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Items: 13

1.

Anti-obesity effects of GIPR antagonists alone and in combination with GLP-1R agonists in preclinical models.

Killion EA, Wang J, Yie J, Shi SD, Bates D, Min X, Komorowski R, Hager T, Deng L, Atangan L, Lu SC, Kurzeja RJM, Sivits G, Lin J, Chen Q, Wang Z, Thibault SA, Abbott CM, Meng T, Clavette B, Murawsky CM, Foltz IN, Rottman JB, Hale C, Véniant MM, Lloyd DJ.

Sci Transl Med. 2018 Dec 19;10(472). pii: eaat3392. doi: 10.1126/scitranslmed.aat3392.

PMID:
30567927
2.

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.

3.

Pharmacologic Effects of FGF21 Are Independent of the "Browning" of White Adipose Tissue.

Véniant MM, Sivits G, Helmering J, Komorowski R, Lee J, Fan W, Moyer C, Lloyd DJ.

Cell Metab. 2015 May 5;21(5):731-8. doi: 10.1016/j.cmet.2015.04.019.

4.

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
5.

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
6.

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
7.

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
8.

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
9.

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
10.

Pharmacological targeting of glucagon and glucagon-like peptide 1 receptors has different effects on energy state and glucose homeostasis in diet-induced obese mice.

Gu W, Lloyd DJ, Chinookswong N, Komorowski R, Sivits G Jr, Graham M, Winters KA, Yan H, Boros LG, Lindberg RA, Véniant MM.

J Pharmacol Exp Ther. 2011 Jul;338(1):70-81. doi: 10.1124/jpet.111.179986. Epub 2011 Apr 6.

PMID:
21471191
11.

Glucagon receptor antagonist-mediated improvements in glycemic control are dependent on functional pancreatic GLP-1 receptor.

Gu W, Winters KA, Motani AS, Komorowski R, Zhang Y, Liu Q, Wu X, Rulifson IC, Sivits G Jr, Graham M, Yan H, Wang P, Moore S, Meng T, Lindberg RA, Véniant MM.

Am J Physiol Endocrinol Metab. 2010 Oct;299(4):E624-32. doi: 10.1152/ajpendo.00102.2010. Epub 2010 Jul 20.

12.

Long-term inhibition of the glucagon receptor with a monoclonal antibody in mice causes sustained improvement in glycemic control, with reversible alpha-cell hyperplasia and hyperglucagonemia.

Gu W, Yan H, Winters KA, Komorowski R, Vonderfecht S, Atangan L, Sivits G, Hill D, Yang J, Bi V, Shen Y, Hu S, Boone T, Lindberg RA, Véniant MM.

J Pharmacol Exp Ther. 2009 Dec;331(3):871-81. doi: 10.1124/jpet.109.157685. Epub 2009 Aug 31.

PMID:
19720878
13.

Fibroblast growth factor 21 reverses hepatic steatosis, increases energy expenditure, and improves insulin sensitivity in diet-induced obese mice.

Xu J, Lloyd DJ, Hale C, Stanislaus S, Chen M, Sivits G, Vonderfecht S, Hecht R, Li YS, Lindberg RA, Chen JL, Jung DY, Zhang Z, Ko HJ, Kim JK, Véniant MM.

Diabetes. 2009 Jan;58(1):250-9. doi: 10.2337/db08-0392. Epub 2008 Oct 7.

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