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Items: 30

1.

Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis.

Maxson JE, Abel ML, Wang J, Deng X, Reckel S, Luty SB, Sun H, Gorenstein J, Hughes SB, Bottomly D, Wilmot B, McWeeney SK, Radich J, Hantschel O, Middleton RE, Gray NS, Druker BJ, Tyner JW.

Cancer Res. 2016 Jan 1;76(1):127-38. doi: 10.1158/0008-5472.CAN-15-0817. Epub 2015 Dec 17.

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.

Evaluating TBK1 as a therapeutic target in cancers with activated IRF3.

Muvaffak A, Pan Q, Yan H, Fernandez R, Lim J, Dolinski B, Nguyen TT, Strack P, Wu S, Chung R, Zhang W, Hulton C, Ripley S, Hirsch H, Nagashima K, Wong KK, Jánne PA, Seidel-Dugan C, Zawel L, Kirschmeier PT, Middleton RE, Morris EJ, Wang Y.

Mol Cancer Res. 2014 Jul;12(7):1055-66. doi: 10.1158/1541-7786.MCR-13-0642. Epub 2014 Apr 21.

4.

The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins.

Lu G, Middleton RE, Sun H, Naniong M, Ott CJ, Mitsiades CS, Wong KK, Bradner JE, Kaelin WG Jr.

Science. 2014 Jan 17;343(6168):305-9. doi: 10.1126/science.1244917. Epub 2013 Nov 29.

5.

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
6.

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
7.

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
8.

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
9.

Oral treatment with a gamma-secretase inhibitor improves long-term potentiation in a mouse model of Alzheimer's disease.

Townsend M, Qu Y, Gray A, Wu Z, Seto T, Hutton M, Shearman MS, Middleton RE.

J Pharmacol Exp Ther. 2010 Apr;333(1):110-9. doi: 10.1124/jpet.109.163691. Epub 2010 Jan 7.

PMID:
20056779
10.

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
11.

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
12.

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
13.

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
14.

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
15.

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
16.

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
17.

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
18.

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
19.

Functional mapping of the transient receptor potential vanilloid 1 intracellular binding site.

Johnson DM, Garrett EM, Rutter R, Bonnert TP, Gao YD, Middleton RE, Sutton KG.

Mol Pharmacol. 2006 Sep;70(3):1005-12. Epub 2006 Jun 8.

PMID:
16763090
20.

A high-capacity membrane potential FRET-based assay for NaV1.8 channels.

Liu CJ, Priest BT, Bugianesi RM, Dulski PM, Felix JP, Dick IE, Brochu RM, Knaus HG, Middleton RE, Kaczorowski GJ, Slaughter RS, Garcia ML, Köhler MG.

Assay Drug Dev Technol. 2006 Feb;4(1):37-48.

PMID:
16506887
21.

A disubstituted succinamide is a potent sodium channel blocker with efficacy in a rat pain model.

Priest BT, Garcia ML, Middleton RE, Brochu RM, Clark S, Dai G, Dick IE, Felix JP, Liu CJ, Reiseter BS, Schmalhofer WA, Shao PP, Tang YS, Chou MZ, Kohler MG, Smith MM, Warren VA, Williams BS, Cohen CJ, Martin WJ, Meinke PT, Parsons WH, Wafford KA, Kaczorowski GJ.

Biochemistry. 2004 Aug 3;43(30):9866-76.

PMID:
15274641
22.

Resiniferatoxin binds to the capsaicin receptor (TRPV1) near the extracellular side of the S4 transmembrane domain.

Chou MZ, Mtui T, Gao YD, Kohler M, Middleton RE.

Biochemistry. 2004 Mar 9;43(9):2501-11.

PMID:
14992587
23.

Substitution of a single residue in Stichodactyla helianthus peptide, ShK-Dap22, reveals a novel pharmacological profile.

Middleton RE, Sanchez M, Linde AR, Bugianesi RM, Dai G, Felix JP, Koprak SL, Staruch MJ, Bruguera M, Cox R, Ghosh A, Hwang J, Jones S, Kohler M, Slaughter RS, McManus OB, Kaczorowski GJ, Garcia ML.

Biochemistry. 2003 Nov 25;42(46):13698-707.

PMID:
14622016
24.

Two tarantula peptides inhibit activation of multiple sodium channels.

Middleton RE, Warren VA, Kraus RL, Hwang JC, Liu CJ, Dai G, Brochu RM, Kohler MG, Gao YD, Garsky VM, Bogusky MJ, Mehl JT, Cohen CJ, Smith MM.

Biochemistry. 2002 Dec 17;41(50):14734-47.

PMID:
12475222
25.

Delay of intracellular calcium transients using a calcium chelator: application to high-throughput screening of the capsaicin receptor ion channel and G-protein-coupled receptors.

Grant SK, Bansal A, Mitra A, Feighner SD, Dai G, Kaczorowski GJ, Middleton RE.

Anal Biochem. 2001 Jul 1;294(1):27-35.

PMID:
11412002
26.
28.

Homodimeric architecture of a ClC-type chloride ion channel.

Middleton RE, Pheasant DJ, Miller C.

Nature. 1996 Sep 26;383(6598):337-40.

PMID:
8848046
29.

Purification, reconstitution, and subunit composition of a voltage-gated chloride channel from Torpedo electroplax.

Middleton RE, Pheasant DJ, Miller C.

Biochemistry. 1994 Nov 15;33(45):13189-98.

PMID:
7947726
30.

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