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Items: 1 to 20 of 130

1.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.

Ashton KS, Andrews KL, Bryan MC, Chen J, Chen K, Chen M, Chmait S, Croghan M, Cupples R, Fotsch C, Helmering J, Jordan SR, Kurzeja RJ, Michelsen K, Pennington LD, Poon SF, Sivits G, Van G, Vonderfecht SL, Wahl RC, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr.

J Med Chem. 2014 Jan 23;57(2):309-24. doi: 10.1021/jm4016735. Epub 2014 Jan 9. Erratum in: J Med Chem. 2014 Mar 27;57(6):2820. Bryan, Marion C [corrected to Bryan, Marian C].

PMID:
24405172
2.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.

St Jean DJ Jr, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C.

J Med Chem. 2014 Jan 23;57(2):325-38. doi: 10.1021/jm4016747. Epub 2014 Jan 9.

PMID:
24405213
3.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series.

Nishimura N, Norman MH, Liu L, Yang KC, Ashton KS, Bartberger MD, Chmait S, Chen J, Cupples R, Fotsch C, Helmering J, Jordan SR, Kunz RK, Pennington LD, Poon SF, Siegmund A, Sivits G, Lloyd DJ, Hale C, St Jean DJ Jr.

J Med Chem. 2014 Apr 10;57(7):3094-116. doi: 10.1021/jm5000497. Epub 2014 Mar 31.

PMID:
24611879
4.

Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors.

Lloyd DJ, St Jean DJ Jr, Kurzeja RJ, Wahl RC, Michelsen K, Cupples R, Chen M, Wu J, Sivits G, Helmering J, Komorowski R, Ashton KS, Pennington LD, Fotsch C, Vazir M, Chen K, Chmait S, Zhang J, Liu L, Norman MH, Andrews KL, Bartberger MD, Van G, Galbreath EJ, Vonderfecht SL, Wang M, Jordan SR, Véniant MM, Hale C.

Nature. 2013 Dec 19;504(7480):437-40. doi: 10.1038/nature12724. Epub 2013 Nov 13.

PMID:
24226772
5.

Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.

Tamayo NA, Norman MH, Bartberger MD, Hong FT, Bo Y, Liu L, Nishimura N, Yang KC, Tadesse S, Fotsch C, Chen J, Chmait S, Cupples R, Hale C, Jordan SR, Lloyd DJ, Sivits G, Van G, St Jean DJ Jr.

J Med Chem. 2015 Jun 11;58(11):4462-82. doi: 10.1021/jm5018175. Epub 2015 Jun 1.

PMID:
25914941
6.

Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 4. Exploration of a novel binding pocket.

Hong FT, Norman MH, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Fotsch C, Jordan SR, Lloyd DJ, Sivits G, Tadesse S, Hale C, St Jean DJ Jr.

J Med Chem. 2014 Jul 24;57(14):5949-64. doi: 10.1021/jm5001979. Epub 2014 Jul 8.

PMID:
25001129
7.

Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.

Pennington LD, Bartberger MD, Croghan MD, Andrews KL, Ashton KS, Bourbeau MP, Chen J, Chmait S, Cupples R, Fotsch C, Helmering J, Hong FT, Hungate RW, Jordan SR, Kong K, Liu L, Michelsen K, Moyer C, Nishimura N, Norman MH, Reichelt A, Siegmund AC, Sivits G, Tadesse S, Tegley CM, Van G, Yang KC, Yao G, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr.

J Med Chem. 2015 Dec 24;58(24):9663-79. doi: 10.1021/acs.jmedchem.5b01367. Epub 2015 Dec 1.

8.

Modulation of glucokinase by glucose, small-molecule activator and glucokinase regulatory protein: steady-state kinetic and cell-based analysis.

Bourbonais FJ, Chen J, Huang C, Zhang Y, Pfefferkorn JA, Landro JA.

Biochem J. 2012 Feb 1;441(3):881-7. doi: 10.1042/BJ20110721.

PMID:
22044397
9.

A patent review of glucokinase activators and disruptors of the glucokinase--glucokinase regulatory protein interaction: 2011-2014.

Filipski KJ, Pfefferkorn JA.

Expert Opin Ther Pat. 2014 Aug;24(8):875-91. doi: 10.1517/13543776.2014.918957. Epub 2014 May 12. Review.

PMID:
24821087
10.

An allosteric activator of glucokinase impairs the interaction of glucokinase and glucokinase regulatory protein and regulates glucose metabolism.

Futamura M, Hosaka H, Kadotani A, Shimazaki H, Sasaki K, Ohyama S, Nishimura T, Eiki J, Nagata Y.

J Biol Chem. 2006 Dec 8;281(49):37668-74. Epub 2006 Oct 6.

11.

Discovery of Small-Molecule Glucokinase Regulatory Protein Modulators That Restore Glucokinase Activity.

Chen K, Michelsen K, Kurzeja RJ, Han J, Vazir M, St Jean DJ Jr, Hale C, Wahl RC.

J Biomol Screen. 2014 Aug;19(7):1014-23. doi: 10.1177/1087057114530468. Epub 2014 Apr 9.

PMID:
24717911
12.

Molecular basis for the role of glucokinase regulatory protein as the allosteric switch for glucokinase.

Choi JM, Seo MH, Kyeong HH, Kim E, Kim HS.

Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):10171-6. doi: 10.1073/pnas.1300457110. Epub 2013 Jun 3.

13.

Biochemical basis of glucokinase activation and the regulation by glucokinase regulatory protein in naturally occurring mutations.

Heredia VV, Carlson TJ, Garcia E, Sun S.

J Biol Chem. 2006 Dec 29;281(52):40201-7. Epub 2006 Nov 2.

14.

Stimulation of hepatocyte glucose metabolism by novel small molecule glucokinase activators.

Brocklehurst KJ, Payne VA, Davies RA, Carroll D, Vertigan HL, Wightman HJ, Aiston S, Waddell ID, Leighton B, Coghlan MP, Agius L.

Diabetes. 2004 Mar;53(3):535-41.

15.

Inhibition of glucokinase translocation by AMP-activated protein kinase is associated with phosphorylation of both GKRP and 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase.

Mukhtar MH, Payne VA, Arden C, Harbottle A, Khan S, Lange AJ, Agius L.

Am J Physiol Regul Integr Comp Physiol. 2008 Mar;294(3):R766-74. doi: 10.1152/ajpregu.00593.2007. Epub 2008 Jan 16.

PMID:
18199594
16.

Biophysical characterization of the interaction between hepatic glucokinase and its regulatory protein: impact of physiological and pharmacological effectors.

Anderka O, Boyken J, Aschenbach U, Batzer A, Boscheinen O, Schmoll D.

J Biol Chem. 2008 Nov 14;283(46):31333-40. doi: 10.1074/jbc.M805434200. Epub 2008 Sep 22.

17.

Identification of a new class of glucokinase activators through structure-based design.

Hinklin RJ, Boyd SA, Chicarelli MJ, Condroski KR, DeWolf WE Jr, Lee PA, Lee W, Singh A, Thomas L, Voegtli WC, Williams L, Aicher TD.

J Med Chem. 2013 Oct 10;56(19):7669-78. doi: 10.1021/jm401116k. Epub 2013 Sep 25.

PMID:
24015910
18.

Targeting glucokinase activation for the treatment of type 2 diabetes--a status review.

Sarabu R, Grimsby J.

Curr Opin Drug Discov Devel. 2005 Sep;8(5):631-7. Review.

PMID:
16159025
20.

Glucotoxicity targets hepatic glucokinase in Zucker diabetic fatty rats, a model of type 2 diabetes associated with obesity.

Ueta K, O'Brien TP, McCoy GA, Kim K, Healey EC, Farmer TD, Donahue EP, Condren AB, Printz RL, Shiota M.

Am J Physiol Endocrinol Metab. 2014 Jun 1;306(11):E1225-38. doi: 10.1152/ajpendo.00507.2013. Epub 2014 Apr 8.

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