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Items: 38

1.

Discovery of Potent and Orally Bioavailable Dihydropyrazole GPR40 Agonists.

Shi J, Gu Z, Jurica EA, Wu X, Haque LE, Williams KN, Hernandez AS, Hong Z, Gao Q, Dabros M, Davulcu AH, Mathur A, Rampulla RA, Gupta AK, Jayaram R, Apedo A, Moore DB, Liu H, Kunselman LK, Brady EJ, Wilkes JJ, Zinker BA, Cai H, Shu YZ, Sun Q, Dierks EA, Foster KA, Xu C, Wang T, Panemangalore R, Cvijic ME, Xie C, Cao GG, Zhou M, Krupinski J, Whaley JM, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2018 Feb 8;61(3):681-694. doi: 10.1021/acs.jmedchem.7b00982. Epub 2018 Jan 27.

PMID:
29316397
2.

Discovery of Pyrrolidine-Containing GPR40 Agonists: Stereochemistry Effects a Change in Binding Mode.

Jurica EA, Wu X, Williams KN, Hernandez AS, Nirschl DS, Rampulla RA, Mathur A, Zhou M, Cao G, Xie C, Jacob B, Cai H, Wang T, Murphy BJ, Liu H, Xu C, Kunselman LK, Hicks MB, Sun Q, Schnur DM, Sitkoff DF, Dierks EA, Apedo A, Moore DB, Foster KA, Cvijic ME, Panemangalore R, Flynn NA, Maxwell BD, Hong Y, Tian Y, Wilkes JJ, Zinker BA, Whaley JM, Barrish JC, Robl JA, Ewing WR, Ellsworth BA.

J Med Chem. 2017 Feb 23;60(4):1417-1431. doi: 10.1021/acs.jmedchem.6b01559. Epub 2017 Feb 9.

PMID:
28112924
3.

Gene expression analysis in rats treated with experimental acetyl-coenzyme A carboxylase inhibitors suggests interactions with the peroxisome proliferator-activated receptor alpha pathway.

Waring JF, Yang Y, Healan-Greenberg CH, Adler AL, Dickinson R, McNally T, Wang X, Weitzberg M, Xu X, Lisowski A, Warder SE, Gu YG, Zinker BA, Blomme EA, Camp HS.

J Pharmacol Exp Ther. 2008 Feb;324(2):507-16. Epub 2007 Nov 19.

PMID:
18025247
4.

Pyrrolidine-constrained phenethylamines: The design of potent, selective, and pharmacologically efficacious dipeptidyl peptidase IV (DPP4) inhibitors from a lead-like screening hit.

Backes BJ, Longenecker K, Hamilton GL, Stewart K, Lai C, Kopecka H, von Geldern TW, Madar DJ, Pei Z, Lubben TH, Zinker BA, Tian Z, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Kempf-Grote AJ, Black-Schaefer C, Sham HL, Trevillyan JM.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):2005-12. Epub 2007 Jan 19.

PMID:
17276063
5.

Discovery of ((4R,5S)-5-amino-4-(2,4,5- trifluorophenyl)cyclohex-1-enyl)-(3- (trifluoromethyl)-5,6-dihydro- [1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanone (ABT-341), a highly potent, selective, orally efficacious, and safe dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Pei Z, Li X, von Geldern TW, Madar DJ, Longenecker K, Yong H, Lubben TH, Stewart KD, Zinker BA, Backes BJ, Judd AS, Mulhern M, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Reinhart GA, Fryer RM, Preusser LC, Kempf-Grote AJ, Sham HL, Trevillyan JM.

J Med Chem. 2006 Nov 2;49(22):6439-42.

PMID:
17064063
6.

Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.

Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM.

J Med Chem. 2006 Oct 19;49(21):6416-20.

PMID:
17034148
7.

Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy)thiazol-5-yl]-1- methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors.

Gu YG, Weitzberg M, Clark RF, Xu X, Li Q, Zhang T, Hansen TM, Liu G, Xin Z, Wang X, Wang R, McNally T, Zinker BA, Frevert EU, Camp HS, Beutel BA, Sham HL.

J Med Chem. 2006 Jun 29;49(13):3770-3. Erratum in: J Med Chem. 2006 Aug 10;49(16):5028. Zinker, Bradley A [added]; Frevert, Ernst U [added]; Camp, Heidi [corrected to Camp, Heidi S].

PMID:
16789734
8.

Discovery, structure-activity relationship, and pharmacological evaluation of (5-substituted-pyrrolidinyl-2-carbonyl)-2-cyanopyrrolidines as potent dipeptidyl peptidase IV inhibitors.

Pei Z, Li X, Longenecker K, von Geldern TW, Wiedeman PE, Lubben TH, Zinker BA, Stewart K, Ballaron SJ, Stashko MA, Mika AK, Beno DW, Long M, Wells H, Kempf-Grote AJ, Madar DJ, McDermott TS, Bhagavatula L, Fickes MG, Pireh D, Solomon LR, Lake MR, Edalji R, Fry EH, Sham HL, Trevillyan JM.

J Med Chem. 2006 Jun 15;49(12):3520-35. Erratum in: J Med Chem. 2006 Aug 24;49(17):5387.

PMID:
16759095
9.

Endothelin antagonism improves hepatic insulin sensitivity associated with insulin signaling in Zucker fatty rats.

Berthiaume N, Carlson CJ, Rondinone CM, Zinker BA.

Metabolism. 2005 Nov;54(11):1515-23.

PMID:
16253642
10.

Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo.

Luo Y, Shoemaker AR, Liu X, Woods KW, Thomas SA, de Jong R, Han EK, Li T, Stoll VS, Powlas JA, Oleksijew A, Mitten MJ, Shi Y, Guan R, McGonigal TP, Klinghofer V, Johnson EF, Leverson JD, Bouska JJ, Mamo M, Smith RA, Gramling-Evans EE, Zinker BA, Mika AK, Nguyen PT, Oltersdorf T, Rosenberg SH, Li Q, Giranda VL.

Mol Cancer Ther. 2005 Jun;4(6):977-86.

11.

Metabolic responses with endothelin antagonism in a model of insulin resistance.

Berthiaume N, Wessale JL, Opgenorth TJ, Zinker BA.

Metabolism. 2005 Jun;54(6):735-40.

PMID:
15931607
12.

Reduction of PTP1B induces differential expression of PI3-kinase (p85alpha) isoforms.

Rondinone CM, Clampit J, Gum RJ, Zinker BA, Jirousek MR, Trevillyan JM.

Biochem Biophys Res Commun. 2004 Oct 15;323(2):652-9.

PMID:
15369800
13.

Development of insulin resistance and endothelin-1 levels in the Zucker fatty rat.

Berthiaume N, Mika AK, Zinker BA.

Metabolism. 2003 Jul;52(7):845-9.

PMID:
12870159
14.

PTP1B antisense-treated mice show regulation of genes involved in lipogenesis in liver and fat.

Waring JF, Ciurlionis R, Clampit JE, Morgan S, Gum RJ, Jolly RA, Kroeger P, Frost L, Trevillyan J, Zinker BA, Jirousek M, Ulrich RG, Rondinone CM.

Mol Cell Endocrinol. 2003 May 30;203(1-2):155-68.

PMID:
12782412
15.

Discovery and structure-activity relationship of oxalylarylaminobenzoic acids as inhibitors of protein tyrosine phosphatase 1B.

Liu G, Szczepankiewicz BG, Pei Z, Janowick DA, Xin Z, Hajduk PJ, Abad-Zapatero C, Liang H, Hutchins CW, Fesik SW, Ballaron SJ, Stashko MA, Lubben T, Mika AK, Zinker BA, Trevillyan JM, Jirousek MR.

J Med Chem. 2003 May 22;46(11):2093-103.

PMID:
12747781
16.

Antisense protein tyrosine phosphatase 1B reverses activation of p38 mitogen-activated protein kinase in liver of ob/ob mice.

Gum RJ, Gaede LL, Heindel MA, Waring JF, Trevillyan JM, Zinker BA, Stark ME, Wilcox D, Jirousek MR, Rondinone CM, Ulrich RG.

Mol Endocrinol. 2003 Jun;17(6):1131-43. Epub 2003 Mar 20.

PMID:
12649327
17.

Reduction of protein tyrosine phosphatase 1B increases insulin-dependent signaling in ob/ob mice.

Gum RJ, Gaede LL, Koterski SL, Heindel M, Clampit JE, Zinker BA, Trevillyan JM, Ulrich RG, Jirousek MR, Rondinone CM.

Diabetes. 2003 Jan;52(1):21-8.

18.

PTP1B antisense oligonucleotide lowers PTP1B protein, normalizes blood glucose, and improves insulin sensitivity in diabetic mice.

Zinker BA, Rondinone CM, Trevillyan JM, Gum RJ, Clampit JE, Waring JF, Xie N, Wilcox D, Jacobson P, Frost L, Kroeger PE, Reilly RM, Koterski S, Opgenorth TJ, Ulrich RG, Crosby S, Butler M, Murray SF, McKay RA, Bhanot S, Monia BP, Jirousek MR.

Proc Natl Acad Sci U S A. 2002 Aug 20;99(17):11357-62. Epub 2002 Aug 8.

19.

Protein tyrosine phosphatase 1B reduction regulates adiposity and expression of genes involved in lipogenesis.

Rondinone CM, Trevillyan JM, Clampit J, Gum RJ, Berg C, Kroeger P, Frost L, Zinker BA, Reilly R, Ulrich R, Butler M, Monia BP, Jirousek MR, Waring JF.

Diabetes. 2002 Aug;51(8):2405-11.

20.

Glycemic and insulinemic responses of nondiabetic healthy adult subjects to an experimental acid-induced viscosity complex incorporated into a glucose beverage.

Wolf BW, Lai CS, Kipnes MS, Ataya DG, Wheeler KB, Zinker BA, Garleb KA, Firkins JL.

Nutrition. 2002 Jul-Aug;18(7-8):621-6.

PMID:
12093442
21.
22.

Glycemic response to a food starch esterified by 1-octenyl succinic anhydride in humans.

Wolf BW, Wolever TM, Bolognesi C, Zinker BA, Garleb KA, Firkins JL.

J Agric Food Chem. 2001 May;49(5):2674-8.

PMID:
11368654
23.

Glucagon response to exercise is critical for accelerated hepatic glutamine metabolism and nitrogen disposal.

Krishna MG, Coker RH, Lacy DB, Zinker BA, Halseth AE, Wasserman DH.

Am J Physiol Endocrinol Metab. 2000 Sep;279(3):E638-45.

24.

Nutrition and exercise in individuals with diabetes.

Zinker BA.

Clin Sports Med. 1999 Jul;18(3):585-606, vii-viii. Review.

PMID:
10410843
25.

A negative arterial-portal venous glucose gradient decreases skeletal muscle glucose uptake.

Galassetti P, Shiota M, Zinker BA, Wasserman DH, Cherrington AD.

Am J Physiol. 1998 Jul;275(1):E101-11. doi: 10.1152/ajpendo.1998.275.1.E101.

PMID:
9688880
26.

Sympathetic drive to liver and nonhepatic splanchnic tissue during prolonged exercise is increased in diabetes.

Coker RH, Krishna MG, Zinker BA, Allen EJ, Lacy DB, Wasserman DH.

Metabolism. 1997 Nov;46(11):1327-32.

PMID:
9361694
27.

Interaction of exercise, insulin, and hypoglycemia studied using euglycemic and hypoglycemic insulin clamps.

Zinker BA, Allison RG, Lacy DB, Wasserman DH.

Am J Physiol. 1997 Apr;272(4 Pt 1):E530-42.

PMID:
9142871
28.

Role of the endocrine pancreas in control of fuel metabolism by the liver during exercise.

Wasserman DH, O'Doherty RM, Zinker BA.

Int J Obes Relat Metab Disord. 1995 Oct;19 Suppl 4:S22-30. Review.

PMID:
8581091
29.

Interaction of decreased arterial PO2 and exercise on carbohydrate metabolism in the dog.

Zinker BA, Wilson RD, Wasserman DH.

Am J Physiol. 1995 Sep;269(3 Pt 1):E409-17.

PMID:
7573417
30.

Carbohydrate metabolism during exercise: influence of circulating fat availability.

Bracy DP, Zinker BA, Jacobs JC, Lacy DB, Wasserman DH.

J Appl Physiol (1985). 1995 Aug;79(2):506-13.

PMID:
7592210
31.

Contribution of pancreatic hormone responses to the elevation in carbohydrate metabolism with reduced PaO2.

Zinker BA, Wilson R, Wasserman DH.

Am J Physiol. 1995 Jun;268(6 Pt 1):E1174-83.

PMID:
7611394
32.

Acute adaptation of carbohydrate metabolism to decreased arterial PO2.

Zinker BA, Namdaran K, Wilson R, Lacy DB, Wasserman DH.

Am J Physiol. 1994 Jun;266(6 Pt 1):E921-9.

PMID:
8023923
33.

Exercise-induced fall in insulin: mechanism of action at the liver and effects on muscle glucose metabolism.

Zinker BA, Mohr T, Kelly P, Namdaran K, Bracy DP, Wasserman DH.

Am J Physiol. 1994 May;266(5 Pt 1):E683-9.

PMID:
7911275
34.

Augmented glucoregulatory hormone concentrations during exhausting exercise in mildly iron-deficient rats.

Zinker BA, Dallman PR, Brooks GA.

Am J Physiol. 1993 Oct;265(4 Pt 2):R863-71.

PMID:
8238458
35.

Regulation of glucose uptake and metabolism by working muscle. An in vivo analysis.

Zinker BA, Lacy DB, Bracy D, Jacobs J, Wasserman DH.

Diabetes. 1993 Jul;42(7):956-65.

PMID:
8513977
36.

Role of glucose and insulin loads to the exercising limb in increasing glucose uptake and metabolism.

Zinker BA, Lacy DB, Bracy DP, Wasserman DH.

J Appl Physiol (1985). 1993 Jun;74(6):2915-21.

PMID:
8365992
37.

Effect of swimming on prednisolone-induced osteoporosis in elderly rats.

Swissa-Sivan A, Statter M, Brooks GA, Azevedo J, Viguie C, Azoury R, Greenfield C, Oman S, Leichter I, Zinker BA, et al.

J Bone Miner Res. 1992 Feb;7(2):161-9.

PMID:
1570761
38.

Effects of a 36-hour fast on human endurance and substrate utilization.

Zinker BA, Britz K, Brooks GA.

J Appl Physiol (1985). 1990 Nov;69(5):1849-55.

PMID:
2272978

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