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Items: 1 to 50 of 71

1.

Comprehensive catalog of dendritically localized mRNA isoforms from sub-cellular sequencing of single mouse neurons.

Middleton SA, Eberwine J, Kim J.

BMC Biol. 2019 Jan 24;17(1):5. doi: 10.1186/s12915-019-0630-z.

2.

BET Inhibition Improves NASH and Liver Fibrosis.

Middleton SA, Rajpal N, Cutler L, Mander P, Rioja I, Prinjha RK, Rajpal D, Agarwal P, Kumar V.

Sci Rep. 2018 Nov 22;8(1):17257. doi: 10.1038/s41598-018-35653-4.

3.

Complete fold annotation of the human proteome using a novel structural feature space.

Middleton SA, Illuminati J, Kim J.

Sci Rep. 2017 Apr 13;7:46321. doi: 10.1038/srep46321.

4.

The purinergic receptor P2X5 regulates inflammasome activity and hyper-multinucleation of murine osteoclasts.

Kim H, Walsh MC, Takegahara N, Middleton SA, Shin HI, Kim J, Choi Y.

Sci Rep. 2017 Mar 15;7(1):196. doi: 10.1038/s41598-017-00139-2.

5.

Acute myeloid leukemia patients' clinical response to idasanutlin (RG7388) is associated with pre-treatment MDM2 protein expression in leukemic blasts.

Reis B, Jukofsky L, Chen G, Martinelli G, Zhong H, So WV, Dickinson MJ, Drummond M, Assouline S, Hashemyan M, Theron M, Blotner S, Lee JH, Kasner M, Yoon SS, Rueger R, Seiter K, Middleton SA, Kelly KR, Vey N, Yee K, Nichols G, Chen LC, Pierceall WE.

Haematologica. 2016 May;101(5):e185-8. doi: 10.3324/haematol.2015.139717. Epub 2016 Feb 11. No abstract available.

6.

MDM2 antagonist clinical response association with a gene expression signature in acute myeloid leukaemia.

Zhong H, Chen G, Jukofsky L, Geho D, Han SW, Birzele F, Bader S, Himmelein L, Cai J, Albertyn Z, Rothe M, Essioux L, Burtscher H, Middleton SA, Rueger R, Chen LC, Dangl M, Nichols G, Pierceall WE.

Br J Haematol. 2015 Nov;171(3):432-5. doi: 10.1111/bjh.13411. Epub 2015 Apr 8. No abstract available.

7.

Pre-clinical evaluation of the MDM2-p53 antagonist RG7388 alone and in combination with chemotherapy in neuroblastoma.

Chen L, Rousseau RF, Middleton SA, Nichols GL, Newell DR, Lunec J, Tweddle DA.

Oncotarget. 2015 Apr 30;6(12):10207-21.

8.

A selective small molecule NOP (ORL-1 receptor) partial agonist for the treatment of anxiety.

Ross TM, Battista K, Bignan GC, Brenneman DE, Connolly PJ, Liu J, Middleton SA, Orsini M, Reitz AB, Rosenthal DI, Scott MK, Vaidya AH.

Bioorg Med Chem Lett. 2015 Feb 1;25(3):602-6. doi: 10.1016/j.bmcl.2014.12.015. Epub 2014 Dec 17.

PMID:
25556095
9.

NoFold: RNA structure clustering without folding or alignment.

Middleton SA, Kim J.

RNA. 2014 Nov;20(11):1671-83. doi: 10.1261/rna.041913.113. Epub 2014 Sep 18.

10.

Structurally diverse MDM2-p53 antagonists act as modulators of MDR-1 function in neuroblastoma.

Chen L, Zhao Y, Halliday GC, Berry P, Rousseau RF, Middleton SA, Nichols GL, Del Bello F, Piergentili A, Newell DR, Lunec J, Tweddle DA.

Br J Cancer. 2014 Aug 12;111(4):716-25. doi: 10.1038/bjc.2014.325. Epub 2014 Jun 12.

11.

Feline mediastinal lymphoma: a retrospective study of signalment, retroviral status, response to chemotherapy and prognostic indicators.

Fabrizio F, Calam AE, Dobson JM, Middleton SA, Murphy S, Taylor SS, Schwartz A, Stell AJ.

J Feline Med Surg. 2014 Aug;16(8):637-44. doi: 10.1177/1098612X13516621. Epub 2013 Dec 23.

PMID:
24366846
12.

Effect of the MDM2 antagonist RG7112 on the P53 pathway in patients with MDM2-amplified, well-differentiated or dedifferentiated liposarcoma: an exploratory proof-of-mechanism study.

Ray-Coquard I, Blay JY, Italiano A, Le Cesne A, Penel N, Zhi J, Heil F, Rueger R, Graves B, Ding M, Geho D, Middleton SA, Vassilev LT, Nichols GL, Bui BN.

Lancet Oncol. 2012 Nov;13(11):1133-40. doi: 10.1016/S1470-2045(12)70474-6. Epub 2012 Oct 17.

PMID:
23084521
13.

Phase I study of RO4929097, a gamma secretase inhibitor of Notch signaling, in patients with refractory metastatic or locally advanced solid tumors.

Tolcher AW, Messersmith WA, Mikulski SM, Papadopoulos KP, Kwak EL, Gibbon DG, Patnaik A, Falchook GS, Dasari A, Shapiro GI, Boylan JF, Xu ZX, Wang K, Koehler A, Song J, Middleton SA, Deutsch J, Demario M, Kurzrock R, Wheler JJ.

J Clin Oncol. 2012 Jul 1;30(19):2348-53. doi: 10.1200/JCO.2011.36.8282. Epub 2012 Apr 23.

14.

Evidence that the kinesin light chain domain contains tetratricopeptide repeat units.

Fisher SQ, Weck M, Landers JE, Emrich J, Middleton SA, Cox J, Gentile L, Parish CA.

J Struct Biol. 2012 Mar;177(3):602-12. doi: 10.1016/j.jsb.2012.01.010. Epub 2012 Feb 4.

PMID:
22330276
15.

Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.

Lin R, Johnson SG, Connolly PJ, Wetter SK, Binnun E, Hughes TV, Murray WV, Pandey NB, Moreno-Mazza SJ, Adams M, Fuentes-Pesquera AR, Middleton SA.

Bioorg Med Chem Lett. 2009 Apr 15;19(8):2333-7. doi: 10.1016/j.bmcl.2009.02.067. Epub 2009 Feb 21.

PMID:
19286381
16.

Synthesis, in vitro activities of (2-cyclopropoxyphenyl)piperidine derivatives for alpha 1a and alpha 1d adrenergic receptor inhibitors.

Li S, Chiu G, Pulito VL, Liu J, Connolly PJ, Middleton SA.

Med Chem. 2009 Jan;5(1):15-22.

PMID:
19149646
17.

Improving hospital preparedness for radiological terrorism: perspectives from emergency department physicians and nurses.

Becker SM, Middleton SA.

Disaster Med Public Health Prep. 2008 Oct;2(3):174-84. doi: 10.1097/DMP.0b013e31817dcd9a.

PMID:
18813129
18.

7-[1H-Indol-2-yl]-2,3-dihydro-isoindol-1-ones as dual Aurora-A/VEGF-R2 kinase inhibitors: design, synthesis, and biological activity.

Hughes TV, Emanuel SL, O'Grady HR, Connolly PJ, Rugg C, Fuentes-Pesquera AR, Karnachi P, Alexander R, Middleton SA.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):5130-3. doi: 10.1016/j.bmcl.2008.07.090. Epub 2008 Jul 26.

PMID:
18718756
19.

A novel 5-[1,3,4-oxadiazol-2-yl]-N-aryl-4,6-pyrimidine diamine having dual EGFR/HER2 kinase activity: design, synthesis, and biological activity.

Hughes TV, Xu G, Wetter SK, Connolly PJ, Emanuel SL, Karnachi P, Pollack SR, Pandey N, Adams M, Moreno-Mazza S, Middleton SA, Greenberger LM.

Bioorg Med Chem Lett. 2008 Sep 1;18(17):4896-9. doi: 10.1016/j.bmcl.2008.07.057. Epub 2008 Jul 17.

PMID:
18678484
20.

4-Amino-6-arylamino-pyrimidine-5-carbaldehyde hydrazones as potent ErbB-2/EGFR dual kinase inhibitors.

Xu G, Abad MC, Connolly PJ, Neeper MP, Struble GT, Springer BA, Emanuel SL, Pandey N, Gruninger RH, Adams M, Moreno-Mazza S, Fuentes-Pesquera AR, Middleton SA.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4615-9. doi: 10.1016/j.bmcl.2008.07.020. Epub 2008 Jul 10.

PMID:
18653333
21.

Discovery of novel 4-amino-6-arylaminopyrimidine-5-carbaldehyde oximes as dual inhibitors of EGFR and ErbB-2 protein tyrosine kinases.

Xu G, Searle LL, Hughes TV, Beck AK, Connolly PJ, Abad MC, Neeper MP, Struble GT, Springer BA, Emanuel SL, Gruninger RH, Pandey N, Adams M, Moreno-Mazza S, Fuentes-Pesquera AR, Middleton SA, Greenberger LM.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3495-9. doi: 10.1016/j.bmcl.2008.05.024. Epub 2008 May 10.

PMID:
18508264
22.
23.

Cellular and in vivo activity of JNJ-28871063, a nonquinazoline pan-ErbB kinase inhibitor that crosses the blood-brain barrier and displays efficacy against intracranial tumors.

Emanuel SL, Hughes TV, Adams M, Rugg CA, Fuentes-Pesquera A, Connolly PJ, Pandey N, Moreno-Mazza S, Butler J, Borowski V, Middleton SA, Gruninger RH, Story JR, Napier C, Hollister B, Greenberger LM.

Mol Pharmacol. 2008 Feb;73(2):338-48. Epub 2007 Nov 1.

PMID:
17975007
24.

Aminocyclohexylsulfonamides: discovery of metabolically stable alpha(1a/1d)-selective adrenergic receptor antagonists for the treatment of benign prostatic hyperplasia/lower urinary tract symptoms (BPH/LUTS).

Chiu G, Li S, Cai H, Connolly PJ, Peng S, Stauber K, Pulito V, Liu J, Middleton SA.

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6123-8. Epub 2007 Sep 18.

PMID:
17904840
25.

Synthesis and evaluation of pyrazolo[3,4-b]pyridine CDK1 inhibitors as anti-tumor agents.

Lin R, Connolly PJ, Lu Y, Chiu G, Li S, Yu Y, Huang S, Li X, Emanuel SL, Middleton SA, Gruninger RH, Adams M, Fuentes-Pesquera AR, Greenberger LM.

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4297-302. Epub 2007 May 16.

PMID:
17532631
26.
27.

4-Aryl-5-cyano-2-aminopyrimidines as VEGF-R2 inhibitors: synthesis and biological evaluation.

Hughes TV, Emanuel SL, Beck AK, Wetter SK, Connolly PJ, Karnachi P, Reuman M, Seraj J, Fuentes-Pesquera AR, Gruninger RH, Middleton SA, Lin R, Davis JM, Moffat DF.

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3266-70. Epub 2007 Apr 10.

PMID:
17481894
28.
29.

Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).

Huang S, Li R, Connolly PJ, Emanuel S, Fuentes-Pesquera A, Adams M, Gruninger RH, Seraj J, Middleton SA, Davis JM, Moffat DF.

Bioorg Med Chem Lett. 2007 Apr 15;17(8):2179-83. Epub 2007 Feb 2.

PMID:
17317182
30.

Metastin (KiSS-1) mimetics identified from peptide structure-activity relationship-derived pharmacophores and directed small molecule database screening.

Orsini MJ, Klein MA, Beavers MP, Connolly PJ, Middleton SA, Mayo KH.

J Med Chem. 2007 Feb 8;50(3):462-71.

PMID:
17266198
31.

1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.

Li S, Chiu G, Pulito VL, Liu J, Connolly PJ, Middleton SA.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1646-50. Epub 2007 Jan 12.

PMID:
17254786
32.

Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.

Huang S, Lin R, Yu Y, Lu Y, Connolly PJ, Chiu G, Li S, Emanuel SL, Middleton SA.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1243-5. Epub 2006 Dec 15.

PMID:
17234412
33.

Role of the ABCG2 drug transporter in the resistance and oral bioavailability of a potent cyclin-dependent kinase/Aurora kinase inhibitor.

Seamon JA, Rugg CA, Emanuel S, Calcagno AM, Ambudkar SV, Middleton SA, Butler J, Borowski V, Greenberger LM.

Mol Cancer Ther. 2006 Oct;5(10):2459-67.

34.

Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.

Huang S, Li R, Connolly PJ, Emanuel S, Middleton SA.

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4818-21. Epub 2006 Jul 25.

PMID:
16870444
35.

8-(Heteroaryl)phenalkyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-ones as opioid receptor modulators.

Jordan AD, Orsini MJ, Middleton SA, Connolly PJ, Brenneman DE, Pan K, Reitz AB.

Med Chem. 2005 Nov;1(6):601-10.

PMID:
16787343
36.

Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.

Huang S, Connolly PJ, Lin R, Emanuel S, Middleton SA.

Bioorg Med Chem Lett. 2006 Jul 15;16(14):3639-41. Epub 2006 May 6.

PMID:
16682186
37.

3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.

Bignan GC, Battista K, Connolly PJ, Orsini MJ, Liu J, Middleton SA, Reitz AB.

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3524-8. Epub 2006 Apr 24.

PMID:
16632355
38.

(6,7-Dimethoxy-2,4-dihydroindeno[1,2-c]pyrazol-3-yl)phenylamines: platelet-derived growth factor receptor tyrosine kinase inhibitors with broad antiproliferative activity against tumor cells.

Ho CY, Ludovici DW, Maharoof US, Mei J, Sechler JL, Tuman RW, Strobel ED, Andraka L, Yen HK, Leo G, Li J, Almond H, Lu H, DeVine A, Tominovich RM, Baker J, Emanuel S, Gruninger RH, Middleton SA, Johnson DL, Galemmo RA Jr.

J Med Chem. 2005 Dec 29;48(26):8163-73.

PMID:
16366598
39.

The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases.

Emanuel S, Rugg CA, Gruninger RH, Lin R, Fuentes-Pesquera A, Connolly PJ, Wetter SK, Hollister B, Kruger WW, Napier C, Jolliffe L, Middleton SA.

Cancer Res. 2005 Oct 1;65(19):9038-46.

40.

Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.

Bignan GC, Battista K, Connolly PJ, Orsini MJ, Liu J, Middleton SA, Reitz AB.

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5022-6.

PMID:
16153834
41.

Synthesis and structure-activity relationships of pyrazine-pyridine biheteroaryls as novel, potent, and selective vascular endothelial growth factor receptor-2 inhibitors.

Kuo GH, Prouty C, Wang A, Emanuel S, Deangelis A, Zhang Y, Song F, Beall L, Connolly PJ, Karnachi P, Chen X, Gruninger RH, Sechler J, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.

J Med Chem. 2005 Jul 28;48(15):4892-909.

PMID:
16033269
42.

Synthesis and identification of [1,3,5]triazine-pyridine biheteroaryl as a novel series of potent cyclin-dependent kinase inhibitors.

Kuo GH, Deangelis A, Emanuel S, Wang A, Zhang Y, Connolly PJ, Chen X, Gruninger RH, Rugg C, Fuentes-Pesquera A, Middleton SA, Jolliffe L, Murray WV.

J Med Chem. 2005 Jul 14;48(14):4535-46.

PMID:
15999992
43.

1-Acyl-1H-[1,2,4]triazole-3,5-diamine analogues as novel and potent anticancer cyclin-dependent kinase inhibitors: synthesis and evaluation of biological activities.

Lin R, Connolly PJ, Huang S, Wetter SK, Lu Y, Murray WV, Emanuel SL, Gruninger RH, Fuentes-Pesquera AR, Rugg CA, Middleton SA, Jolliffe LK.

J Med Chem. 2005 Jun 30;48(13):4208-11.

PMID:
15974571
44.

3-Acyl-2,6-diaminopyridines as cyclin-dependent kinase inhibitors: synthesis and biological evaluation.

Lin R, Lu Y, Wetter SK, Connolly PJ, Turchi IJ, Murray WV, Emanuel SL, Gruninger RH, Fuentes-Pesquera AR, Adams M, Pandey N, Moreno-Mazza S, Middleton SA, Jolliffe LK.

Bioorg Med Chem Lett. 2005 May 2;15(9):2221-4.

PMID:
15837297
45.

Synthesis and discovery of pyrazine-pyridine biheteroaryl as a novel series of potent vascular endothelial growth factor receptor-2 inhibitors.

Kuo GH, Wang A, Emanuel S, Deangelis A, Zhang R, Connolly PJ, Murray WV, Gruninger RH, Sechler J, Fuentes-Pesquera A, Johnson D, Middleton SA, Jolliffe L, Chen X.

J Med Chem. 2005 Mar 24;48(6):1886-900.

PMID:
15771433
46.

The nociceptin pharmacophore site for opioid receptor binding derived from the NMR structure and bioactivity relationships.

Orsini MJ, Nesmelova I, Young HC, Hargittai B, Beavers MP, Liu J, Connolly PJ, Middleton SA, Mayo KH.

J Biol Chem. 2005 Mar 4;280(9):8134-42. Epub 2004 Dec 13.

47.

A vascular endothelial growth factor receptor-2 kinase inhibitor potentiates the activity of the conventional chemotherapeutic agents paclitaxel and doxorubicin in tumor xenograft models.

Emanuel S, Gruninger RH, Fuentes-Pesquera A, Connolly PJ, Seamon JA, Hazel S, Tominovich R, Hollister B, Napier C, D'Andrea MR, Reuman M, Bignan G, Tuman R, Johnson D, Moffatt D, Batchelor M, Foley A, O'Connell J, Allen R, Perry M, Jolliffe L, Middleton SA.

Mol Pharmacol. 2004 Sep;66(3):635-47.

PMID:
15322256
48.

Identification of New World monkey MHC-DRB alleles using PCR, DGGE and direct sequencing.

Middleton SA, Anzenberger G, Knapp LA.

Immunogenetics. 2004 Feb;55(11):785-90. Epub 2004 Jan 9.

PMID:
14714152
49.

Synthesis and discovery of macrocyclic polyoxygenated bis-7-azaindolylmaleimides as a novel series of potent and highly selective glycogen synthase kinase-3beta inhibitors.

Kuo GH, Prouty C, DeAngelis A, Shen L, O'Neill DJ, Shah C, Connolly PJ, Murray WV, Conway BR, Cheung P, Westover L, Xu JZ, Look RA, Demarest KT, Emanuel S, Middleton SA, Jolliffe L, Beavers MP, Chen X.

J Med Chem. 2003 Sep 11;46(19):4021-31.

PMID:
12954055
50.

New epoetin molecules and novel therapeutic approaches.

Barbone FP, Johnson DL, Farrell FX, Collins A, Middleton SA, McMahon FJ, Tullai J, Jolliffe LK.

Nephrol Dial Transplant. 1999;14 Suppl 2:80-4. Review.

PMID:
10334672

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