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Items: 31

1.

MK-8353: Discovery of an Orally Bioavailable Dual Mechanism ERK Inhibitor for Oncology.

Boga SB, Deng Y, Zhu L, Nan Y, Cooper AB, Shipps GW Jr, Doll R, Shih NY, Zhu H, Sun R, Wang T, Paliwal S, Tsui HC, Gao X, Yao X, Desai J, Wang J, Alhassan AB, Kelly J, Patel M, Muppalla K, Gudipati S, Zhang LK, Buevich A, Hesk D, Carr D, Dayananth P, Black S, Mei H, Cox K, Sherborne B, Hruza AW, Xiao L, Jin W, Long B, Liu G, Taylor SA, Kirschmeier P, Windsor WT, Bishop R, Samatar AA.

ACS Med Chem Lett. 2018 Jun 14;9(7):761-767. doi: 10.1021/acsmedchemlett.8b00220. eCollection 2018 Jul 12.

2.

Discovery of 3(S)-thiomethyl pyrrolidine ERK inhibitors for oncology.

Boga SB, Alhassan AB, Cooper AB, Doll R, Shih NY, Shipps G, Deng Y, Zhu H, Nan Y, Sun R, Zhu L, Desai J, Patel M, Muppalla K, Gao X, Wang J, Yao X, Kelly J, Gudipati S, Paliwal S, Tsui HC, Wang T, Sherborne B, Xiao L, Hruza A, Buevich A, Zhang LK, Hesk D, Samatar AA, Carr D, Long B, Black S, Dayananth P, Windsor W, Kirschmeier P, Bishop R.

Bioorg Med Chem Lett. 2018 Jun 15;28(11):2029-2034. doi: 10.1016/j.bmcl.2018.04.063. Epub 2018 Apr 26.

PMID:
29748051
3.

Discovery of a highly potent orally bioavailable imidazo-[1, 2-a]pyrazine Aurora inhibitor.

Yu T, Zhang Y, Kerekes AD, Tagat JR, Doll RJ, Xiao Y, Esposite S, Hruza A, Belanger DB, Voss M, Rainka MP, Basso A, Liu M, Liang L, Sui N, Prelusky D, Rindgen D, Zhang L.

Bioorg Med Chem Lett. 2018 May 1;28(8):1397-1403. doi: 10.1016/j.bmcl.2018.02.037. Epub 2018 Feb 23.

PMID:
29545102
4.

Structure of the insulin receptor-insulin complex by single-particle cryo-EM analysis.

Scapin G, Dandey VP, Zhang Z, Prosise W, Hruza A, Kelly T, Mayhood T, Strickland C, Potter CS, Carragher B.

Nature. 2018 Apr 5;556(7699):122-125. doi: 10.1038/nature26153. Epub 2018 Feb 28.

5.

Discovery of Selective RNA-Binding Small Molecules by Affinity-Selection Mass Spectrometry.

Rizvi NF, Howe JA, Nahvi A, Klein DJ, Fischmann TO, Kim HY, McCoy MA, Walker SS, Hruza A, Richards MP, Chamberlin C, Saradjian P, Butko MT, Mercado G, Burchard J, Strickland C, Dandliker PJ, Smith GF, Nickbarg EB.

ACS Chem Biol. 2018 Mar 16;13(3):820-831. doi: 10.1021/acschembio.7b01013. Epub 2018 Feb 14.

PMID:
29412640
6.

Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.

Sakurada I, Endo T, Hikita K, Hirabayashi T, Hosaka Y, Kato Y, Maeda Y, Matsumoto S, Mizuno T, Nagasue H, Nishimura T, Shimada S, Shinozaki M, Taguchi K, Takeuchi K, Yokoyama T, Hruza A, Reichert P, Zhang T, Wood HB, Nakao K, Furusako S.

Bioorg Med Chem Lett. 2017 Jun 1;27(11):2622-2628. doi: 10.1016/j.bmcl.2017.03.002. Epub 2017 Mar 6.

PMID:
28408226
7.

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
8.

Discovery of 1-(1H-Pyrazolo[4,3-c]pyridin-6-yl)urea Inhibitors of Extracellular Signal-Regulated Kinase (ERK) for the Treatment of Cancers.

Lim J, Kelley EH, Methot JL, Zhou H, Petrocchi A, Chen H, Hill SE, Hinton MC, Hruza A, Jung JO, Maclean JK, Mansueto M, Naumov GN, Philippar U, Raut S, Spacciapoli P, Sun D, Siliphaivanh P.

J Med Chem. 2016 Jul 14;59(13):6501-11. doi: 10.1021/acs.jmedchem.6b00708. Epub 2016 Jul 1.

PMID:
27329786
9.

Dissecting Therapeutic Resistance to ERK Inhibition.

Jha S, Morris EJ, Hruza A, Mansueto MS, Schroeder GK, Arbanas J, McMasters D, Restaino CR, Dayananth P, Black S, Elsen NL, Mannarino A, Cooper A, Fawell S, Zawel L, Jayaraman L, Samatar AA.

Mol Cancer Ther. 2016 Apr;15(4):548-59. doi: 10.1158/1535-7163.MCT-15-0172. Epub 2016 Feb 1.

10.

Development of a novel tricyclic class of potent and selective FIXa inhibitors.

Meng D, Andre P, Bateman TJ, Berger R, Chen YH, Desai K, Dewnani S, Ellsworth K, Feng D, Geissler WM, Guo L, Hruza A, Jian T, Li H, Metzger J, Parker DL, Reichert P, Sherer EC, Smith CJ, Sonatore LM, Tschirret-Guth R, Wu J, Xu J, Zhang T, Campeau LC, Orr R, Poirier M, McCabe-Dunn J, Araki K, Nishimura T, Sakurada I, Hirabayashi T, Wood HB.

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5437-43. doi: 10.1016/j.bmcl.2015.07.078. Epub 2015 Jul 31.

PMID:
26318999
11.

Development of a novel class of potent and selective FIXa inhibitors.

Zhang T, Andre P, Bateman TJ, Chen YH, Desai K, Ellsworth K, Geissler WM, Guo L, Hruza A, Jian T, Meng D, Parker DL Jr, Qian X, Reichert P, Sherer EC, Shu M, Smith CJ, Sonatore LM, Tschirret-Guth R, Nolting AF, Orr R, Campeau LC, Araki K, Nishimura T, Sakurada I, Wood HB.

Bioorg Med Chem Lett. 2015 Nov 1;25(21):4945-4949. doi: 10.1016/j.bmcl.2015.04.057. Epub 2015 Apr 29.

PMID:
25978966
12.

Rapid development of two factor IXa inhibitors from hit to lead.

Parker DL Jr, Walsh S, Li B, Kim E, Sharipour A, Smith C, Chen YH, Berger R, Harper B, Zhang T, Park M, Shu M, Wu J, Xu J, Dewnani S, Sherer EC, Hruza A, Reichert P, Geissler W, Sonatore L, Ellsworth K, Balkovec J, Greenlee W, Wood HB.

Bioorg Med Chem Lett. 2015 Jun 1;25(11):2321-5. doi: 10.1016/j.bmcl.2015.04.025. Epub 2015 Apr 13.

PMID:
25937013
13.

Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase.

Deng Y, Shipps GW Jr, Cooper A, English JM, Annis DA, Carr D, Nan Y, Wang T, Zhu HY, Chuang CC, Dayananth P, Hruza AW, Xiao L, Jin W, Kirschmeier P, Windsor WT, Samatar AA.

J Med Chem. 2014 Nov 13;57(21):8817-26. doi: 10.1021/jm500847m. Epub 2014 Oct 22.

PMID:
25313996
14.

Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor.

Deng Y, Shipps GW Jr, Zhao L, Siddiqui MA, Popovici-Muller J, Curran PJ, Duca JS, Hruza AW, Fischmann TO, Madison VS, Zhang R, McNemar CW, Mayhood TW, Syto R, Annis A, Kirschmeier P, Lees EM, Parry DA, Windsor WT.

Bioorg Med Chem Lett. 2014 Jan 1;24(1):199-203. doi: 10.1016/j.bmcl.2013.11.041. Epub 2013 Nov 23.

PMID:
24332088
15.

Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.

Morris EJ, Jha S, Restaino CR, Dayananth P, Zhu H, Cooper A, Carr D, Deng Y, Jin W, Black S, Long B, Liu J, Dinunzio E, Windsor W, Zhang R, Zhao S, Angagaw MH, Pinheiro EM, Desai J, Xiao L, Shipps G, Hruza A, Wang J, Kelly J, Paliwal S, Gao X, Babu BS, Zhu L, Daublain P, Zhang L, Lutterbach BA, Pelletier MR, Philippar U, Siliphaivanh P, Witter D, Kirschmeier P, Bishop WR, Hicklin D, Gilliland DG, Jayaraman L, Zawel L, Fawell S, Samatar AA.

Cancer Discov. 2013 Jul;3(7):742-50. doi: 10.1158/2159-8290.CD-13-0070. Epub 2013 Apr 24.

16.

Synthesis and SAR studies of imidazo-[1,2-a]-pyrazine Aurora kinase inhibitors with improved off-target kinase selectivity.

Voss ME, Rainka MP, Fleming M, Peterson LH, Belanger DB, Siddiqui MA, Hruza A, Voigt J, Gray K, Basso AD.

Bioorg Med Chem Lett. 2012 May 15;22(10):3544-9. doi: 10.1016/j.bmcl.2012.03.051. Epub 2012 Mar 21.

PMID:
22503250
17.

The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.

Ho GD, Michael Seganish W, Bercovici A, Tulshian D, Greenlee WJ, Van Rijn R, Hruza A, Xiao L, Rindgen D, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R.

Bioorg Med Chem Lett. 2012 Apr 1;22(7):2585-9. doi: 10.1016/j.bmcl.2012.01.113. Epub 2012 Feb 9.

PMID:
22377514
18.

The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia.

Ho GD, Yang SW, Smotryski J, Bercovici A, Nechuta T, Smith EM, McElroy W, Tan Z, Tulshian D, McKittrick B, Greenlee WJ, Hruza A, Xiao L, Rindgen D, Mullins D, Guzzi M, Zhang X, Bleickardt C, Hodgson R.

Bioorg Med Chem Lett. 2012 Jan 15;22(2):1019-22. doi: 10.1016/j.bmcl.2011.11.127. Epub 2011 Dec 9.

PMID:
22222034
19.

Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia.

Yang SW, Smotryski J, McElroy WT, Tan Z, Ho G, Tulshian D, Greenlee WJ, Guzzi M, Zhang X, Mullins D, Xiao L, Hruza A, Chan TM, Rindgen D, Bleickardt C, Hodgson R.

Bioorg Med Chem Lett. 2012 Jan 1;22(1):235-9. doi: 10.1016/j.bmcl.2011.11.023. Epub 2011 Nov 16.

PMID:
22142545
20.

Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core.

Yu T, Tagat JR, Kerekes AD, Doll RJ, Zhang Y, Xiao Y, Esposite S, Belanger DB, Curran PJ, Mandal AK, Siddiqui MA, Shih NY, Basso AD, Liu M, Gray K, Tevar S, Jones J, Lee S, Liang L, Ponery S, Smith EB, Hruza A, Voigt J, Ramanathan L, Prosise W, Hu M.

ACS Med Chem Lett. 2010 Jun 7;1(5):214-8. doi: 10.1021/ml100063w. eCollection 2010 Aug 12.

21.

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann T, Hruza A, Madison V, Nomeir AA, Wang Y, Kirschmeier P, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

ACS Med Chem Lett. 2010 May 17;1(5):204-8. doi: 10.1021/ml100051d. eCollection 2010 Aug 12.

22.

Discovery of imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.

Belanger DB, Curran PJ, Hruza A, Voigt J, Meng Z, Mandal AK, Siddiqui MA, Basso AD, Gray K.

Bioorg Med Chem Lett. 2010 Sep 1;20(17):5170-4. doi: 10.1016/j.bmcl.2010.07.008. Epub 2010 Jul 8.

PMID:
20674350
23.

Discovery of C-imidazole azaheptapyridine FPT inhibitors.

Zhu HY, Cooper AB, Desai J, Njoroge G, Kirschmeier P, Bishop WR, Strickland C, Hruza A, Doll RJ, Girijavallabhan VM.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1134-6. doi: 10.1016/j.bmcl.2009.12.013. Epub 2009 Dec 6.

PMID:
20056542
24.

Synthesis, properties, and applications of diazotrifluropropanoyl-containing photoactive analogs of farnesyl diphosphate containing modified linkages for enhanced stability.

Hovlid ML, Edelstein RL, Henry O, Ochocki J, DeGraw A, Lenevich S, Talbot T, Young VG, Hruza AW, Lopez-Gallego F, Labello NP, Strickland CL, Schmidt-Dannert C, Distefano MD.

Chem Biol Drug Des. 2010 Jan;75(1):51-67. doi: 10.1111/j.1747-0285.2009.00914.x.

25.

Structure-guided discovery of cyclin-dependent kinase inhibitors.

Fischmann TO, Hruza A, Duca JS, Ramanathan L, Mayhood T, Windsor WT, Le HV, Guzi TJ, Dwyer MP, Paruch K, Doll RJ, Lees E, Parry D, Seghezzi W, Madison V.

Biopolymers. 2008 May;89(5):372-9.

PMID:
17937404
26.

Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.

Paruch K, Dwyer MP, Alvarez C, Brown C, Chan TY, Doll RJ, Keertikar K, Knutson C, McKittrick B, Rivera J, Rossman R, Tucker G, Fischmann TO, Hruza A, Madison V, Nomeir AA, Wang Y, Lees E, Parry D, Sgambellone N, Seghezzi W, Schultz L, Shanahan F, Wiswell D, Xu X, Zhou Q, James RA, Paradkar VM, Park H, Rokosz LR, Stauffer TM, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6220-3. Epub 2007 Sep 8.

PMID:
17904841
27.

Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.

Dwyer MP, Paruch K, Alvarez C, Doll RJ, Keertikar K, Duca J, Fischmann TO, Hruza A, Madison V, Lees E, Parry D, Seghezzi W, Sgambellone N, Shanahan F, Wiswell D, Guzi TJ.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6216-9. Epub 2007 Sep 8.

PMID:
17904366
28.

Binding affinities and geometries of various metal ligands in peptide deformylase inhibitors.

Madison V, Duca J, Bennett F, Bohanon S, Cooper A, Chu M, Desai J, Girijavallabhan V, Hare R, Hruza A, Hendrata S, Huang Y, Kravec C, Malcolm B, McCormick J, Miesel L, Ramanathan L, Reichert P, Saksena A, Wang J, Weber PC, Zhu H, Fischmann T.

Biophys Chem. 2002 Dec 10;101-102:239-47.

PMID:
12488004
29.

Structural characterization of nitric oxide synthase isoforms reveals striking active-site conservation.

Fischmann TO, Hruza A, Niu XD, Fossetta JD, Lunn CA, Dolphin E, Prongay AJ, Reichert P, Lundell DJ, Narula SK, Weber PC.

Nat Struct Biol. 1999 Mar;6(3):233-42.

PMID:
10074942
30.

Zinc mediated dimer of human interferon-alpha 2b revealed by X-ray crystallography.

Radhakrishnan R, Walter LJ, Hruza A, Reichert P, Trotta PP, Nagabhushan TL, Walter MR.

Structure. 1996 Dec 15;4(12):1453-63.

31.

A homology model of human interferon alpha-2.

Murgolo NJ, Windsor WT, Hruza A, Reichert P, Tsarbopoulos A, Baldwin S, Huang E, Pramanik B, Ealick S, Trotta PP.

Proteins. 1993 Sep;17(1):62-74.

PMID:
8234245

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