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Items: 50

1.

A comparative study of the binding properties, dipeptidyl peptidase-4 (DPP-4) inhibitory activity and glucose-lowering efficacy of the DPP-4 inhibitors alogliptin, linagliptin, saxagliptin, sitagliptin and vildagliptin in mice.

Berger JP, SinhaRoy R, Pocai A, Kelly TM, Scapin G, Gao YD, Pryor KAD, Wu JK, Eiermann GJ, Xu SS, Zhang X, Tatosian DA, Weber AE, Thornberry NA, Carr RD.

Endocrinol Diabetes Metab. 2017 Nov 24;1(1):e00002. doi: 10.1002/edm2.2. eCollection 2018 Jan.

2.

Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiac hypertrophy.

Myers RW, Guan HP, Ehrhart J, Petrov A, Prahalada S, Tozzo E, Yang X, Kurtz MM, Trujillo M, Gonzalez Trotter D, Feng D, Xu S, Eiermann G, Holahan MA, Rubins D, Conarello S, Niu X, Souza SC, Miller C, Liu J, Lu K, Feng W, Li Y, Painter RE, Milligan JA, He H, Liu F, Ogawa A, Wisniewski D, Rohm RJ, Wang L, Bunzel M, Qian Y, Zhu W, Wang H, Bennet B, LaFranco Scheuch L, Fernandez GE, Li C, Klimas M, Zhou G, van Heek M, Biftu T, Weber A, Kelley DE, Thornberry N, Erion MD, Kemp DM, Sebhat IK.

Science. 2017 Aug 4;357(6350):507-511. doi: 10.1126/science.aah5582. Epub 2017 Jul 13.

PMID:
28705990
3.

Discovery of orally active hepatoselective glucokinase activators for treatment of Type II Diabetes Mellitus.

Xu J, Lin S, Myers RW, Trujillo ME, Pachanski MJ, Malkani S, Chen HS, Chen Z, Campbell B, Eiermann GJ, Elowe N, Farrer BT, Feng W, Fu Q, Kats-Kagan R, Kavana M, McMasters DR, Mitra K, Tong X, Xu L, Zhang F, Zhang R, Addona GH, Berger JP, Zhang B, Parmee ER.

Bioorg Med Chem Lett. 2017 May 1;27(9):2063-2068. doi: 10.1016/j.bmcl.2016.10.088. Epub 2016 Oct 31.

PMID:
28284809
4.

Novel, highly potent systemic glucokinase activators for the treatment of Type 2 Diabetes Mellitus.

Xu J, Lin S, Myers RW, Addona G, Berger JP, Campbell B, Chen HS, Chen Z, Eiermann GJ, Elowe NH, Farrer BT, Feng W, Fu Q, Kats-Kagan R, Kavana M, Malkani S, McMasters DR, Mitra K, Pachanski MJ, Tong X, Trujillo ME, Xu L, Zhang B, Zhang F, Zhang R, Parmee ER.

Bioorg Med Chem Lett. 2017 May 1;27(9):2069-2073. doi: 10.1016/j.bmcl.2016.10.085. Epub 2016 Oct 31.

PMID:
28284804
5.

Discovery and Optimization of a Novel Triazole Series of GPR142 Agonists for the Treatment of Type 2 Diabetes.

Guo L, Parker DL, Zang Y, Sweis RF, Liu W, Sherer EC, Buist N, Terebetski J, Kelly T, Bugianesi R, Priest BT, Dingley KH, Li X, Mitelman S, Salituro G, Trujillo ME, Pachanski M, Kirkland M, Powles MA, Eiermann GJ, Feng Y, Shang J, Howard AD, Ujjainwalla F, Sinz CJ, Debenham JS, Edmondson SD, Nargund RP, Hagmann WK, Li D.

ACS Med Chem Lett. 2016 Oct 12;7(12):1107-1111. eCollection 2016 Dec 8.

6.

Quantifying rates of glucose production in vivo following an intraperitoneal tracer bolus.

Wang SP, Zhou D, Yao Z, Satapati S, Chen Y, Daurio NA, Petrov A, Shen X, Metzger D, Yin W, Nawrocki AR, Eiermann GJ, Hwa J, Fancourt C, Miller C, Herath K, Roddy TP, Slipetz D, Erion MD, Previs SF, Kelley DE.

Am J Physiol Endocrinol Metab. 2016 Dec 1;311(6):E911-E921. doi: 10.1152/ajpendo.00182.2016. Epub 2016 Sep 20.

7.

The discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors.

Cox JM, Chu HD, Kuethe JT, Gao YD, Scapin G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Sinha-Roy R, Weber AE, Biftu T.

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2622-6. doi: 10.1016/j.bmcl.2016.04.020. Epub 2016 Apr 9.

PMID:
27106708
8.

SAR exploration at the C-3 position of tetrahydro-β-carboline sstr3 antagonists.

He S, Dobbelaar PH, Guo L, Ye Z, Liu J, Jian T, Truong Q, Shah SK, Du W, Qi H, Bakshi RK, Hong Q, Dellureficio JD, Sherer E, Pasternak A, Feng Z, Reibarkh M, Lin M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK.

Bioorg Med Chem Lett. 2016 Mar 15;26(6):1529-1535. doi: 10.1016/j.bmcl.2016.02.022. Epub 2016 Feb 10.

PMID:
26898814
9.

Structure-activity-relationship of amide and sulfonamide analogs of omarigliptin.

Chen P, Feng D, Qian X, Apgar J, Wilkening R, Kuethe JT, Gao YD, Scapin G, Cox J, Doss G, Eiermann G, He H, Li X, Lyons KA, Metzger J, Petrov A, Wu JK, Xu S, Weber AE, Yan Y, Roy RS, Biftu T.

Bioorg Med Chem Lett. 2015 Dec 15;25(24):5767-71. doi: 10.1016/j.bmcl.2015.10.070. Epub 2015 Oct 30.

PMID:
26546218
10.

Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.

Shah SK, He S, Guo L, Truong Q, Qi H, Du W, Lai Z, Liu J, Jian T, Hong Q, Dobbelaar P, Ye Z, Sherer E, Feng Z, Yu Y, Wong F, Samuel K, Madiera M, Karanam BV, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Feng Y, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Pachanski M, Fernandez G, Nelson D, Bunting P, Morissette P, Volksdorf S, Kerr J, Zhang BB, Howard AD, Zhou YP, Pasternak A, Nargund RP, Hagmann WK.

ACS Med Chem Lett. 2015 Mar 18;6(5):513-7. doi: 10.1021/ml500514w. eCollection 2015 May 14.

11.

Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.

He S, Lai Z, Ye Z, Dobbelaar PH, Shah SK, Truong Q, Du W, Guo L, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Reibarkh M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang B, Howard AD, Zhou YP, Nargund RP, Hagmann WK.

ACS Med Chem Lett. 2014 Apr 21;5(7):748-53. doi: 10.1021/ml500028c. eCollection 2014 Jul 10.

12.

Diamine Derivatives as Novel Small-Molecule, Potent, and Subtype-Selective Somatostatin SST3 Receptor Agonists.

Li D, Wu Z, Yu Y, Ball RG, Guo L, Sherer E, He S, Hong Q, Lai Z, Qi H, Truong Q, Yang DX, Chicchi GG, Tsao KL, Trusca D, Trujillo M, Pachanski M, Eiermann GJ, Howard AD, Zhou YP, Zhang BB, Nargund RP, Hagmann WK.

ACS Med Chem Lett. 2014 Apr 24;5(6):690-5. doi: 10.1021/ml500079u. eCollection 2014 Jun 12.

13.

Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE.

J Med Chem. 2014 Apr 24;57(8):3205-12. doi: 10.1021/jm401992e. Epub 2014 Apr 2.

PMID:
24660890
14.

A PEGylated analog of the gut hormone oxyntomodulin with long-lasting antihyperglycemic, insulinotropic and anorexigenic activity.

Bianchi E, Carrington PE, Ingallinella P, Finotto M, Santoprete A, Petrov A, Eiermann G, Kosinski J, Marsh DJ, Pocai A, SinhaRoy R, Pessi A.

Bioorg Med Chem. 2013 Nov 15;21(22):7064-73. doi: 10.1016/j.bmc.2013.09.016. Epub 2013 Sep 19.

PMID:
24094437
15.

Novel tetrahydropyran analogs as dipeptidyl peptidase IV inhibitors: Profile of clinical candidate (2R,3S,5R)-2- (2,5-difluorophenyl)-5-(4,6-dihydropyrrolo [3,4-c]pyrazol-5-(1H)-yl)tetrahydro-2H-pyran-3-amine (23) [corrected].

Biftu T, Qian X, Chen P, Feng D, Scapin G, Gao YD, Cox J, Roy RS, Eiermann G, He H, Lyons K, Salituro G, Patel S, Petrov A, Xu F, Xu SS, Zhang B, Caldwell C, Wu JK, Lyons K, Weber AE.

Bioorg Med Chem Lett. 2013 Oct 1;23(19):5361-6. doi: 10.1016/j.bmcl.2013.07.061. Epub 2013 Aug 5. Erratum in: Bioorg Med Chem Lett. 2014 Jun 1;24(11):2590.

PMID:
23972441
16.

Optimization of co-agonism at GLP-1 and glucagon receptors to safely maximize weight reduction in DIO-rodents.

Day JW, Gelfanov V, Smiley D, Carrington PE, Eiermann G, Chicchi G, Erion MD, Gidda J, Thornberry NA, Tschöp MH, Marsh DJ, SinhaRoy R, DiMarchi R, Pocai A.

Biopolymers. 2012;98(5):443-50. doi: 10.1002/bip.22072.

PMID:
23203689
17.

The role of voltage-gated potassium channels Kv2.1 and Kv2.2 in the regulation of insulin and somatostatin release from pancreatic islets.

Li XN, Herrington J, Petrov A, Ge L, Eiermann G, Xiong Y, Jensen MV, Hohmeier HE, Newgard CB, Garcia ML, Wagner M, Zhang BB, Thornberry NA, Howard AD, Kaczorowski GJ, Zhou YP.

J Pharmacol Exp Ther. 2013 Feb;344(2):407-16. doi: 10.1124/jpet.112.199083. Epub 2012 Nov 16.

PMID:
23161216
18.

The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.

He S, Ye Z, Truong Q, Shah S, Du W, Guo L, Dobbelaar PH, Lai Z, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Pasternak A, Feng Z, deJesus R, Yang L, Reibarkh M, Bradley SA, Holmes MA, Ball RG, Ruck RT, Huffman MA, Wong F, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Eiermann GJ, Li C, Zhang BB, Howard AD, Zhou YP, Nargund RP, Hagmann WK.

ACS Med Chem Lett. 2012 May 7;3(6):484-9. doi: 10.1021/ml300063m. eCollection 2012 Jun 14.

19.

Differential effects of oxyntomodulin and GLP-1 on glucose metabolism.

Du X, Kosinski JR, Lao J, Shen X, Petrov A, Chicchi GG, Eiermann GJ, Pocai A.

Am J Physiol Endocrinol Metab. 2012 Jul 15;303(2):E265-71. doi: 10.1152/ajpendo.00142.2012. Epub 2012 May 22.

20.

Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.

Pasternak A, Feng Z, de Jesus R, Ye Z, He S, Dobbelaar P, Bradley SA, Chicchi GG, Tsao KL, Trusca D, Eiermann GJ, Li C, Feng Y, Wu M, Shao Q, Zhang BB, Nargund R, Mills SG, Howard AD, Yang L, Zhou YP.

ACS Med Chem Lett. 2012 Feb 27;3(4):289-93. doi: 10.1021/ml200272z. eCollection 2012 Apr 12.

21.

Plasma lipid profiling across species for the identification of optimal animal models of human dyslipidemia.

Yin W, Carballo-Jane E, McLaren DG, Mendoza VH, Gagen K, Geoghagen NS, McNamara LA, Gorski JN, Eiermann GJ, Petrov A, Wolff M, Tong X, Wilsie LC, Akiyama TE, Chen J, Thankappan A, Xue J, Ping X, Andrews G, Wickham LA, Gai CL, Trinh T, Kulick AA, Donnelly MJ, Voronin GO, Rosa R, Cumiskey AM, Bekkari K, Mitnaul LJ, Puig O, Chen F, Raubertas R, Wong PH, Hansen BC, Koblan KS, Roddy TP, Hubbard BK, Strack AM.

J Lipid Res. 2012 Jan;53(1):51-65. doi: 10.1194/jlr.M019927. Epub 2011 Oct 23.

22.

3-Substituted 3-(4-aryloxyaryl)-propanoic acids as GPR40 agonists.

Walsh SP, Severino A, Zhou C, He J, Liang GB, Tan CP, Cao J, Eiermann GJ, Xu L, Salituro G, Howard AD, Mills SG, Yang L.

Bioorg Med Chem Lett. 2011 Jun 1;21(11):3390-4. doi: 10.1016/j.bmcl.2011.03.114. Epub 2011 Apr 8.

PMID:
21514824
23.

Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists.

Zhou C, Tang C, Chang E, Ge M, Lin S, Cline E, Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Salituro G, Meinke P, Mosley R, Akiyama TE, Einstein M, Kumar S, Berger J, Howard AD, Thornberry N, Mills SG, Yang L.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1298-301. doi: 10.1016/j.bmcl.2009.10.052. Epub 2009 Oct 15.

PMID:
20064714
24.

Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes.

Mu J, Petrov A, Eiermann GJ, Woods J, Zhou YP, Li Z, Zycband E, Feng Y, Zhu L, Roy RS, Howard AD, Li C, Thornberry NA, Zhang BB.

Eur J Pharmacol. 2009 Nov 25;623(1-3):148-54. doi: 10.1016/j.ejphar.2009.09.027. Epub 2009 Sep 16.

PMID:
19765579
25.

Glucagon-like peptide 1/glucagon receptor dual agonism reverses obesity in mice.

Pocai A, Carrington PE, Adams JR, Wright M, Eiermann G, Zhu L, Du X, Petrov A, Lassman ME, Jiang G, Liu F, Miller C, Tota LM, Zhou G, Zhang X, Sountis MM, Santoprete A, Capito' E, Chicchi GG, Thornberry N, Bianchi E, Pessi A, Marsh DJ, SinhaRoy R.

Diabetes. 2009 Oct;58(10):2258-66. doi: 10.2337/db09-0278. Epub 2009 Jul 14.

26.

Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.

Edmondson SD, Mastracchio A, Cox JM, Eiermann GJ, He H, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Xu S, Zhu B, Thornberry NA, Roy RS, Weber AE.

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4097-101. doi: 10.1016/j.bmcl.2009.06.011. Epub 2009 Jun 6.

PMID:
19539471
27.

Genetic ablation or pharmacological blockade of dipeptidyl peptidase IV does not impact T cell-dependent immune responses.

Vora KA, Porter G, Peng R, Cui Y, Pryor K, Eiermann G, Zaller DM.

BMC Immunol. 2009 Apr 9;10:19. doi: 10.1186/1471-2172-10-19.

28.

Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice.

Tan CP, Feng Y, Zhou YP, Eiermann GJ, Petrov A, Zhou C, Lin S, Salituro G, Meinke P, Mosley R, Akiyama TE, Einstein M, Kumar S, Berger JP, Mills SG, Thornberry NA, Yang L, Howard AD.

Diabetes. 2008 Aug;57(8):2211-9. doi: 10.2337/db08-0130. Epub 2008 May 13.

29.

An automated electrophysiology serum shift assay for K(V) channels.

Ratliff KS, Petrov A, Eiermann GJ, Deng Q, Green MD, Kaczorowski GJ, McManus OB, Herrington J.

Assay Drug Dev Technol. 2008 Apr;6(2):243-53. doi: 10.1089/adt.2008.128.

PMID:
18471078
30.

Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.

Kim D, Kowalchick JE, Brockunier LL, Parmee ER, Eiermann GJ, Fisher MH, He H, Leiting B, Lyons K, Scapin G, Patel SB, Petrov A, Pryor KD, Roy RS, Wu JK, Zhang X, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE.

J Med Chem. 2008 Feb 14;51(3):589-602. doi: 10.1021/jm070330v. Epub 2008 Jan 18.

PMID:
18201067
31.

4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.

Kaelin DE, Smenton AL, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE, Duffy JL.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5806-11. Epub 2007 Aug 26.

PMID:
17851076
32.

Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors.

Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A, Scapin G, Patel RA, Thornberry NA, Weber AE, Kim D.

Bioorg Med Chem Lett. 2007 Nov 1;17(21):5934-9. Epub 2007 Aug 23.

PMID:
17827003
33.

Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).

Kim D, Kowalchick JE, Edmondson SD, Mastracchio A, Xu J, Eiermann GJ, Leiting B, Wu JK, Pryor KD, Patel RA, He H, Lyons KA, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3373-7. Epub 2007 Apr 5.

PMID:
17434732
34.

Rational design of a novel, potent, and orally bioavailable cyclohexylamine DPP-4 inhibitor by application of molecular modeling and X-ray crystallography of sitagliptin.

Biftu T, Scapin G, Singh S, Feng D, Becker JW, Eiermann G, He H, Lyons K, Patel S, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Doss GA, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3384-7. Epub 2007 Apr 2.

PMID:
17433672
35.

4-aminophenylalanine and 4-aminocyclohexylalanine derivatives as potent, selective, and orally bioavailable inhibitors of dipeptidyl peptidase IV.

Duffy JL, Kirk BA, Wang L, Eiermann GJ, He H, Leiting B, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 May 15;17(10):2879-85. Epub 2007 Feb 25.

PMID:
17350841
36.

Optimization of 1,4-diazepan-2-one containing dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes.

Liang GB, Qian X, Feng D, Biftu T, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Wu J, Zhang X, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 Apr 1;17(7):1903-7. Epub 2007 Jan 24.

PMID:
17291750
37.

(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Biftu T, Feng D, Qian X, Liang GB, Kieczykowski G, Eiermann G, He H, Leiting B, Lyons K, Petrov A, Sinha-Roy R, Zhang B, Scapin G, Patel S, Gao YD, Singh S, Wu J, Zhang X, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):49-52. Epub 2006 Oct 5.

PMID:
17055272
38.

Discovery of potent, selective, and orally bioavailable oxadiazole-based dipeptidyl peptidase IV inhibitors.

Xu J, Wei L, Mathvink RJ, Edmondson SD, Eiermann GJ, He H, Leone JF, Leiting B, Lyons KA, Marsilio F, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2006 Oct 15;16(20):5373-7. Epub 2006 Aug 17.

PMID:
16919457
39.

(2S,3S)-3-Amino-4-(3,3-difluoropyrrolidin-1-yl)-N,N-dimethyl-4-oxo-2-(4-[1,2,4]triazolo[1,5-a]-pyridin-6-ylphenyl)butanamide: a selective alpha-amino amide dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Edmondson SD, Mastracchio A, Mathvink RJ, He J, Harper B, Park YJ, Beconi M, Di Salvo J, Eiermann GJ, He H, Leiting B, Leone JF, Levorse DA, Lyons K, Patel RA, Patel SB, Petrov A, Scapin G, Shang J, Roy RS, Smith A, Wu JK, Xu S, Zhu B, Thornberry NA, Weber AE.

J Med Chem. 2006 Jun 15;49(12):3614-27.

PMID:
16759103
40.

Discovery of potent, selective, and orally bioavailable pyridone-based dipeptidyl peptidase-4 inhibitors.

Xu J, Wei L, Mathvink R, Edmondson SD, Mastracchio A, Eiermann GJ, He H, Leone JF, Leiting B, Lyons KA, Marsilio F, Patel RA, Petrov A, Wu JK, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2006 Mar 1;16(5):1346-9. Epub 2005 Dec 5.

PMID:
16332437
41.

Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9.

Lankas GR, Leiting B, Roy RS, Eiermann GJ, Beconi MG, Biftu T, Chan CC, Edmondson S, Feeney WP, He H, Ippolito DE, Kim D, Lyons KA, Ok HO, Patel RA, Petrov AN, Pryor KA, Qian X, Reigle L, Woods A, Wu JK, Zaller D, Zhang X, Zhu L, Weber AE, Thornberry NA.

Diabetes. 2005 Oct;54(10):2988-94.

42.

Discovery of potent and selective orally bioavailable beta-substituted phenylalanine derived dipeptidyl peptidase IV inhibitors.

Edmondson SD, Mastracchio A, Duffy JL, Eiermann GJ, He H, Ita I, Leiting B, Leone JF, Lyons KA, Makarewicz AM, Patel RA, Petrov A, Wu JK, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2005 Jun 15;15(12):3048-52.

PMID:
15908206
43.

(2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.

Kim D, Wang L, Beconi M, Eiermann GJ, Fisher MH, He H, Hickey GJ, Kowalchick JE, Leiting B, Lyons K, Marsilio F, McCann ME, Patel RA, Petrov A, Scapin G, Patel SB, Roy RS, Wu JK, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE.

J Med Chem. 2005 Jan 13;48(1):141-51.

PMID:
15634008
44.

Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.

Caldwell CG, Chen P, He J, Parmee ER, Leiting B, Marsilio F, Patel RA, Wu JK, Eiermann GJ, Petrov A, He H, Lyons KA, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2004 Mar 8;14(5):1265-8.

PMID:
14980678
45.

4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.

Parmee ER, He J, Mastracchio A, Edmondson SD, Colwell L, Eiermann G, Feeney WP, Habulihaz B, He H, Kilburn R, Leiting B, Lyons K, Marsilio F, Patel RA, Petrov A, Di Salvo J, Wu JK, Thornberry NA, Weber AE.

Bioorg Med Chem Lett. 2004 Jan 5;14(1):43-6.

PMID:
14684294
46.

Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.

Hale JJ, Mills SG, MacCoss M, Finke PE, Cascieri MA, Sadowski S, Ber E, Chicchi GG, Kurtz M, Metzger J, Eiermann G, Tsou NN, Tattersall FD, Rupniak NM, Williams AR, Rycroft W, Hargreaves R, MacIntyre DE.

J Med Chem. 1998 Nov 5;41(23):4607-14.

PMID:
9804700
47.

Recombinant human interleukin-1 beta-induced increase in levels of proteoglycans, stromelysin, and leukocytes in rabbit synovial fluid.

McDonnell J, Hoerrner LA, Lark MW, Harper C, Dey T, Lobner J, Eiermann G, Kazazis D, Singer II, Moore VL.

Arthritis Rheum. 1992 Jul;35(7):799-805.

PMID:
1320383
48.

The role of CD18 in IL-8 induced dermal and synovial inflammation.

Forrest MJ, Eiermann GJ, Meurer R, Walakovits LA, MacIntyre DE.

Br J Pharmacol. 1992 Jun;106(2):287-94.

49.

Extensive laminin and basement membrane accumulation occurs at the onset of bleomycin-induced rodent pulmonary fibrosis.

Singer II, Kawka DW, McNally SM, Eiermann GJ, Metzger JM, Peterson LB.

Am J Pathol. 1986 Nov;125(2):258-68.

50.

Polymorphonuclear leukocyte participation in acute oleic-acid-induced lung injury.

Eiermann GJ, Dickey BF, Thrall RS.

Am Rev Respir Dis. 1983 Nov;128(5):845-50.

PMID:
6638672

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