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Items: 31


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.


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.


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.


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.


Structure-based design of β-site APP cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease.

Yuan J, Venkatraman S, Zheng Y, McKeever BM, Dillard LW, Singh SB.

J Med Chem. 2013 Jun 13;56(11):4156-80. doi: 10.1021/jm301659n. Epub 2013 Apr 5. Review.


New renin inhibitor VTP-27999 alters renin immunoreactivity and does not unfold prorenin.

Krop M, Lu X, Verdonk K, Schalekamp MA, van Gool JM, McKeever BM, Gregg R, Danser AH.

Hypertension. 2013 May;61(5):1075-82. doi: 10.1161/HYPERTENSIONAHA.111.00967. Epub 2013 Mar 4.


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.


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.


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.


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.


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.


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.


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.


Expression, purification and crystallization of human 5-lipoxygenase-activating protein with leukotriene-biosynthesis inhibitors.

Xu S, McKeever BM, Wisniewski D, Miller DK, Spencer RH, Chu L, Ujjainwalla F, Yamin TT, Evans JF, Becker JW, Ferguson AD.

Acta Crystallogr Sect F Struct Biol Cryst Commun. 2007 Dec 1;63(Pt 12):1054-7. Epub 2007 Nov 30.


Crystal structure of inhibitor-bound human 5-lipoxygenase-activating protein.

Ferguson AD, McKeever BM, Xu S, Wisniewski D, Miller DK, Yamin TT, Spencer RH, Chu L, Ujjainwalla F, Cunningham BR, Evans JF, Becker JW.

Science. 2007 Jul 27;317(5837):510-2. Epub 2007 Jun 28.


The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands.

Wilkening RR, Ratcliffe RW, Tynebor EC, Wildonger KJ, Fried AK, Hammond ML, Mosley RT, Fitzgerald PM, Sharma N, McKeever BM, Nilsson S, Carlquist M, Thorsell A, Locco L, Katz R, Frisch K, Birzin ET, Wilkinson HA, Mitra S, Cai S, Hayes EC, Schaeffer JM, Rohrer SP.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3489-94. Epub 2006 May 2.


Design and synthesis of alpha-aryloxyphenylacetic acid derivatives: a novel class of PPARalpha/gamma dual agonists with potent antihyperglycemic and lipid modulating activity.

Shi GQ, Dropinski JF, McKeever BM, Xu S, Becker JW, Berger JP, MacNaul KL, Elbrecht A, Zhou G, Doebber TW, Wang P, Chao YS, Forrest M, Heck JV, Moller DE, Jones AB.

J Med Chem. 2005 Jun 30;48(13):4457-68.


Amino acid substitution of arginine 80 in 17beta-hydroxysteroid dehydrogenase type 3 and its effect on NADPH cofactor binding and oxidation/reduction kinetics.

McKeever BM, Hawkins BK, Geissler WM, Wu L, Sheridan RP, Mosley RT, Andersson S.

Biochim Biophys Acta. 2002 Nov 19;1601(1):29-37.


The three-dimensional structure of human granzyme B compared to caspase-3, key mediators of cell death with cleavage specificity for aspartic acid in P1.

Rotonda J, Garcia-Calvo M, Bull HG, Geissler WM, McKeever BM, Willoughby CA, Thornberry NA, Becker JW.

Chem Biol. 2001 Apr;8(4):357-68.


Positions of His-64 and a bound water in human carbonic anhydrase II upon binding three structurally related inhibitors.

Smith GM, Alexander RS, Christianson DW, McKeever BM, Ponticello GS, Springer JP, Randall WC, Baldwin JJ, Habecker CN.

Protein Sci. 1994 Jan;3(1):118-25.


FK-506-binding protein: three-dimensional structure of the complex with the antagonist L-685,818.

Becker JW, Rotonda J, McKeever BM, Chan HK, Marcy AI, Wiederrecht G, Hermes JD, Springer JP.

J Biol Chem. 1993 May 25;268(15):11335-9.


Site-directed mutagenesis of glutathione S-transferase YaYa. Important roles of tyrosine 9 and aspartic acid 101 in catalysis.

Wang RW, Newton DJ, Huskey SE, McKeever BM, Pickett CB, Lu AY.

J Biol Chem. 1992 Oct 5;267(28):19866-71.


Synthesis and antiviral activity of a series of HIV-1 protease inhibitors with functionality tethered to the P1 or P1' phenyl substituents: X-ray crystal structure assisted design.

Thompson WJ, Fitzgerald PM, Holloway MK, Emini EA, Darke PL, McKeever BM, Schleif WA, Quintero JC, Zugay JA, Tucker TJ, et al.

J Med Chem. 1992 May 15;35(10):1685-701.


Coalitions and spiraling health care costs.

Perkins JA, McKeever BM.

Bus Health. 1991 Sep 15;9(10):42, 44-5. No abstract available.


New isomeric classes of topically active ocular hypotensive carbonic anhydrase inhibitors: 5-substituted thieno[2,3-b]thiophene-2-sulfonamides and 5-substituted thieno[3,2-b]thiophene-2-sulfonamides.

Prugh JD, Hartman GD, Mallorga PJ, McKeever BM, Michelson SR, Murcko MA, Schwam H, Smith RL, Sondey JM, Springer JP, et al.

J Med Chem. 1991 Jun;34(6):1805-18.


Crystallographic analysis of a complex between human immunodeficiency virus type 1 protease and acetyl-pepstatin at 2.0-A resolution.

Fitzgerald PM, McKeever BM, VanMiddlesworth JF, Springer JP, Heimbach JC, Leu CT, Herber WK, Dixon RA, Darke PL.

J Biol Chem. 1990 Aug 25;265(24):14209-19.


Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1.

Navia MA, Fitzgerald PM, McKeever BM, Leu CT, Heimbach JC, Herber WK, Sigal IS, Darke PL, Springer JP.

Nature. 1989 Feb 16;337(6208):615-20.


Crystallization of the aspartylprotease from the human immunodeficiency virus, HIV-1.

McKeever BM, Navia MA, Fitzgerald PM, Springer JP, Leu CT, Heimbach JC, Herbert WK, Sigal IS, Darke PL.

J Biol Chem. 1989 Feb 5;264(4):1919-21.


Structure of human neutrophil elastase in complex with a peptide chloromethyl ketone inhibitor at 1.84-A resolution.

Navia MA, McKeever BM, Springer JP, Lin TY, Williams HR, Fluder EM, Dorn CP, Hoogsteen K.

Proc Natl Acad Sci U S A. 1989 Jan;86(1):7-11.


Crystallization of human neutrophil elastase.

Williams HR, Lin TY, Navia MA, Springer JP, McKeever BM, Hoogsteen K, Dorn CP Jr.

J Biol Chem. 1987 Dec 15;262(35):17178-81.

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