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Items: 1 to 20 of 102

1.

The relationship of glucokinase activator-induced hypoglycemia with arteriopathy, neuronal necrosis, and peripheral neuropathy in nonclinical studies.

Pettersen JC, Litchfield J, Neef N, Schmidt SP, Shirai N, Walters KM, Enerson BE, Chatman LA, Pfefferkorn JA.

Toxicol Pathol. 2014 Jun;42(4):696-708. doi: 10.1177/0192623314526006. Epub 2014 Apr 24.

2.

Utilization of the Zucker Diabetic Fatty (ZDF) Rat Model for Investigating Hypoglycemia-related Toxicities.

Tirmenstein M, Horvath J, Graziano M, Mangipudy R, Dorr T, Colman K, Zinker B, Kirby M, Cheng PT, Patrone L, Kozlosky J, Reilly TP, Wang V, Janovitz E.

Toxicol Pathol. 2015 Aug;43(6):825-37. doi: 10.1177/0192623315581020. Epub 2015 Jun 17.

3.

Glucokinase activators AZD6370 and AZD1656 do not affect the central counterregulatory response to hypoglycemia in healthy males.

Norjavaara E, Ericsson H, Sjöberg F, Leonsson-Zachrisson M, Sjöstrand M, Morrow LA, Hompesch M.

J Clin Endocrinol Metab. 2012 Sep;97(9):3319-25. doi: 10.1210/jc.2012-1496. Epub 2012 Jun 21.

PMID:
22723318
4.

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.

5.

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.

6.

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
7.

Adaptation of glucokinase gene expression in the rat dorsal vagal complex in a model for recurrent intermediate insulin-induced hypoglycemia: impact of gender.

Genabai NK, Vavaiya KV, Briski KP.

J Mol Neurosci. 2009 Jan;37(1):80-5. doi: 10.1007/s12031-008-9126-y. Epub 2008 Jul 9.

PMID:
18612599
8.

Discovery of piragliatin--first glucokinase activator studied in type 2 diabetic patients.

Sarabu R, Bizzarro FT, Corbett WL, Dvorozniak MT, Geng W, Grippo JF, Haynes NE, Hutchings S, Garofalo L, Guertin KR, Hilliard DW, Kabat M, Kester RF, Ka W, Liang Z, Mahaney PE, Marcus L, Matschinsky FM, Moore D, Racha J, Radinov R, Ren Y, Qi L, Pignatello M, Spence CL, Steele T, Tengi J, Grimsby J.

J Med Chem. 2012 Aug 23;55(16):7021-36. doi: 10.1021/jm3008689. Epub 2012 Aug 1.

PMID:
22809456
9.
11.
12.

Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator.

Sharma R, Litchfield J, Atkinson K, Eng H, Amin NB, Denney WS, Pettersen JC, Goosen TC, Di L, Lee E, Pfefferkorn JA, Dalvie DK, Kalgutkar AS.

Drug Metab Dispos. 2014 Nov;42(11):1926-39. doi: 10.1124/dmd.114.060087. Epub 2014 Aug 20.

13.
14.

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.

15.

GKAs for diabetes therapy: why no clinically useful drug after two decades of trying?

Matschinsky FM.

Trends Pharmacol Sci. 2013 Feb;34(2):90-9. doi: 10.1016/j.tips.2012.11.007. Epub 2013 Jan 7.

PMID:
23305809
16.

Peripheral neuropathy in rats induced by insulin treatment.

Sidenius P, Jakobsen J.

Diabetes. 1983 Apr;32(4):383-6.

PMID:
6299868
17.

Piragliatin (RO4389620), a novel glucokinase activator, lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus: a mechanistic study.

Bonadonna RC, Heise T, Arbet-Engels C, Kapitza C, Avogaro A, Grimsby J, Zhi J, Grippo JF, Balena R.

J Clin Endocrinol Metab. 2010 Nov;95(11):5028-36. doi: 10.1210/jc.2010-1041. Epub 2010 Aug 25.

PMID:
20739378
18.

Ventromedial hypothalamic glucokinase is an important mediator of the counterregulatory response to insulin-induced hypoglycemia.

Levin BE, Becker TC, Eiki J, Zhang BB, Dunn-Meynell AA.

Diabetes. 2008 May;57(5):1371-9. doi: 10.2337/db07-1755. Epub 2008 Feb 21.

19.

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
20.

Insulin-induced hypoglycemic peripheral motor neuropathy in spontaneously diabetic WBN/Kob rats.

Ozaki K, Sano T, Tsuji N, Matsuura T, Narama I.

Comp Med. 2010 Aug;60(4):282-7.

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