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Items: 1 to 20 of 364

1.

Single and dual targeting of mutant EGFR with an allosteric inhibitor.

To C, Jang J, Chen T, Park E, Mushajiang M, De Clercq DJH, Xu M, Wang S, Cameron MD, Heppner DE, Shin BH, Gero TW, Yang A, Dahlberg SE, Wong KK, Eck MJ, Gray NS, Janne PA.

Cancer Discov. 2019 May 15. pii: CD-18-0903. doi: 10.1158/2159-8290.CD-18-0903. [Epub ahead of print]

PMID:
31092401
2.

BCL2 Amplicon Loss and Transcriptional Remodeling Drives ABT-199 Resistance in B Cell Lymphoma Models.

Zhao X, Ren Y, Lawlor M, Shah BD, Park PMC, Lwin T, Wang X, Liu K, Wang M, Gao J, Li T, Xu M, Silva AS, Lee K, Zhang T, Koomen JM, Jiang H, Sudalagunta PR, Meads MB, Cheng F, Bi C, Fu K, Fan H, Dalton WS, Moscinski LC, Shain KH, Sotomayor EM, Wang GG, Gray NS, Cleveland JL, Qi J, Tao J.

Cancer Cell. 2019 May 13;35(5):752-766.e9. doi: 10.1016/j.ccell.2019.04.005.

PMID:
31085176
3.

JNK2 Is Required for the Tumorigenic Properties of Melanoma Cells.

Du L, Anderson A, Nguyen K, Ojeda SS, Ortiz-Rivera I, Nguyen TN, Zhang T, Kaoud TS, Gray NS, Dalby KN, Tsai KY.

ACS Chem Biol. 2019 May 17. doi: 10.1021/acschembio.9b00083. [Epub ahead of print]

PMID:
31063355
4.

CDK12 loss in cancer cells affects DNA damage response genes through premature cleavage and polyadenylation.

Krajewska M, Dries R, Grassetti AV, Dust S, Gao Y, Huang H, Sharma B, Day DS, Kwiatkowski N, Pomaville M, Dodd O, Chipumuro E, Zhang T, Greenleaf AL, Yuan GC, Gray NS, Young RA, Geyer M, Gerber SA, George RE.

Nat Commun. 2019 Apr 15;10(1):1757. doi: 10.1038/s41467-019-09703-y.

5.

Leveraging Compound Promiscuity to Identify Targetable Cysteines within the Kinome.

Rao S, Gurbani D, Du G, Everley RA, Browne CM, Chaikuad A, Tan L, Schröder M, Gondi S, Ficarro SB, Sim T, Kim ND, Berberich MJ, Knapp S, Marto JA, Westover KD, Sorger PK, Gray NS.

Cell Chem Biol. 2019 Apr 11. pii: S2451-9456(19)30076-5. doi: 10.1016/j.chembiol.2019.02.021. [Epub ahead of print]

PMID:
30982749
6.

Peptide-based covalent inhibitors of MALT1 paracaspase.

Hatcher JM, Du G, Fontán L, Us I, Qiao Q, Chennamadhavuni S, Shao J, Wu H, Melnick A, Gray NS, Scott DA.

Bioorg Med Chem Lett. 2019 Jun 1;29(11):1336-1339. doi: 10.1016/j.bmcl.2019.03.046. Epub 2019 Mar 29.

PMID:
30954428
7.

Discovery of Covalent CDK14 Inhibitors with Pan-TAIRE Family Specificity.

Ferguson FM, Doctor ZM, Ficarro SB, Browne CM, Marto JA, Johnson JL, Yaron TM, Cantley LC, Kim ND, Sim T, Berberich MJ, Kalocsay M, Sorger PK, Gray NS.

Cell Chem Biol. 2019 Mar 11. pii: S2451-9456(19)30070-4. doi: 10.1016/j.chembiol.2019.02.015. [Epub ahead of print]

PMID:
30930164
8.

Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models.

Silva MC, Ferguson FM, Cai Q, Donovan KA, Nandi G, Patnaik D, Zhang T, Huang HT, Lucente DE, Dickerson BC, Mitchison TJ, Fischer ES, Gray NS, Haggarty SJ.

Elife. 2019 Mar 25;8. pii: e45457. doi: 10.7554/eLife.45457.

9.

Development of a Selective CDK7 Covalent Inhibitor Reveals Predominant Cell-Cycle Phenotype.

Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, Lin CY, Kwiatkowski N, Gray NS.

Cell Chem Biol. 2019 Mar 6. pii: S2451-9456(19)30067-4. doi: 10.1016/j.chembiol.2019.02.012. [Epub ahead of print]

PMID:
30905681
10.

A multi-targeted probe-based strategy to identify signaling vulnerabilities in cancers.

Rao S, Du G, Hafner M, Subramanian K, Sorger PK, Gray NS.

J Biol Chem. 2019 Mar 11. pii: jbc.RA118.006805. doi: 10.1074/jbc.RA118.006805. [Epub ahead of print]

11.

Targeting chronic myeloid leukemia stem cells with ERK5 pathway inhibitors.

4° JOINT MEETING OF PATHOLOGY AND LABORATORY MEDICINE SIPMET–SIPMEL - SECOND JOINT MEETING IN COLLABORATION WITH ASIP–AMP–UEMS–WASPALM - 4° SIPMEL NATIONAL CONGRESS - 34° SIPMET NATIONAL CONGRESS - 4° CONGRESS OF PATHOLOGY AND LABORATORY MEDICINE, Tusa I, Cheloni G, Poteti M, Gozzini A, Deng X, Gray NS, Li S, Dello Sbarba P, Rovida E.

J Biol Regul Homeost Agents. 2018 Jul-Aug;32(4 Suppl. 1):36. No abstract available.

PMID:
30810012
12.

Development of Dual and Selective Degraders of Cyclin-Dependent Kinases 4 and 6.

Jiang B, Wang ES, Donovan KA, Liang Y, Fischer ES, Zhang T, Gray NS.

Angew Chem Int Ed Engl. 2019 May 6;58(19):6321-6326. doi: 10.1002/anie.201901336. Epub 2019 Mar 29.

PMID:
30802347
13.

Identification of small molecule inhibitors targeting the Zika virus envelope protein.

Pitts J, Hsia CY, Lian W, Wang J, Pfeil MP, Kwiatkowski N, Li Z, Jang J, Gray NS, Yang PL.

Antiviral Res. 2019 Apr;164:147-153. doi: 10.1016/j.antiviral.2019.02.008. Epub 2019 Feb 13.

PMID:
30771406
14.

Conformational flexibility and inhibitor binding to unphosphorylated interleukin-1 receptor-associated kinase 4 (IRAK4).

Wang L, Ferrao R, Li Q, Hatcher JM, Choi HG, Buhrlage SJ, Gray NS, Wu H.

J Biol Chem. 2019 Mar 22;294(12):4511-4519. doi: 10.1074/jbc.RA118.005428. Epub 2019 Jan 24.

PMID:
30679311
15.

Small-molecule targeting of brachyury transcription factor addiction in chordoma.

Sharifnia T, Wawer MJ, Chen T, Huang QY, Weir BA, Sizemore A, Lawlor MA, Goodale A, Cowley GS, Vazquez F, Ott CJ, Francis JM, Sassi S, Cogswell P, Sheppard HE, Zhang T, Gray NS, Clarke PA, Blagg J, Workman P, Sommer J, Hornicek F, Root DE, Hahn WC, Bradner JE, Wong KK, Clemons PA, Lin CY, Kotz JD, Schreiber SL.

Nat Med. 2019 Feb;25(2):292-300. doi: 10.1038/s41591-018-0312-3. Epub 2019 Jan 21.

PMID:
30664779
16.

Psychopathy and impulsivity: The relationship of psychopathy to different aspects of UPPS-P impulsivity.

Gray NS, Weidacker K, Snowden RJ.

Psychiatry Res. 2019 Feb;272:474-482. doi: 10.1016/j.psychres.2018.12.155. Epub 2018 Dec 29.

PMID:
30611967
17.

Small Molecules Targeting the Flavivirus E Protein with Broad-Spectrum Activity and Antiviral Efficacy in Vivo.

Li PC, Jang J, Hsia CY, Groomes PV, Lian W, de Wispelaere M, Pitts JD, Wang J, Kwiatkowski N, Gray NS, Yang PL.

ACS Infect Dis. 2019 Mar 8;5(3):460-472. doi: 10.1021/acsinfecdis.8b00322. Epub 2019 Jan 14.

PMID:
30608640
18.

Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML.

Brand M, Jiang B, Bauer S, Donovan KA, Liang Y, Wang ES, Nowak RP, Yuan JC, Zhang T, Kwiatkowski N, Müller AC, Fischer ES, Gray NS, Winter GE.

Cell Chem Biol. 2019 Feb 21;26(2):300-306.e9. doi: 10.1016/j.chembiol.2018.11.006. Epub 2018 Dec 27.

PMID:
30595531
19.

Bruton tyrosine kinase degradation as a therapeutic strategy for cancer.

Dobrovolsky D, Wang ES, Morrow S, Leahy C, Faust T, Nowak RP, Donovan KA, Yang G, Li Z, Fischer ES, Treon SP, Weinstock DM, Gray NS.

Blood. 2019 Feb 28;133(9):952-961. doi: 10.1182/blood-2018-07-862953. Epub 2018 Dec 13.

PMID:
30545835
20.

A Chemoproteomic Strategy for Direct and Proteome-Wide Covalent Inhibitor Target-Site Identification.

Browne CM, Jiang B, Ficarro SB, Doctor ZM, Johnson JL, Card JD, Sivakumaren SC, Alexander WM, Yaron TM, Murphy CJ, Kwiatkowski NP, Zhang T, Cantley LC, Gray NS, Marto JA.

J Am Chem Soc. 2019 Jan 9;141(1):191-203. doi: 10.1021/jacs.8b07911. Epub 2018 Dec 20.

PMID:
30518210

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