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Items: 20

1.

Bone marrow niches of germline FANCC/FANCG deficient mice enable efficient and durable engraftment of hematopoietic stem cells after transplantation.

Zha J, Kunselman L, Fan JM, Olson TS.

Haematologica. 2019 Jul;104(7):e284-e287. doi: 10.3324/haematol.2018.202143. Epub 2019 Jan 24. No abstract available.

2.

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
3.

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
4.

Discovery and Preclinical Evaluation of BMS-711939, an Oxybenzylglycine Based PPARα Selective Agonist.

Shi Y, Li J, Kennedy LJ, Tao S, Hernández AS, Lai Z, Chen S, Wong H, Zhu J, Trehan A, Lim NK, Zhang H, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Muckelbauer J, Chang C, Krystek SR, Li YX, Hosagrahara V, Zhang L, Kadiyala P, Xu C, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA.

ACS Med Chem Lett. 2016 Apr 4;7(6):590-4. doi: 10.1021/acsmedchemlett.6b00033. eCollection 2016 Jun 9.

5.

Synthesis and biological evaluation of novel pyrrolidine acid analogs as potent dual PPARα/γ agonists.

Zhang H, Ding CZ, Lai Z, Chen SS, Devasthale P, Herpin T, Morton G, Qu F, Ryono D, Smirk R, Wang W, Wu S, Ye XX, Li YX, Apedo A, Farrelly D, Wang T, Gu L, Morgan N, Flynn N, Chu C, Kunselman L, Lippy J, Locke K, O'Malley K, Harrity T, Cap M, Zhang L, Hosagrahara V, Kadiyala P, Xu C, Doweyko AM, Zahler R, Hariharan N, Cheng PT.

Bioorg Med Chem Lett. 2015 Mar 15;25(6):1196-205. doi: 10.1016/j.bmcl.2015.01.066. Epub 2015 Feb 4.

PMID:
25686852
6.

Discovery of 3-hydroxy-4-cyano-isoquinolines as novel, potent, and selective inhibitors of human 11β-hydroxydehydrogenase 1 (11β-HSD1).

Wu SC, Yoon D, Chin J, van Kirk K, Seethala R, Golla R, He B, Harrity T, Kunselman LK, Morgan NN, Ponticiello RP, Taylor JR, Zebo R, Harper TW, Li W, Wang M, Zhang L, Sleczka BG, Nayeem A, Sheriff S, Camac DM, Morin PE, Everlof JG, Li YX, Ferraro CA, Kieltyka K, Shou W, Vath MB, Zvyaga TA, Gordon DA, Robl JA.

Bioorg Med Chem Lett. 2011 Nov 15;21(22):6693-8. doi: 10.1016/j.bmcl.2011.09.058. Epub 2011 Sep 21.

PMID:
21983444
7.

Discovery of an oxybenzylglycine based peroxisome proliferator activated receptor alpha selective agonist 2-((3-((2-(4-chlorophenyl)-5-methyloxazol-4-yl)methoxy)benzyl)(methoxycarbonyl)amino)acetic acid (BMS-687453).

Li J, Kennedy LJ, Shi Y, Tao S, Ye XY, Chen SY, Wang Y, Hernández AS, Wang W, Devasthale PV, Chen S, Lai Z, Zhang H, Wu S, Smirk RA, Bolton SA, Ryono DE, Zhang H, Lim NK, Chen BC, Locke KT, O'Malley KM, Zhang L, Srivastava RA, Miao B, Meyers DS, Monshizadegan H, Search D, Grimm D, Zhang R, Harrity T, Kunselman LK, Cap M, Kadiyala P, Hosagrahara V, Zhang L, Xu C, Li YX, Muckelbauer JK, Chang C, An Y, Krystek SR, Blanar MA, Zahler R, Mukherjee R, Cheng PT, Tino JA.

J Med Chem. 2010 Apr 8;53(7):2854-64. doi: 10.1021/jm9016812.

PMID:
20218621
8.

Design, synthesis and structure-activity relationships of azole acids as novel, potent dual PPAR alpha/gamma agonists.

Zhang H, Ryono DE, Devasthale P, Wang W, O'Malley K, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Locke K, Zhang L, Lippy J, Kunselman L, Morgan N, Flynn N, Moore L, Hosagrahara V, Zhang L, Kadiyala P, Xu C, Doweyko AM, Bell A, Chang C, Muckelbauer J, Zahler R, Hariharan N, Cheng PT.

Bioorg Med Chem Lett. 2009 Mar 1;19(5):1451-6. doi: 10.1016/j.bmcl.2009.01.030. Epub 2009 Jan 15.

PMID:
19201606
9.

Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.

Wang W, Devasthale P, Farrelly D, Gu L, Harrity T, Cap M, Chu C, Kunselman L, Morgan N, Ponticiello R, Zebo R, Zhang L, Locke K, Lippy J, O'Malley K, Hosagrahara V, Zhang L, Kadiyala P, Chang C, Muckelbauer J, Doweyko AM, Zahler R, Ryono D, Hariharan N, Cheng PT.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1939-44. doi: 10.1016/j.bmcl.2008.01.126. Epub 2008 Feb 7.

PMID:
18291645
10.

The Guinea pig as a preclinical model for demonstrating the efficacy and safety of statins.

Madsen CS, Janovitz E, Zhang R, Nguyen-Tran V, Ryan CS, Yin X, Monshizadegan H, Chang M, D'Arienzo C, Scheer S, Setters R, Search D, Chen X, Zhuang S, Kunselman L, Peters A, Harrity T, Apedo A, Huang C, Cuff CA, Kowala MC, Blanar MA, Sun CQ, Robl JA, Stein PD.

J Pharmacol Exp Ther. 2008 Feb;324(2):576-86. Epub 2007 Nov 6.

PMID:
17986646
11.

The dual peroxisome proliferator-activated receptor alpha/gamma activator muraglitazar prevents the natural progression of diabetes in db/db mice.

Tozzo E, Ponticiello R, Swartz J, Farrelly D, Zebo R, Welzel G, Egan D, Kunselman L, Peters A, Gu L, French M, Chen S, Devasthale P, Janovitz E, Staal A, Harrity T, Belder R, Cheng PT, Whaley J, Taylor S, Hariharan N.

J Pharmacol Exp Ther. 2007 Apr;321(1):107-15. Epub 2007 Jan 26.

PMID:
17259449
12.

Muraglitazar, a novel dual (alpha/gamma) peroxisome proliferator-activated receptor activator, improves diabetes and other metabolic abnormalities and preserves beta-cell function in db/db mice.

Harrity T, Farrelly D, Tieman A, Chu C, Kunselman L, Gu L, Ponticiello R, Cap M, Qu F, Shao C, Wang W, Zhang H, Fenderson W, Chen S, Devasthale P, Jeon Y, Seethala R, Yang WP, Ren J, Zhou M, Ryono D, Biller S, Mookhtiar KA, Wetterau J, Gregg R, Cheng PT, Hariharan N.

Diabetes. 2006 Jan;55(1):240-8.

13.

5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.

Sulsky R, Robl JA, Biller SA, Harrity TW, Wetterau J, Connolly F, Jolibois K, Kunselman L.

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5067-70.

PMID:
15380200
14.

Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.

Magnin DR, Biller SA, Wetterau J, Robl JA, Dickson JK Jr, Taunk P, Harrity TW, Lawrence RM, Sun CQ, Wang T, Logan J, Fryszman O, Connolly F, Jolibois K, Kunselman L.

Bioorg Med Chem Lett. 2003 Apr 7;13(7):1337-40.

PMID:
12657277
15.

A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors.

Robl JA, Sulsky R, Sun CQ, Simpkins LM, Wang T, Dickson JK Jr, Chen Y, Magnin DR, Taunk P, Slusarchyk WA, Biller SA, Lan SJ, Connolly F, Kunselman LK, Sabrah T, Jamil H, Gordon D, Harrity TW, Wetterau JR.

J Med Chem. 2001 Mar 15;44(6):851-6.

PMID:
11300866
16.

An MTP inhibitor that normalizes atherogenic lipoprotein levels in WHHL rabbits.

Wetterau JR, Gregg RE, Harrity TW, Arbeeny C, Cap M, Connolly F, Chu CH, George RJ, Gordon DA, Jamil H, Jolibois KG, Kunselman LK, Lan SJ, Maccagnan TJ, Ricci B, Yan M, Young D, Chen Y, Fryszman OM, Logan JV, Musial CL, Poss MA, Robl JA, Simpkins LM, Slusarchyk WA, Sulsky R, Taunk P, Magnin DR, Tino JA, Lawrence RM, Dickson JK Jr, Biller SA.

Science. 1998 Oct 23;282(5389):751-4.

17.

Orally active squalene synthase inhibitors: bis((acyloxy)alkyl) prodrugs of the alpha-phosphonosulfonic acid moiety.

Dickson JK Jr, Biller SA, Magnin DR, Petrillo EW Jr, Hillyer JW, Hsieh DC, Lan SJ, Rinehart JK, Gregg RE, Harrity TW, Jolibois KG, Kalinowski SS, Kunselman LK, Mookhtiar KA, Ciosek CP Jr.

J Med Chem. 1996 Feb 2;39(3):661-4. No abstract available.

PMID:
8576906
18.

alpha-Phosphonosulfonic acids: potent and selective inhibitors of squalene synthase.

Magnin DR, Biller SA, Chen Y, Dickson JK Jr, Fryszman OM, Lawrence RM, Logan JV, Sieber-McMaster ES, Sulsky RB, Traeger SC, Hsieh DC, Lan SJ, Rinehart JK, Harrity TW, Jolibois KG, Kunselman LK, Rich LC, Slusarchyk DA, Ciosek CP Jr.

J Med Chem. 1996 Feb 2;39(3):657-60. No abstract available.

PMID:
8576905
19.

Lipophilic 1,1-bisphosphonates are potent squalene synthase inhibitors and orally active cholesterol lowering agents in vivo.

Ciosek CP Jr, Magnin DR, Harrity TW, Logan JV, Dickson JK Jr, Gordon EM, Hamilton KA, Jolibois KG, Kunselman LK, Lawrence RM, et al.

J Biol Chem. 1993 Nov 25;268(33):24832-7.

20.

Amphotericin B lipid complex therapy of experimental fungal infections in mice.

Clark JM, Whitney RR, Olsen SJ, George RJ, Swerdel MR, Kunselman L, Bonner DP.

Antimicrob Agents Chemother. 1991 Apr;35(4):615-21.

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