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Items: 39

1.

Potent benzoazepinone γ-secretase modulators with improved bioavailability.

Methot JL, Fischer C, Li C, Rivkin A, Ahearn SP, Brown WC, Kattar S, Kelley E, Mampreian DM, Schell A, Rosenau A, Zhou H, Ball R, Deshmukh SV, Jeliazkova-Mecheva VV, Diaz D, Moy LY, Kenific CM, Moxham C, Shah S, Nuthall H, Szewczak AA, Hill A, Hughes B, Smotrov N, Munoz B, Miller TA, Shearman MS.

Bioorg Med Chem Lett. 2015 Sep 1;25(17):3495-500. doi: 10.1016/j.bmcl.2015.06.032. Epub 2015 Jun 15.

PMID:
26142947
2.

Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.

Methot JL, Hoffman DM, Witter DJ, Stanton MG, Harrington P, Hamblett C, Siliphaivanh P, Wilson K, Hubbs J, Heidebrecht R, Kral AM, Ozerova N, Fleming JC, Wang H, Szewczak AA, Middleton RE, Hughes B, Cruz JC, Haines BB, Chenard M, Kenific CM, Harsch A, Secrist JP, Miller TA.

ACS Med Chem Lett. 2014 Jan 2;5(4):340-5. doi: 10.1021/ml4004233. eCollection 2014 Apr 10.

3.

High-throughput quality control of DMSO acoustic dispensing using photometric dye methods.

Quintero C, Tran K, Szewczak AA.

J Lab Autom. 2013 Aug;18(4):296-305. doi: 10.1177/2211068213486787. Epub 2013 Apr 29.

PMID:
23629143
4.

Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.

Northrup AB, Katcher MH, Altman MD, Chenard M, Daniels MH, Deshmukh SV, Falcone D, Guerin DJ, Hatch H, Li C, Lu W, Lutterbach B, Allison TJ, Patel SB, Reilly JF, Reutershan M, Rickert KW, Rosenstein C, Soisson SM, Szewczak AA, Walker D, Wilson K, Young JR, Pan BS, Dinsmore CJ.

J Med Chem. 2013 Mar 28;56(6):2294-310. doi: 10.1021/jm301619u. Epub 2013 Mar 18.

PMID:
23379595
5.

Efficacious intermittent dosing of a novel JAK2 inhibitor in mouse models of polycythemia vera.

Kraus M, Wang Y, Aleksandrowicz D, Bachman E, Szewczak AA, Walker D, Xu L, Bouthillette M, Childers KM, Dolinski B, Haidle AM, Kopinja J, Lee L, Lim J, Little KD, Ma Y, Mathur A, Mo JR, O'Hare E, Otte RD, Taoka BM, Wang W, Yin H, Zabierek AA, Zhang W, Zhao S, Zhu J, Young JR, Marshall CG.

PLoS One. 2012;7(5):e37207. doi: 10.1371/journal.pone.0037207. Epub 2012 May 18.

6.

Triazoloamides as potent γ-secretase modulators with reduced hERG liability.

Fischer C, Zultanski SL, Zhou H, Methot JL, Shah S, Nuthall H, Hughes BL, Smotrov N, Hill A, Szewczak AA, Moxham CM, Bays N, Middleton RE, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2012 May 1;22(9):3140-6. doi: 10.1016/j.bmcl.2012.03.054. Epub 2012 Mar 21.

PMID:
22497762
7.

Discovery of 1-amino-5H-pyrido[4,3-b]indol-4-carboxamide inhibitors of Janus kinase 2 (JAK2) for the treatment of myeloproliferative disorders.

Lim J, Taoka B, Otte RD, Spencer K, Dinsmore CJ, Altman MD, Chan G, Rosenstein C, Sharma S, Su HP, Szewczak AA, Xu L, Yin H, Zugay-Murphy J, Marshall CG, Young JR.

J Med Chem. 2011 Oct 27;54(20):7334-49. doi: 10.1021/jm200909u. Epub 2011 Sep 26.

PMID:
21942426
8.

Isolation, structure, and biological activities of Fellutamides C and D from an undescribed Metulocladosporiella (Chaetothyriales) using the genome-wide Candida albicans fitness test.

Xu D, Ondeyka J, Harris GH, Zink D, Kahn JN, Wang H, Bills G, Platas G, Wang W, Szewczak AA, Liberator P, Roemer T, Singh SB.

J Nat Prod. 2011 Aug 26;74(8):1721-30. doi: 10.1021/np2001573. Epub 2011 Jul 13.

PMID:
21761939
9.

Triazoles as γ-secretase modulators.

Fischer C, Zultanski SL, Zhou H, Methot JL, Brown WC, Mampreian DM, Schell AJ, Shah S, Nuthall H, Hughes BL, Smotrov N, Kenific CM, Cruz JC, Walker D, Bouthillette M, Nikov GN, Savage DF, Jeliazkova-Mecheva VV, Diaz D, Szewczak AA, Bays N, Middleton RE, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2011 Jul 1;21(13):4083-7. doi: 10.1016/j.bmcl.2011.04.089. Epub 2011 May 4.

PMID:
21616665
10.

Discovery of a 5H-benzo[4,5]cyclohepta[1,2-b]pyridin-5-one (MK-2461) inhibitor of c-Met kinase for the treatment of cancer.

Katz JD, Jewell JP, Guerin DJ, Lim J, Dinsmore CJ, Deshmukh SV, Pan BS, Marshall CG, Lu W, Altman MD, Dahlberg WK, Davis L, Falcone D, Gabarda AE, Hang G, Hatch H, Holmes R, Kunii K, Lumb KJ, Lutterbach B, Mathvink R, Nazef N, Patel SB, Qu X, Reilly JF, Rickert KW, Rosenstein C, Soisson SM, Spencer KB, Szewczak AA, Walker D, Wang W, Young J, Zeng Q.

J Med Chem. 2011 Jun 23;54(12):4092-108. doi: 10.1021/jm200112k. Epub 2011 May 24.

PMID:
21608528
11.

Quinazolinones as γ-secretase modulators.

Fischer C, Shah S, Hughes BL, Nikov GN, Crispino JL, Middleton RE, Szewczak AA, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2011 Jan 15;21(2):773-6. doi: 10.1016/j.bmcl.2010.11.111. Epub 2010 Nov 26.

PMID:
21190851
12.

Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor.

Nagashima K, Shumway SD, Sathyanarayanan S, Chen AH, Dolinski B, Xu Y, Keilhack H, Nguyen T, Wiznerowicz M, Li L, Lutterbach BA, Chi A, Paweletz C, Allison T, Yan Y, Munshi SK, Klippel A, Kraus M, Bobkova EV, Deshmukh S, Xu Z, Mueller U, Szewczak AA, Pan BS, Richon V, Pollock R, Blume-Jensen P, Northrup A, Andersen JN.

J Biol Chem. 2011 Feb 25;286(8):6433-48. doi: 10.1074/jbc.M110.156463. Epub 2010 Nov 30.

13.

Purine derivatives as potent gamma-secretase modulators.

Rivkin A, Ahearn SP, Chichetti SM, Hamblett CL, Garcia Y, Martinez M, Hubbs JL, Reutershan MH, Daniels MH, Siliphaivanh P, Otte KM, Li C, Rosenau A, Surdi LM, Jung J, Hughes BL, Crispino JL, Nikov GN, Middleton RE, Moxham CM, Szewczak AA, Shah S, Moy LY, Kenific CM, Tanga F, Cruz JC, Andrade P, Angagaw MH, Shomer NH, Miller T, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2010 Apr 1;20(7):2279-82. doi: 10.1016/j.bmcl.2010.02.008. Epub 2010 Feb 6.

PMID:
20207146
14.

MK-2461, a novel multitargeted kinase inhibitor, preferentially inhibits the activated c-Met receptor.

Pan BS, Chan GK, Chenard M, Chi A, Davis LJ, Deshmukh SV, Gibbs JB, Gil S, Hang G, Hatch H, Jewell JP, Kariv I, Katz JD, Kunii K, Lu W, Lutterbach BA, Paweletz CP, Qu X, Reilly JF, Szewczak AA, Zeng Q, Kohl NE, Dinsmore CJ.

Cancer Res. 2010 Feb 15;70(4):1524-33. doi: 10.1158/0008-5472.CAN-09-2541. Epub 2010 Feb 9.

15.

Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.

Rivkin A, Ahearn SP, Chichetti SM, Kim YR, Li C, Rosenau A, Kattar SD, Jung J, Shah S, Hughes BL, Crispino JL, Middleton RE, Szewczak AA, Munoz B, Shearman MS.

Bioorg Med Chem Lett. 2010 Feb 1;20(3):1269-71. doi: 10.1016/j.bmcl.2009.11.101. Epub 2009 Nov 23.

PMID:
20022243
16.

Fluorinated piperidine acetic acids as gamma-secretase modulators.

Stanton MG, Hubbs J, Sloman D, Hamblett C, Andrade P, Angagaw M, Bi G, Black RM, Crispino J, Cruz JC, Fan E, Farris G, Hughes BL, Kenific CM, Middleton RE, Nikov G, Sajonz P, Shah S, Shomer N, Szewczak AA, Tanga F, Tudge MT, Shearman M, Munoz B.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):755-8. doi: 10.1016/j.bmcl.2009.11.034. Epub 2009 Nov 13.

PMID:
20005099
17.

Exploring the pharmacokinetic properties of phosphorus-containing selective HDAC 1 and 2 inhibitors (SHI-1:2).

Heidebrecht RW Jr, Chenard M, Close J, Dahlberg WK, Fleming J, Grimm JB, Hamill JE, Harsch A, Haines BB, Hughes B, Kral AM, Middleton RE, Mushti C, Ozerova N, Szewczak AA, Wang H, Wilson K, Witter DJ, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2009 Apr 1;19(7):2053-8. doi: 10.1016/j.bmcl.2009.02.009. Epub 2009 Feb 8.

PMID:
19268585
18.

Parallel medicinal chemistry approaches to selective HDAC1/HDAC2 inhibitor (SHI-1:2) optimization.

Kattar SD, Surdi LM, Zabierek A, Methot JL, Middleton RE, Hughes B, Szewczak AA, Dahlberg WK, Kral AM, Ozerova N, Fleming JC, Wang H, Secrist P, Harsch A, Hamill JE, Cruz JC, Kenific CM, Chenard M, Miller TA, Berk SC, Tempest P.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1168-72. doi: 10.1016/j.bmcl.2008.12.083. Epub 2008 Dec 25.

PMID:
19138845
19.

SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2).

Methot JL, Hamblett CL, Mampreian DM, Jung J, Harsch A, Szewczak AA, Dahlberg WK, Middleton RE, Hughes B, Fleming JC, Wang H, Kral AM, Ozerova N, Cruz JC, Haines B, Chenard M, Kenific CM, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. doi: 10.1016/j.bmcl.2008.10.052. Epub 2008 Oct 14.

PMID:
18951790
20.

High-throughput analysis of HGF-stimulated cell scattering.

Chan GK, Lutterbach BA, Pan BS, Kariv I, Szewczak AA.

J Biomol Screen. 2008 Oct;13(9):847-54. doi: 10.1177/1087057108324497. Epub 2008 Sep 23.

PMID:
18812567
21.

Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).

Wilson KJ, Witter DJ, Grimm JB, Siliphaivanh P, Otte KM, Kral AM, Fleming JC, Harsch A, Hamill JE, Cruz JC, Chenard M, Szewczak AA, Middleton RE, Hughes BL, Dahlberg WK, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1859-63. doi: 10.1016/j.bmcl.2008.02.012. Epub 2008 Feb 10.

PMID:
18304810
22.

Exploration of the internal cavity of histone deacetylase (HDAC) with selective HDAC1/HDAC2 inhibitors (SHI-1:2).

Methot JL, Chakravarty PK, Chenard M, Close J, Cruz JC, Dahlberg WK, Fleming J, Hamblett CL, Hamill JE, Harrington P, Harsch A, Heidebrecht R, Hughes B, Jung J, Kenific CM, Kral AM, Meinke PT, Middleton RE, Ozerova N, Sloman DL, Stanton MG, Szewczak AA, Tyagarajan S, Witter DJ, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Feb 1;18(3):973-8. doi: 10.1016/j.bmcl.2007.12.031. Epub 2008 Jan 7.

PMID:
18182289
23.

Amino acid derivatives as histone deacetylase inhibitors.

Hubbs JL, Zhou H, Kral AM, Fleming JC, Dahlberg WK, Hughes BL, Middleton RE, Szewczak AA, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):34-8. Epub 2007 Nov 13.

PMID:
18042381
24.

The discovery of 6-amino nicotinamides as potent and selective histone deacetylase inhibitors.

Hamblett CL, Methot JL, Mampreian DM, Sloman DL, Stanton MG, Kral AM, Fleming JC, Cruz JC, Chenard M, Ozerova N, Hitz AM, Wang H, Deshmukh SV, Nazef N, Harsch A, Hughes B, Dahlberg WK, Szewczak AA, Middleton RE, Mosley RT, Secrist JP, Miller TA.

Bioorg Med Chem Lett. 2007 Oct 1;17(19):5300-9. Epub 2007 Aug 16.

PMID:
17761416
25.

A high-throughput competitive scintillation proximity aminoacyl-tRNA synthetase charging assay to measure amino acid concentration.

Forbes CD, Myung J, Szewczak AA, Landro JA.

Anal Biochem. 2007 Apr 15;363(2):246-54. Epub 2007 Jan 26. Erratum in: Anal Biochem. 2008 Jun 15;377(2):274. Szewczak, Alexander A [added].

PMID:
17316538
26.

Identification of an active site ligand for a group I ribozyme catalytic metal ion.

Szewczak AA, Kosek AB, Piccirilli JA, Strobel SA.

Biochemistry. 2002 Feb 26;41(8):2516-25.

PMID:
11851398
27.

An important base triple anchors the substrate helix recognition surface within the Tetrahymena ribozyme active site.

Szewczak AA, Ortoleva-Donnelly L, Zivarts MV, Oyelere AK, Kazantsev AV, Strobel SA.

Proc Natl Acad Sci U S A. 1999 Sep 28;96(20):11183-8.

28.

A minor groove RNA triple helix within the catalytic core of a group I intron.

Szewczak AA, Ortoleva-Donnelly L, Ryder SP, Moncoeur E, Strobel SA.

Nat Struct Biol. 1998 Dec;5(12):1037-42.

PMID:
9846872
29.

Thermodynamic stability of the P4-P6 domain RNA tertiary structure measured by temperature gradient gel electrophoresis.

Szewczak AA, Podell ER, Bevilacqua PC, Cech TR.

Biochemistry. 1998 Aug 11;37(32):11162-70.

PMID:
9698362
30.

The chemical basis of adenosine conservation throughout the Tetrahymena ribozyme.

Ortoleva-Donnelly L, Szewczak AA, Gutell RR, Strobel SA.

RNA. 1998 May;4(5):498-519.

31.
32.

RNA tertiary structure mediation by adenosine platforms.

Cate JH, Gooding AR, Podell E, Zhou K, Golden BL, Szewczak AA, Kundrot CE, Cech TR, Doudna JA.

Science. 1996 Sep 20;273(5282):1696-9.

PMID:
8781229
33.

Selecting apt RNAs for NMR.

Cech TR, Szewczak AA.

RNA. 1996 Jul;2(7):625-7. No abstract available.

34.

The sarcin/ricin loop, a modular RNA.

Szewczak AA, Moore PB.

J Mol Biol. 1995 Mar 17;247(1):81-98.

PMID:
7897662
35.

The conformation of the sarcin/ricin loop from 28S ribosomal RNA.

Szewczak AA, Moore PB, Chang YL, Wool IG.

Proc Natl Acad Sci U S A. 1993 Oct 15;90(20):9581-5.

37.

An NMR characterization of the regA protein-binding site of bacteriophage T4 gene 44 mRNA.

Szewczak AA, Webster KR, Spicer EK, Moore PB.

J Biol Chem. 1991 Sep 25;266(27):17832-7.

38.

On the conformation of the alpha sarcin stem-loop of 28S rRNA.

Szewczak AA, Chan YL, Moore PB, Wool IG.

Biochimie. 1991 Jul-Aug;73(7-8):871-7.

PMID:
1742362
39.

On the use of T7 RNA polymerase transcripts for physical investigation.

Szewczak AA, White SA, Gewirth DT, Moore PB.

Nucleic Acids Res. 1990 Jul 25;18(14):4139-42.

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