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Items: 34

1.

Therapeutic targeting of preleukemia cells in a mouse model of NPM1 mutant acute myeloid leukemia.

Uckelmann HJ, Kim SM, Wong EM, Hatton C, Giovinazzo H, Gadrey JY, Krivtsov AV, Rücker FG, Döhner K, McGeehan GM, Levine RL, Bullinger L, Vassiliou GS, Armstrong SA.

Science. 2020 Jan 31;367(6477):586-590. doi: 10.1126/science.aax5863.

PMID:
32001657
2.

A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia.

Krivtsov AV, Evans K, Gadrey JY, Eschle BK, Hatton C, Uckelmann HJ, Ross KN, Perner F, Olsen SN, Pritchard T, McDermott L, Jones CD, Jing D, Braytee A, Chacon D, Earley E, McKeever BM, Claremon D, Gifford AJ, Lee HJ, Teicher BA, Pimanda JE, Beck D, Perry JA, Smith MA, McGeehan GM, Lock RB, Armstrong SA.

Cancer Cell. 2019 Dec 9;36(6):660-673.e11. doi: 10.1016/j.ccell.2019.11.001.

PMID:
31821784
3.

Discovery of Potent Inhibitors of 11β-Hydroxysteroid Dehydrogenase Type 1 Using a Novel Growth-Based Protocol of in Silico Screening and Optimization in CONTOUR.

Liu Z, Singh SB, Zheng Y, Lindblom P, Tice C, Dong C, Zhuang L, Zhao Y, Kruk BA, Lala D, Claremon DA, McGeehan GM, Gregg RD, Cain R.

J Chem Inf Model. 2019 Aug 26;59(8):3422-3436. doi: 10.1021/acs.jcim.9b00198. Epub 2019 Aug 8.

PMID:
31355641
4.

Discovery of BI 135585, an in vivo efficacious oxazinanone-based 11β hydroxysteroid dehydrogenase type 1 inhibitor.

Zhuang L, Tice CM, Xu Z, Zhao W, Cacatian S, Ye YJ, Singh SB, Lindblom P, McKeever BM, Krosky PM, Zhao Y, Lala D, Kruk BA, Meng S, Howard L, Johnson JA, Bukhtiyarov Y, Panemangalore R, Guo J, Guo R, Himmelsbach F, Hamilton B, Schuler-Metz A, Schauerte H, Gregg R, McGeehan GM, Leftheris K, Claremon DA.

Bioorg Med Chem. 2017 Jul 15;25(14):3649-3657. doi: 10.1016/j.bmc.2017.04.033. Epub 2017 Apr 29.

PMID:
28528082
5.

Brain penetrant liver X receptor (LXR) modulators based on a 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole core.

Tice CM, Noto PB, Fan KY, Zhao W, Lotesta SD, Dong C, Marcus AP, Zheng YJ, Chen G, Wu Z, Van Orden R, Zhou J, Bukhtiyarov Y, Zhao Y, Lipinski K, Howard L, Guo J, Kandpal G, Meng S, Hardy A, Krosky P, Gregg RE, Leftheris K, McKeever BM, Singh SB, Lala D, McGeehan GM, Zhuang L, Claremon DA.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):5044-5050. doi: 10.1016/j.bmcl.2016.08.089. Epub 2016 Aug 29.

PMID:
27599745
6.

Influence of sub-chronic selective 11β-hydroxysteroid dehydrogenase 1 inhibition on the hypothalamic-pituitary-adrenal axis in female cynomolgus monkeys.

Hamilton BS, Schoelch C, Schuler-Metz A, Krosky P, Lala DS, Claremon DA, McGeehan GM.

Eur J Pharmacol. 2016 Oct 15;789:68-74. doi: 10.1016/j.ejphar.2016.07.004. Epub 2016 Jul 5.

PMID:
27393460
7.

Discovery of a Novel, Orally Efficacious Liver X Receptor (LXR) β Agonist.

Zheng Y, Zhuang L, Fan KY, Tice CM, Zhao W, Dong C, Lotesta SD, Leftheris K, Lindblom PR, Liu Z, Shimada J, Noto PB, Meng S, Hardy A, Howard L, Krosky P, Guo J, Lipinski K, Kandpal G, Bukhtiyarov Y, Zhao Y, Lala D, Van Orden R, Zhou J, Chen G, Wu Z, McKeever BM, McGeehan GM, Gregg RE, Claremon DA, Singh SB.

J Med Chem. 2016 Apr 14;59(7):3264-71. doi: 10.1021/acs.jmedchem.5b02029. Epub 2016 Mar 29.

PMID:
26990539
8.

Identification of spirooxindole and dibenzoxazepine motifs as potent mineralocorticoid receptor antagonists.

Lotesta SD, Marcus AP, Zheng Y, Leftheris K, Noto PB, Meng S, Kandpal G, Chen G, Zhou J, McKeever B, Bukhtiyarov Y, Zhao Y, Lala DS, Singh SB, McGeehan GM.

Bioorg Med Chem. 2016 Mar 15;24(6):1384-91. doi: 10.1016/j.bmc.2016.02.014. Epub 2016 Feb 9.

PMID:
26897089
9.

Pharmacological characterization of the selective 11β-hydroxysteroid dehydrogenase 1 inhibitor, BI 135585, a clinical candidate for the treatment of type 2 diabetes.

Hamilton BS, Himmelsbach F, Nar H, Schuler-Metz A, Krosky P, Guo J, Guo R, Meng S, Zhao Y, Lala DS, Zhuang L, Claremon DA, McGeehan GM.

Eur J Pharmacol. 2015 Jan 5;746:50-5. doi: 10.1016/j.ejphar.2014.10.053. Epub 2014 Nov 8.

PMID:
25445047
10.

Regulation of sphingomyelin phosphodiesterase acid-like 3A gene (SMPDL3A) by liver X receptors.

Noto PB, Bukhtiyarov Y, Shi M, McKeever BM, McGeehan GM, Lala DS.

Mol Pharmacol. 2012 Oct;82(4):719-27. Epub 2012 Jul 18.

PMID:
22810003
11.

Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.

Jia L, Simpson RD, Yuan J, Xu Z, Zhao W, Cacatian S, Tice CM, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Bukhtiyarov Y, Johnson JA, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.

ACS Med Chem Lett. 2011 Aug 9;2(10):747-51. doi: 10.1021/ml200137x. eCollection 2011 Oct 13.

12.

Structure-based design and synthesis of 1,3-oxazinan-2-one inhibitors of 11β-hydroxysteroid dehydrogenase type 1.

Xu Z, Tice CM, Zhao W, Cacatian S, Ye YJ, Singh SB, Lindblom P, McKeever BM, Krosky PM, Kruk BA, Berbaum J, Harrison RK, Johnson JA, Bukhtiyarov Y, Panemangalore R, Scott BB, Zhao Y, Bruno JG, Togias J, Guo J, Guo R, Carroll PJ, McGeehan GM, Zhuang L, He W, Claremon DA.

J Med Chem. 2011 Sep 8;54(17):6050-62. doi: 10.1021/jm2005354. Epub 2011 Aug 4.

PMID:
21786805
13.

Biphenyl/diphenyl ether renin inhibitors: filling the S1 pocket of renin via the S3 pocket.

Yuan J, Simpson RD, Zhao W, Tice CM, Xu Z, Cacatian S, Jia L, Flaherty PT, Guo J, Ishchenko A, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Panemangalore R, Bentley R, Doe CP, Harrison RK, McGeehan GM, Singh SB, Dillard LW, Baldwin JJ, Claremon DA.

Bioorg Med Chem Lett. 2011 Aug 15;21(16):4836-43. doi: 10.1016/j.bmcl.2011.06.043. Epub 2011 Jun 17.

PMID:
21741239
14.

Discovery and optimization of adamantyl carbamate inhibitors of 11β-HSD1.

Tice CM, Zhao W, Krosky PM, Kruk BA, Berbaum J, Johnson JA, Bukhtiyarov Y, Panemangalore R, Scott BB, Zhao Y, Bruno JG, Howard L, Togias J, Ye YJ, Singh SB, McKeever BM, Lindblom PR, Guo J, Guo R, Nar H, Schuler-Metz A, Gregg RE, Leftheris K, Harrison RK, McGeehan GM, Zhuang L, Claremon DA.

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6725-9. doi: 10.1016/j.bmcl.2010.08.142. Epub 2010 Sep 7.

PMID:
20864344
15.

Spirocyclic ureas: orally bioavailable 11 beta-HSD1 inhibitors identified by computer-aided drug design.

Tice CM, Zhao W, Xu Z, Cacatian ST, Simpson RD, Ye YJ, Singh SB, McKeever BM, Lindblom P, Guo J, Krosky PM, Kruk BA, Berbaum J, Harrison RK, Johnson JJ, Bukhtiyarov Y, Panemangalore R, Scott BB, Zhao Y, Bruno JG, Zhuang L, McGeehan GM, He W, Claremon DA.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):881-6. doi: 10.1016/j.bmcl.2009.12.082. Epub 2010 Jan 4.

PMID:
20064717
16.

Optimization of orally bioavailable alkyl amine renin inhibitors.

Xu Z, Cacatian S, Yuan J, Simpson RD, Jia L, Zhao W, Tice CM, Flaherty PT, Guo J, Ishchenko A, Singh SB, Wu Z, McKeever BM, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Bentley R, Doe CP, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):694-9. doi: 10.1016/j.bmcl.2009.11.066. Epub 2009 Dec 1.

PMID:
19959358
17.

Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.

Tice CM, Xu Z, Yuan J, Simpson RD, Cacatian ST, Flaherty PT, Zhao W, Guo J, Ishchenko A, Singh SB, Wu Z, Scott BB, Bukhtiyarov Y, Berbaum J, Mason J, Panemangalore R, Cappiello MG, Müller D, Harrison RK, McGeehan GM, Dillard LW, Baldwin JJ, Claremon DA.

Bioorg Med Chem Lett. 2009 Jul 1;19(13):3541-5. doi: 10.1016/j.bmcl.2009.04.140. Epub 2009 May 5.

PMID:
19457666
18.

Purification and characterization of recombinant human renin for X-ray crystallization studies.

Wu Z, Cappiello MG, Scott BB, Bukhtiyarov Y, McGeehan GM.

BMC Biochem. 2008 Jun 26;9:19. doi: 10.1186/1471-2091-9-19.

19.

Cloning, characterization and site-directed mutagenesis of canine renin.

Bukhtiyarov Y, Zecher M, Panemangalore R, Wu Z, Bruno JG, Yuan J, Xu Z, Dillard LW, McGeehan GM, Harrison RK, Scott BB.

J Biochem. 2007 Dec;142(6):671-80. Epub 2007 Oct 17.

PMID:
17942478
20.

Development of inhibitors of the aspartyl protease renin for the treatment of hypertension.

Scott BB, McGeehan GM, Harrison RK.

Curr Protein Pept Sci. 2006 Jun;7(3):241-54. Review.

PMID:
16787263
21.

Purification and characterization of recombinant human cathepsin E expressed in human kidney cell line 293.

Cappiello MG, Wu Z, Scott BB, McGeehan GM, Harrison RK.

Protein Expr Purif. 2004 Sep;37(1):53-60.

PMID:
15294281
23.

Method to analyze collagenase and gelatinase activity by fibroblasts in culture.

Gould LJ, Yager DR, McGeehan GM, Diegelmann RF.

In Vitro Cell Dev Biol Anim. 1999 Feb;35(2):75-9.

PMID:
10475260
24.

Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.

Groneberg RD, Burns CJ, Morrissette MM, Ullrich JW, Morris RL, Darnbrough S, Djuric SW, Condon SM, McGeehan GM, Labaudiniere R, Neuenschwander K, Scotese AC, Kline JA.

J Med Chem. 1999 Feb 25;42(4):541-4. No abstract available.

PMID:
10052961
25.

Effect of matrix metalloproteinase inhibitors on tumor growth and spontaneous metastasis.

Conway JG, Trexler SJ, Wakefield JA, Marron BE, Emerson DL, Bickett DM, Deaton DN, Garrison D, Elder M, McElroy A, Willmott N, Dockerty AJ, McGeehan GM.

Clin Exp Metastasis. 1996 Mar;14(2):115-24.

PMID:
8605725
26.

Monoclonal antibodies against human collagenase and stromelysin.

Su JL, Becherer JD, Edwards C, Bukhart W, McGeehan GM, Champion BR.

Hybridoma. 1995 Aug;14(4):383-90.

PMID:
8522351
27.

Defined substrate mixtures for mapping of proteinase specificities.

McGeehan GM, Bickett DM, Wiseman JS, Green M, Berman J.

Methods Enzymol. 1995;248:35-46. No abstract available.

PMID:
7674932
28.

Characterization of the peptide substrate specificities of interstitial collagenase and 92-kDa gelatinase. Implications for substrate optimization.

McGeehan GM, Bickett DM, Green M, Kassel D, Wiseman JS, Berman J.

J Biol Chem. 1994 Dec 30;269(52):32814-20.

29.

A high throughput fluorogenic substrate for stromelysin (MMP-3).

Bickett DM, Green MD, Wagner C, Roth JT, Berman J, McGeehan GM.

Ann N Y Acad Sci. 1994 Sep 6;732:351-5.

PMID:
7978805
30.

Regulation of tumour necrosis factor-alpha processing by a metalloproteinase inhibitor.

McGeehan GM, Becherer JD, Bast RC Jr, Boyer CM, Champion B, Connolly KM, Conway JG, Furdon P, Karp S, Kidao S, et al.

Nature. 1994 Aug 18;370(6490):558-61.

PMID:
8052311
31.

Isotope effects and alternative substrate reactivities for tryptophan 2,3-dioxygenase.

Leeds JM, Brown PJ, McGeehan GM, Brown FK, Wiseman JS.

J Biol Chem. 1993 Aug 25;268(24):17781-6.

32.

A high throughput fluorogenic substrate for interstitial collagenase (MMP-1) and gelatinase (MMP-9).

Bickett DM, Green MD, Berman J, Dezube M, Howe AS, Brown PJ, Roth JT, McGeehan GM.

Anal Biochem. 1993 Jul;212(1):58-64.

PMID:
8368516
33.

The ribonuclease from an extinct bovid ruminant.

Stackhouse J, Presnell SR, McGeehan GM, Nambiar KP, Benner SA.

FEBS Lett. 1990 Mar 12;262(1):104-6.

34.

An improved system for expressing pancreatic ribonuclease in Escherichia coli.

McGeehan GM, Benner SA.

FEBS Lett. 1989 Apr 10;247(1):55-6.

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