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Items: 22

1.

Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.

Mandal M, Mitra K, Grotz D, Lin X, Palamanda J, Kumari P, Buevich A, Caldwell JP, Chen X, Cox K, Favreau L, Hyde L, Kennedy ME, Kuvelkar R, Liu X, Mazzola RD, Parker E, Rindgen D, Sherer E, Wang H, Zhu Z, Stamford AW, Cumming JN.

J Med Chem. 2018 Dec 13;61(23):10700-10708. doi: 10.1021/acs.jmedchem.8b01326. Epub 2018 Nov 15.

PMID:
30388368
2.

Discovery of a 3-(4-Pyrimidinyl) Indazole (MLi-2), an Orally Available and Selective Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitor that Reduces Brain Kinase Activity.

Scott JD, DeMong DE, Greshock TJ, Basu K, Dai X, Harris J, Hruza A, Li SW, Lin SI, Liu H, Macala MK, Hu Z, Mei H, Zhang H, Walsh P, Poirier M, Shi ZC, Xiao L, Agnihotri G, Baptista MA, Columbus J, Fell MJ, Hyde LA, Kuvelkar R, Lin Y, Mirescu C, Morrow JA, Yin Z, Zhang X, Zhou X, Chang RK, Embrey MW, Sanders JM, Tiscia HE, Drolet RE, Kern JT, Sur SM, Renger JJ, Bilodeau MT, Kennedy ME, Parker EM, Stamford AW, Nargund R, McCauley JA, Miller MW.

J Med Chem. 2017 Apr 13;60(7):2983-2992. doi: 10.1021/acs.jmedchem.7b00045. Epub 2017 Mar 16.

PMID:
28245354
3.

Discovery of the 3-Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)-A β-Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer's Disease.

Scott JD, Li SW, Brunskill AP, Chen X, Cox K, Cumming JN, Forman M, Gilbert EJ, Hodgson RA, Hyde LA, Jiang Q, Iserloh U, Kazakevich I, Kuvelkar R, Mei H, Meredith J, Misiaszek J, Orth P, Rossiter LM, Slater M, Stone J, Strickland CO, Voigt JH, Wang G, Wang H, Wu Y, Greenlee WJ, Parker EM, Kennedy ME, Stamford AW.

J Med Chem. 2016 Dec 8;59(23):10435-10450. Epub 2016 Nov 18.

PMID:
27933948
4.

The BACE1 inhibitor verubecestat (MK-8931) reduces CNS β-amyloid in animal models and in Alzheimer's disease patients.

Kennedy ME, Stamford AW, Chen X, Cox K, Cumming JN, Dockendorf MF, Egan M, Ereshefsky L, Hodgson RA, Hyde LA, Jhee S, Kleijn HJ, Kuvelkar R, Li W, Mattson BA, Mei H, Palcza J, Scott JD, Tanen M, Troyer MD, Tseng JL, Stone JA, Parker EM, Forman MS.

Sci Transl Med. 2016 Nov 2;8(363):363ra150.

PMID:
27807285
5.

TarO-specific inhibitors of wall teichoic acid biosynthesis restore β-lactam efficacy against methicillin-resistant staphylococci.

Lee SH, Wang H, Labroli M, Koseoglu S, Zuck P, Mayhood T, Gill C, Mann P, Sher X, Ha S, Yang SW, Mandal M, Yang C, Liang L, Tan Z, Tawa P, Hou Y, Kuvelkar R, DeVito K, Wen X, Xiao J, Batchlett M, Balibar CJ, Liu J, Xiao J, Murgolo N, Garlisi CG, Sheth PR, Flattery A, Su J, Tan C, Roemer T.

Sci Transl Med. 2016 Mar 9;8(329):329ra32. doi: 10.1126/scitranslmed.aad7364.

PMID:
26962156
6.

Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.

Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW.

J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22.

PMID:
26937601
7.

Discovery of potent iminoheterocycle BACE1 inhibitors.

Caldwell JP, Mazzola RD, Durkin J, Chen J, Chen X, Favreau L, Kennedy M, Kuvelkar R, Lee J, McHugh N, McKittrick B, Orth P, Stamford A, Strickland C, Voigt J, Wang L, Zhang L, Zhang Q, Zhu Z.

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5455-9. doi: 10.1016/j.bmcl.2014.10.006. Epub 2014 Oct 23.

PMID:
25455483
8.

Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.

Stamford AW, Scott JD, Li SW, Babu S, Tadesse D, Hunter R, Wu Y, Misiaszek J, Cumming JN, Gilbert EJ, Huang C, McKittrick BA, Hong L, Guo T, Zhu Z, Strickland C, Orth P, Voigt JH, Kennedy ME, Chen X, Kuvelkar R, Hodgson R, Hyde LA, Cox K, Favreau L, Parker EM, Greenlee WJ.

ACS Med Chem Lett. 2012 Nov 8;3(11):897-902. Epub 2012 Jul 12.

9.

Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.

Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW.

J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1.

PMID:
22989333
10.

Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.

Cumming JN, Smith EM, Wang L, Misiaszek J, Durkin J, Pan J, Iserloh U, Wu Y, Zhu Z, Strickland C, Voigt J, Chen X, Kennedy ME, Kuvelkar R, Hyde LA, Cox K, Favreau L, Czarniecki MF, Greenlee WJ, McKittrick BA, Parker EM, Stamford AW.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2444-9. doi: 10.1016/j.bmcl.2012.02.013. Epub 2012 Feb 16.

PMID:
22390835
11.

Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.

Cumming J, Babu S, Huang Y, Carrol C, Chen X, Favreau L, Greenlee W, Guo T, Kennedy M, Kuvelkar R, Le T, Li G, McHugh N, Orth P, Ozgur L, Parker E, Saionz K, Stamford A, Strickland C, Tadesse D, Voigt J, Zhang L, Zhang Q.

Bioorg Med Chem Lett. 2010 May 1;20(9):2837-42. doi: 10.1016/j.bmcl.2010.03.050. Epub 2010 Mar 12.

PMID:
20347593
12.

Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.

Zhu Z, Sun ZY, Ye Y, Voigt J, Strickland C, Smith EM, Cumming J, Wang L, Wong J, Wang YS, Wyss DF, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Parker E, McKittrick BA, Stamford A, Czarniecki M, Greenlee W, Hunter JC.

J Med Chem. 2010 Feb 11;53(3):951-65. doi: 10.1021/jm901408p.

PMID:
20043696
13.

Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.

Cumming JN, Le TX, Babu S, Carroll C, Chen X, Favreau L, Gaspari P, Guo T, Hobbs DW, Huang Y, Iserloh U, Kennedy ME, Kuvelkar R, Li G, Lowrie J, McHugh NA, Ozgur L, Pan J, Parker EM, Saionz K, Stamford AW, Strickland C, Tadesse D, Voigt J, Wang L, Wu Y, Zhang L, Zhang Q.

Bioorg Med Chem Lett. 2008 Jun 1;18(11):3236-41. doi: 10.1016/j.bmcl.2008.04.050. Epub 2008 Apr 25. Erratum in: Bioorg Med Chem Lett. 2008 Aug 1;18(15):4447.

PMID:
18468890
14.

Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.

Iserloh U, Wu Y, Cumming JN, Pan J, Wang LY, Stamford AW, Kennedy ME, Kuvelkar R, Chen X, Parker EM, Strickland C, Voigt J.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):414-7. Epub 2007 Nov 6.

PMID:
18023580
15.

Differential inhibitor sensitivity between human recombinant and native photoreceptor cGMP-phosphodiesterases (PDE6s).

Zhang J, Kuvelkar R, Wu P, Egan RW, Billah MM, Wang P.

Biochem Pharmacol. 2004 Sep 1;68(5):867-73.

PMID:
15294449
16.

Induction of lysosomal and plasma membrane-bound sialidases in human T-cells via T-cell receptor.

Wang P, Zhang J, Bian H, Wu P, Kuvelkar R, Kung TT, Crawley Y, Egan RW, Billah MM.

Biochem J. 2004 Jun 1;380(Pt 2):425-33.

17.

Mapping and characterization of the epitope(s) of Sch 55700, a humanized mAb, that inhibits human IL-5.

Zhang J, Kuvelkar R, Murgolo NJ, Taremi SS, Chou CC, Wang P, Billah MM, Egan RW.

Int Immunol. 1999 Dec;11(12):1935-44.

PMID:
10590259
18.

A scintillation proximity assay for human interleukin-5 (hIL-5) high-affinity binding in insect cells coexpressing hIL-5 receptor alpha and beta subunits.

Zhang J, Wu P, Kuvelkar R, Schwartz JL, Egan RW, Billah MM, Wang P.

Anal Biochem. 1999 Mar 1;268(1):134-42.

PMID:
10036172
19.

Evidence for multiple promoters of the human IL-5 receptor alpha subunit gene: a novel 6-base pair element determines cell-specific promoter function.

Zhang J, Kuvelkar R, Cheewatrakoolpong B, Williams S, Egan RW, Billah MM.

J Immunol. 1997 Dec 1;159(11):5412-21.

PMID:
9548481
20.

Clonogenic potential of myeloid leukaemia cells in vitro is restricted to leukaemia cells expressing the CD34 antigen.

Yin M, Silvestri FF, Banavali SD, Gopal V, Hulette BC, Kuvelkar RB, Young AN, Mayers G, Preisler HD.

Eur J Cancer. 1993;29A(16):2279-83.

PMID:
7509165
21.

c-myc and c-myb expression in acute myelogenous leukemia.

Gopal V, Hulette B, Li YQ, Kuvelkar R, Raza A, Larson R, Goldberg J, Tricot G, Bennett J, Preisler H.

Leuk Res. 1992 Oct;16(10):1003-11.

PMID:
1405703
22.

High c-myc protein expression in benign colorectal lesions correlates with the degree of dysplasia.

Pavelic ZP, Pavelic L, Kuvelkar R, Gapany SR.

Anticancer Res. 1992 Jan-Feb;12(1):171-5.

PMID:
1567165

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