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Items: 1 to 20 of 110

1.

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.

PMID:
24405213
2.

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. Erratum in: J Med Chem. 2014 Mar 27;57(6):2820. Bryan, Marion C [corrected to Bryan, Marian C].

PMID:
24405172
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.

PMID:
24611879
4.

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.

5.

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.

PMID:
24226772
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.

PMID:
25001129
7.

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.

PMID:
25914941
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.

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.

10.

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.

11.

Discovery and structure-activity relationships of a novel class of quinazoline glucokinase activators.

Iino T, Sasaki Y, Bamba M, Mitsuya M, Ohno A, Kamata K, Hosaka H, Maruki H, Futamura M, Yoshimoto R, Ohyama S, Sasaki K, Chiba M, Ohtake N, Nagata Y, Eiki J, Nishimura T.

Bioorg Med Chem Lett. 2009 Oct 1;19(19):5531-8. doi: 10.1016/j.bmcl.2009.08.064.

PMID:
19726182
12.

Mice mutant for glucokinase regulatory protein exhibit decreased liver glucokinase: a sequestration mechanism in metabolic regulation.

Farrelly D, Brown KS, Tieman A, Ren J, Lira SA, Hagan D, Gregg R, Mookhtiar KA, Hariharan N.

Proc Natl Acad Sci U S A. 1999 Dec 7;96(25):14511-6.

13.

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.

14.

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. Review.

PMID:
24821087
15.

SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: discovery of PSN-GK1.

Bertram LS, Black D, Briner PH, Chatfield R, Cooke A, Fyfe MC, Murray PJ, Naud F, Nawano M, Procter MJ, Rakipovski G, Rasamison CM, Reynet C, Schofield KL, Shah VK, Spindler F, Taylor A, Turton R, Williams GM, Wong-Kai-In P, Yasuda K.

J Med Chem. 2008 Jul 24;51(14):4340-5. doi: 10.1021/jm8003202.

PMID:
18588279
16.

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.

PMID:
24015910
17.

Nonracemic synthesis of GK-GKRP disruptor AMG-3969.

Bourbeau MP, Ashton KS, Yan J, St Jean DJ Jr.

J Org Chem. 2014 Apr 18;79(8):3684-7. doi: 10.1021/jo500336e.

PMID:
24678849
18.

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.

PMID:
24717911
19.

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.

PMID:
22196621
20.

Treatment of type 2 diabetes by adenoviral-mediated overexpression of the glucokinase regulatory protein.

Slosberg ED, Desai UJ, Fanelli B, St Denny I, Connelly S, Kaleko M, Boettcher BR, Caplan SL.

Diabetes. 2001 Aug;50(8):1813-20.

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