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Items: 42

1.

Discovery of Immunologically Inspired Small Molecules that Target the Viral Envelope Protein.

Lian W, Jang J, Potisopon S, Li PC, Rahmeh A, Wang J, Kwiatkowski NP, Gray NS, Yang PL.

ACS Infect Dis. 2018 Jul 20. doi: 10.1021/acsinfecdis.8b00127. [Epub ahead of print]

PMID:
30027735
2.

Development of Highly Potent and Selective Steroidal Inhibitors and Degraders of CDK8.

Hatcher JM, Wang ES, Johannessen L, Kwiatkowski N, Sim T, Gray NS.

ACS Med Chem Lett. 2018 Mar 18;9(6):540-545. doi: 10.1021/acsmedchemlett.8b00011. eCollection 2018 Jun 14.

PMID:
29937979
3.

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands.

Gechijian LN, Buckley DL, Lawlor MA, Reyes JM, Paulk J, Ott CJ, Winter GE, Erb MA, Scott TG, Xu M, Seo HS, Dhe-Paganon S, Kwiatkowski NP, Perry JA, Qi J, Gray NS, Bradner JE.

Nat Chem Biol. 2018 Apr;14(4):405-412. doi: 10.1038/s41589-018-0010-y. Epub 2018 Mar 5.

PMID:
29507391
4.

Allele-Specific Chromatin Recruitment and Therapeutic Vulnerabilities of ESR1 Activating Mutations.

Jeselsohn R, Bergholz JS, Pun M, Cornwell M, Liu W, Nardone A, Xiao T, Li W, Qiu X, Buchwalter G, Feiglin A, Abell-Hart K, Fei T, Rao P, Long H, Kwiatkowski N, Zhang T, Gray N, Melchers D, Houtman R, Liu XS, Cohen O, Wagle N, Winer EP, Zhao J, Brown M.

Cancer Cell. 2018 Feb 12;33(2):173-186.e5. doi: 10.1016/j.ccell.2018.01.004.

PMID:
29438694
5.

High MITF Expression Is Associated with Super-Enhancers and Suppressed by CDK7 Inhibition in Melanoma.

Eliades P, Abraham BJ, Ji Z, Miller DM, Christensen CL, Kwiatkowski N, Kumar R, Njauw CN, Taylor M, Miao B, Zhang T, Wong KK, Gray NS, Young RA, Tsao H.

J Invest Dermatol. 2018 Jul;138(7):1582-1590. doi: 10.1016/j.jid.2017.09.056. Epub 2018 Feb 8.

PMID:
29408204
6.

EWS/FLI Confers Tumor Cell Synthetic Lethality to CDK12 Inhibition in Ewing Sarcoma.

Iniguez AB, Stolte B, Wang EJ, Conway AS, Alexe G, Dharia NV, Kwiatkowski N, Zhang T, Abraham BJ, Mora J, Kalev P, Leggett A, Chowdhury D, Benes CH, Young RA, Gray NS, Stegmaier K.

Cancer Cell. 2018 Feb 12;33(2):202-216.e6. doi: 10.1016/j.ccell.2017.12.009. Epub 2018 Jan 18.

PMID:
29358035
7.

Overcoming Resistance to the THZ Series of Covalent Transcriptional CDK Inhibitors.

Gao Y, Zhang T, Terai H, Ficarro SB, Kwiatkowski N, Hao MF, Sharma B, Christensen CL, Chipumuro E, Wong KK, Marto JA, Hammerman PS, Gray NS, George RE.

Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5. doi: 10.1016/j.chembiol.2017.11.007. Epub 2017 Dec 21.

PMID:
29276047
8.

ER Stress Signaling Promotes the Survival of Cancer "Persister Cells" Tolerant to EGFR Tyrosine Kinase Inhibitors.

Terai H, Kitajima S, Potter DS, Matsui Y, Quiceno LG, Chen T, Kim TJ, Rusan M, Thai TC, Piccioni F, Donovan KA, Kwiatkowski N, Hinohara K, Wei G, Gray NS, Fischer ES, Wong KK, Shimamura T, Letai A, Hammerman PS, Barbie DA.

Cancer Res. 2018 Feb 15;78(4):1044-1057. doi: 10.1158/0008-5472.CAN-17-1904. Epub 2017 Dec 19.

PMID:
29259014
9.

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.

Olson CM, Jiang B, Erb MA, Liang Y, Doctor ZM, Zhang Z, Zhang T, Kwiatkowski N, Boukhali M, Green JL, Haas W, Nomanbhoy T, Fischer ES, Young RA, Bradner JE, Winter GE, Gray NS.

Nat Chem Biol. 2018 Feb;14(2):163-170. doi: 10.1038/nchembio.2538. Epub 2017 Dec 18.

10.

Suppression of Adaptive Responses to Targeted Cancer Therapy by Transcriptional Repression.

Rusan M, Li K, Li Y, Christensen CL, Abraham BJ, Kwiatkowski N, Buczkowski KA, Bockorny B, Chen T, Li S, Rhee K, Zhang H, Chen W, Terai H, Tavares T, Leggett AL, Li T, Wang Y, Zhang T, Kim TJ, Hong SH, Poudel-Neupane N, Silkes M, Mudianto T, Tan L, Shimamura T, Meyerson M, Bass AJ, Watanabe H, Gray NS, Young RA, Wong KK, Hammerman PS.

Cancer Discov. 2018 Jan;8(1):59-73. doi: 10.1158/2159-8290.CD-17-0461. Epub 2017 Oct 20.

PMID:
29054992
11.

Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors.

Kalan S, Amat R, Schachter MM, Kwiatkowski N, Abraham BJ, Liang Y, Zhang T, Olson CM, Larochelle S, Young RA, Gray NS, Fisher RP.

Cell Rep. 2017 Oct 10;21(2):467-481. doi: 10.1016/j.celrep.2017.09.056.

12.

Corrigendum: Small genomic insertions form enhancers that misregulate oncogenes.

Abraham BJ, Hnisz D, Weintraub AS, Kwiatkowski N, Li CH, Li Z, Weichert-Leahey N, Rahman S, Liu Y, Etchin J, Li B, Shen S, Lee TI, Zhang J, Look AT, Mansour MR, Young RA.

Nat Commun. 2017 Jun 1;8:15797. doi: 10.1038/ncomms15797.

13.

Corrigendum: THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors.

Cayrol F, Praditsuktavorn P, Fernando TM, Kwiatkowski N, Marullo R, Calvo-Vidal MN, Phillip J, Pera B, Yang SN, Takpradit K, Roman L, Gaudiano M, Crescenzo R, Ruan J, Inghirami G, Zhang T, Cremaschi G, Gray NS, Cerchietti L.

Nat Commun. 2017 Feb 20;8:14747. doi: 10.1038/ncomms14747. No abstract available.

14.

Small genomic insertions form enhancers that misregulate oncogenes.

Abraham BJ, Hnisz D, Weintraub AS, Kwiatkowski N, Li CH, Li Z, Weichert-Leahey N, Rahman S, Liu Y, Etchin J, Li B, Shen S, Lee TI, Zhang J, Look AT, Mansour MR, Young RA.

Nat Commun. 2017 Feb 9;8:14385. doi: 10.1038/ncomms14385.

15.

THZ1 targeting CDK7 suppresses STAT transcriptional activity and sensitizes T-cell lymphomas to BCL2 inhibitors.

Cayrol F, Praditsuktavorn P, Fernando TM, Kwiatkowski N, Marullo R, Calvo-Vidal MN, Phillip J, Pera B, Yang SN, Takpradit K, Roman L, Gaudiano M, Crescenzo R, Ruan J, Inghirami G, Zhang T, Cremaschi G, Gray NS, Cerchietti L.

Nat Commun. 2017 Jan 30;8:14290. doi: 10.1038/ncomms14290.

16.

Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors.

Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, Geyer M, Bullock AN, Young RA, Gray NS.

Nat Chem Biol. 2016 Oct;12(10):876-84. doi: 10.1038/nchembio.2166. Epub 2016 Aug 29.

17.

Practical Utility and Accuracy of Matrix-Assisted Laser Desorption Ionization-Time of Flight Mass Spectrometry for Identification of Corynebacterium Species and Other Medically Relevant Coryneform-Like Bacteria.

Suwantarat N, Weik C, Romagnoli M, Ellis BC, Kwiatkowski N, Carroll KC.

Am J Clin Pathol. 2016 Jan;145(1):22-8. doi: 10.1093/ajcp/aqv006.

PMID:
26712867
18.

CDK7-dependent transcriptional addiction in triple-negative breast cancer.

Wang Y, Zhang T, Kwiatkowski N, Abraham BJ, Lee TI, Xie S, Yuzugullu H, Von T, Li H, Lin Z, Stover DG, Lim E, Wang ZC, Iglehart JD, Young RA, Gray NS, Zhao JJ.

Cell. 2015 Sep 24;163(1):174-86. doi: 10.1016/j.cell.2015.08.063.

19.

Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor.

Christensen CL, Kwiatkowski N, Abraham BJ, Carretero J, Al-Shahrour F, Zhang T, Chipumuro E, Herter-Sprie GS, Akbay EA, Altabef A, Zhang J, Shimamura T, Capelletti M, Reibel JB, Cavanaugh JD, Gao P, Liu Y, Michaelsen SR, Poulsen HS, Aref AR, Barbie DA, Bradner JE, George RE, Gray NS, Young RA, Wong KK.

Cancer Cell. 2014 Dec 8;26(6):909-922. doi: 10.1016/j.ccell.2014.10.019. Erratum in: Cancer Cell. 2015 Jan 12;27(1):149.

20.

CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer.

Chipumuro E, Marco E, Christensen CL, Kwiatkowski N, Zhang T, Hatheway CM, Abraham BJ, Sharma B, Yeung C, Altabef A, Perez-Atayde A, Wong KK, Yuan GC, Gray NS, Young RA, George RE.

Cell. 2014 Nov 20;159(5):1126-1139. doi: 10.1016/j.cell.2014.10.024. Epub 2014 Nov 6.

21.

Tivantinib (ARQ 197) efficacy is independent of MET inhibition in non-small-cell lung cancer cell lines.

Calles A, Kwiatkowski N, Cammarata BK, Ercan D, Gray NS, Jänne PA.

Mol Oncol. 2015 Jan;9(1):260-9. doi: 10.1016/j.molonc.2014.08.011. Epub 2014 Aug 29.

22.

Targeting transcription regulation in cancer with a covalent CDK7 inhibitor.

Kwiatkowski N, Zhang T, Rahl PB, Abraham BJ, Reddy J, Ficarro SB, Dastur A, Amzallag A, Ramaswamy S, Tesar B, Jenkins CE, Hannett NM, McMillin D, Sanda T, Sim T, Kim ND, Look T, Mitsiades CS, Weng AP, Brown JR, Benes CH, Marto JA, Young RA, Gray NS.

Nature. 2014 Jul 31;511(7511):616-20. doi: 10.1038/nature13393. Epub 2014 Jun 22.

23.

Fusarium solani species complex associated with carapace lesions and branchitis in captive American horseshoe crabs Limulus polyphemus.

Tuxbury KA, Shaw GC, Montali RJ, Clayton LA, Kwiatkowski NP, Dykstra MJ, Mankowski JL.

Dis Aquat Organ. 2014 Jul 3;109(3):223-30. doi: 10.3354/dao02764.

PMID:
24991848
24.

Effects of the selective MPS1 inhibitor MPS1-IN-3 on glioblastoma sensitivity to antimitotic drugs.

Tannous BA, Kerami M, Van der Stoop PM, Kwiatkowski N, Wang J, Zhou W, Kessler AF, Lewandrowski G, Hiddingh L, Sol N, Lagerweij T, Wedekind L, Niers JM, Barazas M, Nilsson RJ, Geerts D, De Witt Hamer PC, Hagemann C, Vandertop WP, Van Tellingen O, Noske DP, Gray NS, Würdinger T.

J Natl Cancer Inst. 2013 Sep 4;105(17):1322-31. doi: 10.1093/jnci/djt168. Epub 2013 Aug 12.

25.

Characterization of Torin2, an ATP-competitive inhibitor of mTOR, ATM, and ATR.

Liu Q, Xu C, Kirubakaran S, Zhang X, Hur W, Liu Y, Kwiatkowski NP, Wang J, Westover KD, Gao P, Ercan D, Niepel M, Thoreen CC, Kang SA, Patricelli MP, Wang Y, Tupper T, Altabef A, Kawamura H, Held KD, Chou DM, Elledge SJ, Janne PA, Wong KK, Sabatini DM, Gray NS.

Cancer Res. 2013 Apr 15;73(8):2574-86. doi: 10.1158/0008-5472.CAN-12-1702. Epub 2013 Feb 22.

26.

Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy.

Zhang Z, Kwiatkowski N, Zeng H, Lim SM, Gray NS, Zhang W, Yang PL.

Mol Biosyst. 2012 Oct;8(10):2523-6. doi: 10.1039/c2mb25099c.

27.

Evaluation of nucleic acid sequencing of the D1/D2 region of the large subunit of the 28S rDNA and the internal transcribed spacer region using SmartGene IDNS [corrected] software for identification of filamentous fungi in a clinical laboratory.

Kwiatkowski NP, Babiker WM, Merz WG, Carroll KC, Zhang SX.

J Mol Diagn. 2012 Jul;14(4):393-401. doi: 10.1016/j.jmoldx.2012.02.004. Epub 2012 May 11. Erratum in: J Mol Diagn. 2012 Nov;14(6):634.

PMID:
22579969
28.

Actinomucor elegans as an emerging cause of Mucormycosis.

Mahmud A, Lee R, Munfus-McCray D, Kwiatkowski N, Subramanian A, Neofytos D, Carroll K, Zhang SX.

J Clin Microbiol. 2012 Mar;50(3):1092-5. doi: 10.1128/JCM.05338-11. Epub 2012 Jan 11.

29.

Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen.

Kwiatkowski N, Deng X, Wang J, Tan L, Villa F, Santaguida S, Huang HC, Mitchison T, Musacchio A, Gray N.

ACS Chem Biol. 2012 Jan 20;7(1):185-96. doi: 10.1021/cb200305u. Epub 2011 Oct 21.

30.

High-throughput kinase profiling: a more efficient approach toward the discovery of new kinase inhibitors.

Miduturu CV, Deng X, Kwiatkowski N, Yang W, Brault L, Filippakopoulos P, Chung E, Yang Q, Schwaller J, Knapp S, King RW, Lee JD, Herrgard S, Zarrinkar P, Gray NS.

Chem Biol. 2011 Jul 29;18(7):868-79. doi: 10.1016/j.chembiol.2011.05.010.

31.

Rapidly progressive cutaneous Rhizopus microsporus infection presenting as Fournier's gangrene in a patient with acute myelogenous leukemia.

Durand CM, Alonso CD, Subhawong AP, Kwiatkowski NP, Showel M, Carroll KC, Marr KA.

Transpl Infect Dis. 2011 Aug;13(4):392-6. doi: 10.1111/j.1399-3062.2011.00601.x. Epub 2011 Mar 28.

32.

Discovery of a benzo[e]pyrimido-[5,4-b][1,4]diazepin-6(11H)-one as a Potent and Selective Inhibitor of Big MAP Kinase 1.

Deng X, Yang Q, Kwiatkowski N, Sim T, McDermott U, Settleman JE, Lee JD, Gray NS.

ACS Med Chem Lett. 2011 Mar 10;2(3):195-200. Epub 2011 Jan 12.

33.

Cut homeobox 1 causes chromosomal instability by promoting bipolar division after cytokinesis failure.

Sansregret L, Vadnais C, Livingstone J, Kwiatkowski N, Awan A, Cadieux C, Leduy L, Hallett MT, Nepveu A.

Proc Natl Acad Sci U S A. 2011 Feb 1;108(5):1949-54. doi: 10.1073/pnas.1008403108. Epub 2011 Jan 18.

34.

Release of Mps1 from kinetochores is crucial for timely anaphase onset.

Jelluma N, Dansen TB, Sliedrecht T, Kwiatkowski NP, Kops GJ.

J Cell Biol. 2010 Oct 18;191(2):281-90. doi: 10.1083/jcb.201003038. Epub 2010 Oct 11.

35.

Chemical genetic strategy identifies histone deacetylase 1 (HDAC1) and HDAC2 as therapeutic targets in sickle cell disease.

Bradner JE, Mak R, Tanguturi SK, Mazitschek R, Haggarty SJ, Ross K, Chang CY, Bosco J, West N, Morse E, Lin K, Shen JP, Kwiatkowski NP, Gheldof N, Dekker J, DeAngelo DJ, Carr SA, Schreiber SL, Golub TR, Ebert BL.

Proc Natl Acad Sci U S A. 2010 Jul 13;107(28):12617-22. doi: 10.1073/pnas.1006774107. Epub 2010 Jun 28.

36.

Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function.

Kwiatkowski N, Jelluma N, Filippakopoulos P, Soundararajan M, Manak MS, Kwon M, Choi HG, Sim T, Deveraux QL, Rottmann S, Pellman D, Shah JV, Kops GJ, Knapp S, Gray NS.

Nat Chem Biol. 2010 May;6(5):359-68. doi: 10.1038/nchembio.345. Epub 2010 Apr 11.

37.

Structural origin of selectivity in class II-selective histone deacetylase inhibitors.

Estiu G, Greenberg E, Harrison CB, Kwiatkowski NP, Mazitschek R, Bradner JE, Wiest O.

J Med Chem. 2008 May 22;51(10):2898-906. doi: 10.1021/jm7015254. Epub 2008 Apr 16.

PMID:
18412327
38.

Discovery of selective aminothiazole aurora kinase inhibitors.

Andersen CB, Wan Y, Chang JW, Riggs B, Lee C, Liu Y, Sessa F, Villa F, Kwiatkowski N, Suzuki M, Nallan L, Heald R, Musacchio A, Gray NS.

ACS Chem Biol. 2008 Mar 20;3(3):180-92. doi: 10.1021/cb700200w. Epub 2008 Feb 29.

PMID:
18307303
39.

Human HDAC7 harbors a class IIa histone deacetylase-specific zinc binding motif and cryptic deacetylase activity.

Schuetz A, Min J, Allali-Hassani A, Schapira M, Shuen M, Loppnau P, Mazitschek R, Kwiatkowski NP, Lewis TA, Maglathin RL, McLean TH, Bochkarev A, Plotnikov AN, Vedadi M, Arrowsmith CH.

J Biol Chem. 2008 Apr 25;283(17):11355-63. doi: 10.1074/jbc.M707362200. Epub 2008 Feb 19.

40.

Rapid, standardized method for determination of Mycobacterium tuberculosis drug susceptibility by use of mycolic acid analysis.

Parrish N, Osterhout G, Dionne K, Sweeney A, Kwiatkowski N, Carroll K, Jost KC Jr, Dick J.

J Clin Microbiol. 2007 Dec;45(12):3915-20. Epub 2007 Oct 3.

41.

Use of peptide nucleic acid-fluorescence in situ hybridization for definitive, rapid identification of five common Candida species.

Reller ME, Mallonee AB, Kwiatkowski NP, Merz WG.

J Clin Microbiol. 2007 Nov;45(11):3802-3. Epub 2007 Sep 5.

42.

MT FdR: a ferredoxin reductase from M. tuberculosis that couples to MT CYP51.

Zanno A, Kwiatkowski N, Vaz AD, Guardiola-Diaz HM.

Biochim Biophys Acta. 2005 Apr-May;1707(2-3):157-69. Epub 2004 Dec 15.

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