addona G, Berger JP, Campbell B, Chen HS, Chen Z, Eiermann GJ, Elowe NH, Farrer BT, Feng W, Fu Q, Kats-Kagan R, Kavana M, Malkani S, McMasters DR, Mitra K, Pachanski MJ, Tong X, Trujillo ME, Xu L, Zhang B, Zhang F, Zhang R, Parmee ER.

Bioorg Med Chem Lett. 2017 May 1;27(9):2069-2073. doi: 10.1016/j.bmcl.2016.10.085. Epub 2016 Oct 31.

PMID:
28284804
9.

Antidiabetic potential of a novel dual-target activator of glucokinase and peroxisome proliferator activated receptor-γ.

Lei L, Liu Q, Liu S, Huan Y, Sun S, Chen Z, Li L, Feng Z, Li Y, Shen Z.

Metabolism. 2015 Oct;64(10):1250-61. doi: 10.1016/j.metabol.2015.06.014. Epub 2015 Jun 23.

PMID:
26189598
10.

Discovery of 3-(4-methanesulfonylphenoxy)-N-[1-(2-methoxy-ethoxymethyl)-1H-pyrazol-3-yl]-5-(3-methylpyridin-2-yl)-benzamide as a novel glucokinase activator (GKA) for the treatment of type 2 diabetes mellitus.

Park K, Lee BM, Hyun KH, Lee DH, Choi HH, Kim H, Chong W, Kim KB, Nam SY.

Bioorg Med Chem. 2014 Apr 1;22(7):2280-93. doi: 10.1016/j.bmc.2014.02.009. Epub 2014 Feb 17.

PMID:
24588963
11.

Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs.

Eiki J, Nagata Y, Futamura M, Sasaki-Yamamoto K, Iino T, Nishimura T, Chiba M, Ohyama S, Yoshida-Yoshimioto R, Fujii K, Hosaka H, Goto-Shimazaki H, Kadotani A, Ohe T, Lin S, Langdon RB, Berger JP.

Mol Pharmacol. 2011 Dec;80(6):1156-65. doi: 10.1124/mol.111.074401. Epub 2011 Sep 21.

12.

Small molecule glucokinase activators as novel anti-diabetic agents.

Leighton B, Atkinson A, Coghlan MP.

Biochem Soc Trans. 2005 Apr;33(Pt 2):371-4. Review.

PMID:
15787609
13.

Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.

Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP.

J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24.

PMID:
22196621
14.

Recent updates on glucokinase activators for the treatment of type 2 diabetes mellitus.

Grewal AS, Sekhon BS, Lather V.

Mini Rev Med Chem. 2014;14(7):585-602. Review.

PMID:
25052034
15.

Effects of glucokinase activators GKA50 and LY2121260 on proliferation and apoptosis in pancreatic INS-1 beta cells.

Wei P, Shi M, Barnum S, Cho H, Carlson T, Fraser JD.

Diabetologia. 2009 Oct;52(10):2142-50. doi: 10.1007/s00125-009-1446-0. Epub 2009 Jul 30.

PMID:
19641898
16.
17.

Lessons from glucokinase activators: the problem of declining efficacy.

Agius L.

Expert Opin Ther Pat. 2014 Nov;24(11):1155-9. doi: 10.1517/13543776.2014.965680. Epub 2014 Sep 30. Review.

PMID:
25266490
18.

A novel glucokinase activator modulates pancreatic islet and hepatocyte function.

Efanov AM, Barrett DG, Brenner MB, Briggs SL, Delaunois A, Durbin JD, Giese U, Guo H, Radloff M, Gil GS, Sewing S, Wang Y, Weichert A, Zaliani A, Gromada J.

Endocrinology. 2005 Sep;146(9):3696-701. Epub 2005 May 26.

PMID:
15919746
19.

Exendin-4 ameliorates diabetic symptoms through activation of glucokinase.

Dhanesha N, Joharapurkar A, Shah G, Dhote V, Kshirsagar S, Bahekar R, Jain M.

J Diabetes. 2012 Dec;4(4):369-77. doi: 10.1111/j.1753-0407.2012.00193.x.

PMID:
22356440
20.

Chronic glucokinase activation reduces glycaemia and improves glucose tolerance in high-fat diet fed mice.

Winzell MS, Coghlan M, Leighton B, Frangioudakis G, Smith DM, Storlien LH, Ahrén B.

Eur J Pharmacol. 2011 Aug 1;663(1-3):80-6. doi: 10.1016/j.ejphar.2011.05.009. Epub 2011 May 11.

PMID:
21586282

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