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Items: 1 to 50 of 370

1.

BORIS promotes chromatin regulatory interactions in treatment-resistant cancer cells.

Debruyne DN, Dries R, Sengupta S, Seruggia D, Gao Y, Sharma B, Huang H, Moreau L, McLane M, Day DS, Marco E, Chen T, Gray NS, Wong KK, Orkin SH, Yuan GC, Young RA, George RE.

Nature. 2019 Aug;572(7771):676-680. doi: 10.1038/s41586-019-1472-0. Epub 2019 Aug 7.

PMID:
31391581
2.

Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations.

de Wispelaere M, Du G, Donovan KA, Zhang T, Eleuteri NA, Yuan JC, Kalabathula J, Nowak RP, Fischer ES, Gray NS, Yang PL.

Nat Commun. 2019 Aug 1;10(1):3468. doi: 10.1038/s41467-019-11429-w.

3.

Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice.

Tang X, Drotar J, Li K, Clairmont CD, Brumm AS, Sullins AJ, Wu H, Liu XS, Wang J, Gray NS, Sur M, Jaenisch R.

Sci Transl Med. 2019 Jul 31;11(503). pii: eaau0164. doi: 10.1126/scitranslmed.aau0164.

PMID:
31366578
4.

The Triarchic Model of Psychopathy and Antisocial Behavior: Results From an Offender Population With Personality Disorder.

Gray NS, Blumenthal S, Shuker R, Wood H, Fonagy P, Snowden RJ.

J Interpers Violence. 2019 Jun 13:886260519853404. doi: 10.1177/0886260519853404. [Epub ahead of print]

PMID:
31189393
5.

Synthesis and structure activity relationships of a series of 4-amino-1H-pyrazoles as covalent inhibitors of CDK14.

Ferguson FM, Doctor ZM, Ficarro SB, Marto JA, Kim ND, Sim T, Gray NS.

Bioorg Med Chem Lett. 2019 Aug 1;29(15):1985-1993. doi: 10.1016/j.bmcl.2019.05.024. Epub 2019 May 23.

PMID:
31175010
6.

Quinoline and thiazolopyridine allosteric inhibitors of MALT1.

Scott DA, Hatcher JM, Liu H, Fu M, Du G, Fontán L, Us I, Casalena G, Qiao Q, Wu H, Melnick A, Gray NS.

Bioorg Med Chem Lett. 2019 Jul 15;29(14):1694-1698. doi: 10.1016/j.bmcl.2019.05.040. Epub 2019 May 20.

PMID:
31129051
7.

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, Jänne PA.

Cancer Discov. 2019 Jul;9(7):926-943. doi: 10.1158/2159-8290.CD-18-0903. Epub 2019 May 15.

PMID:
31092401
8.

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
9.

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 Jul 19;14(7):1426-1435. doi: 10.1021/acschembio.9b00083. Epub 2019 May 17.

PMID:
31063355
10.

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.

11.

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 Jun 20;26(6):818-829.e9. doi: 10.1016/j.chembiol.2019.02.021. Epub 2019 Apr 11.

PMID:
30982749
12.

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
13.

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 Jun 20;26(6):804-817.e12. doi: 10.1016/j.chembiol.2019.02.015. Epub 2019 Mar 28.

PMID:
30930164
14.

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.

15.

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 Jun 20;26(6):792-803.e10. doi: 10.1016/j.chembiol.2019.02.012. Epub 2019 Mar 21.

PMID:
30905681
16.

A multitargeted 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 May 24;294(21):8664-8673. doi: 10.1074/jbc.RA118.006805. Epub 2019 Mar 11.

17.

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
18.

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
19.

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
20.

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
21.

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.

22.

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
23.

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
24.

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
25.

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
26.

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
27.

Emotional modulation of the pupil response in psychopathy.

Burley DT, Gray NS, Snowden RJ.

Personal Disord. 2019 Jul;10(4):365-375. doi: 10.1037/per0000313. Epub 2018 Dec 3.

28.

Targeted degradation of BRD9 reverses oncogenic gene expression in synovial sarcoma.

Brien GL, Remillard D, Shi J, Hemming ML, Chabon J, Wynne K, Dillon ET, Cagney G, Van Mierlo G, Baltissen MP, Vermeulen M, Qi J, Fröhling S, Gray NS, Bradner JE, Vakoc CR, Armstrong SA.

Elife. 2018 Nov 15;7. pii: e41305. doi: 10.7554/eLife.41305.

29.

Targeting MYC dependency in ovarian cancer through inhibition of CDK7 and CDK12/13.

Zeng M, Kwiatkowski NP, Zhang T, Nabet B, Xu M, Liang Y, Quan C, Wang J, Hao M, Palakurthi S, Zhou S, Zeng Q, Kirschmeier PT, Meghani K, Leggett AL, Qi J, Shapiro GI, Liu JF, Matulonis UA, Lin CY, Konstantinopoulos PA, Gray NS.

Elife. 2018 Nov 13;7. pii: e39030. doi: 10.7554/eLife.39030.

30.

A non-canonical SWI/SNF complex is a synthetic lethal target in cancers driven by BAF complex perturbation.

Michel BC, D'Avino AR, Cassel SH, Mashtalir N, McKenzie ZM, McBride MJ, Valencia AM, Zhou Q, Bocker M, Soares LMM, Pan J, Remillard DI, Lareau CA, Zullow HJ, Fortoul N, Gray NS, Bradner JE, Chan HM, Kadoch C.

Nat Cell Biol. 2018 Dec;20(12):1410-1420. doi: 10.1038/s41556-018-0221-1. Epub 2018 Nov 5.

31.

Targeting the Extracellular Signal-Regulated Kinase 5 Pathway to Suppress Human Chronic Myeloid Leukemia Stem Cells.

Tusa I, Cheloni G, Poteti M, Gozzini A, DeSouza NH, Shan Y, Deng X, Gray NS, Li S, Rovida E, Dello Sbarba P.

Stem Cell Reports. 2018 Oct 9;11(4):929-943. doi: 10.1016/j.stemcr.2018.08.016. Epub 2018 Sep 20.

32.

A High-Throughput Immune-Oncology Screen Identifies EGFR Inhibitors as Potent Enhancers of Antigen-Specific Cytotoxic T-lymphocyte Tumor Cell Killing.

Lizotte PH, Hong RL, Luster TA, Cavanaugh ME, Taus LJ, Wang S, Dhaneshwar A, Mayman N, Yang A, Kulkarni M, Badalucco L, Fitzpatrick E, Kao HF, Kuraguchi M, Bittinger M, Kirschmeier PT, Gray NS, Barbie DA, Jänne PA.

Cancer Immunol Res. 2018 Dec;6(12):1511-1523. doi: 10.1158/2326-6066.CIR-18-0193. Epub 2018 Sep 21.

33.

First SAR Study for Overriding NRAS Mutant Driven Acute Myeloid Leukemia.

Cho H, Shin I, Ju E, Choi S, Hur W, Kim H, Hong E, Kim ND, Choi HG, Gray NS, Sim T.

J Med Chem. 2018 Sep 27;61(18):8353-8373. doi: 10.1021/acs.jmedchem.8b00882. Epub 2018 Sep 11.

PMID:
30153003
34.

Structural and Atropisomeric Factors Governing the Selectivity of Pyrimido-benzodiazipinones as Inhibitors of Kinases and Bromodomains.

Wang J, Erazo T, Ferguson FM, Buckley DL, Gomez N, Muñoz-Guardiola P, Diéguez-Martínez N, Deng X, Hao M, Massefski W, Fedorov O, Offei-Addo NK, Park PM, Dai L, DiBona A, Becht K, Kim ND, McKeown MR, Roberts JM, Zhang J, Sim T, Alessi DR, Bradner JE, Lizcano JM, Blacklow SC, Qi J, Xu X, Gray NS.

ACS Chem Biol. 2018 Sep 21;13(9):2438-2448. doi: 10.1021/acschembio.7b00638. Epub 2018 Aug 31.

PMID:
30102854
35.

Novel Scaffolds for Dual Specificity Tyrosine-Phosphorylation-Regulated Kinase (DYRK1A) Inhibitors.

Czarna A, Wang J, Zelencova D, Liu Y, Deng X, Choi HG, Zhang T, Zhou W, Chang JW, Kildalsen H, Seternes OM, Gray NS, Engh RA, Rothweiler U.

J Med Chem. 2018 Sep 13;61(17):7560-7572. doi: 10.1021/acs.jmedchem.7b01847. Epub 2018 Aug 23.

PMID:
30095246
36.

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 Sep 14;4(9):1395-1406. doi: 10.1021/acsinfecdis.8b00127. Epub 2018 Aug 29.

37.

Specific covalent inhibition of MALT1 paracaspase suppresses B cell lymphoma growth.

Fontán L, Qiao Q, Hatcher JM, Casalena G, Us I, Teater M, Durant M, Du G, Xia M, Bilchuk N, Chennamadhavuni S, Palladino G, Inghirami G, Philippar U, Wu H, Scott DA, Gray NS, Melnick A.

J Clin Invest. 2018 Oct 1;128(10):4397-4412. doi: 10.1172/JCI99436. Epub 2018 Jul 19.

38.

BMX-Mediated Regulation of Multiple Tyrosine Kinases Contributes to Castration Resistance in Prostate Cancer.

Chen S, Cai C, Sowalsky AG, Ye H, Ma F, Yuan X, Simon NI, Gray NS, Balk SP.

Cancer Res. 2018 Sep 15;78(18):5203-5215. doi: 10.1158/0008-5472.CAN-17-3615. Epub 2018 Jul 16.

39.

Structure of the Human cGAS-DNA Complex Reveals Enhanced Control of Immune Surveillance.

Zhou W, Whiteley AT, de Oliveira Mann CC, Morehouse BR, Nowak RP, Fischer ES, Gray NS, Mekalanos JJ, Kranzusch PJ.

Cell. 2018 Jul 12;174(2):300-311.e11. doi: 10.1016/j.cell.2018.06.026.

40.

How small-molecule inhibitors of dengue-virus infection interfere with viral membrane fusion.

Chao LH, Jang J, Johnson A, Nguyen A, Gray NS, Yang PL, Harrison SC.

Elife. 2018 Jul 12;7. pii: e36461. doi: 10.7554/eLife.36461.

41.

Discovery of a Highly Potent and Broadly Effective Epidermal Growth Factor Receptor and HER2 Exon 20 Insertion Mutant Inhibitor.

Jang J, Son J, Park E, Kosaka T, Saxon JA, De Clercq DJH, Choi HG, Tanizaki J, Eck MJ, Jänne PA, Gray NS.

Angew Chem Int Ed Engl. 2018 Sep 3;57(36):11629-11633. doi: 10.1002/anie.201805187. Epub 2018 Aug 3.

42.

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.

43.

Inhibition of Flaviviruses by Targeting a Conserved Pocket on the Viral Envelope Protein.

de Wispelaere M, Lian W, Potisopon S, Li PC, Jang J, Ficarro SB, Clark MJ, Zhu X, Kaplan JB, Pitts JD, Wales TE, Wang J, Engen JR, Marto JA, Gray NS, Yang PL.

Cell Chem Biol. 2018 Aug 16;25(8):1006-1016.e8. doi: 10.1016/j.chembiol.2018.05.011. Epub 2018 Jun 21.

44.

Plasticity in binding confers selectivity in ligand-induced protein degradation.

Nowak RP, DeAngelo SL, Buckley D, He Z, Donovan KA, An J, Safaee N, Jedrychowski MP, Ponthier CM, Ishoey M, Zhang T, Mancias JD, Gray NS, Bradner JE, Fischer ES.

Nat Chem Biol. 2018 Jul;14(7):706-714. doi: 10.1038/s41589-018-0055-y. Epub 2018 Jun 11.

45.

Selective Inhibition of the Myeloid Src-Family Kinase Fgr Potently Suppresses AML Cell Growth in Vitro and in Vivo.

Weir MC, Shu ST, Patel RK, Hellwig S, Chen L, Tan L, Gray NS, Smithgall TE.

ACS Chem Biol. 2018 Jun 15;13(6):1551-1559. doi: 10.1021/acschembio.8b00154. Epub 2018 May 30.

46.

Chemically Induced Degradation of Anaplastic Lymphoma Kinase (ALK).

Powell CE, Gao Y, Tan L, Donovan KA, Nowak RP, Loehr A, Bahcall M, Fischer ES, Jänne PA, George RE, Gray NS.

J Med Chem. 2018 May 10;61(9):4249-4255. doi: 10.1021/acs.jmedchem.7b01655. Epub 2018 Apr 24.

47.

RAS-MAPK Reactivation Facilitates Acquired Resistance in FGFR1-Amplified Lung Cancer and Underlies a Rationale for Upfront FGFR-MEK Blockade.

Bockorny B, Rusan M, Chen W, Liao RG, Li Y, Piccioni F, Wang J, Tan L, Thorner AR, Li T, Zhang Y, Miao C, Ovesen T, Shapiro GI, Kwiatkowski DJ, Gray NS, Meyerson M, Hammerman PS, Bass AJ.

Mol Cancer Ther. 2018 Jul;17(7):1526-1539. doi: 10.1158/1535-7163.MCT-17-0464. Epub 2018 Apr 13.

48.

It Takes Two To Target: A Study in KRAS Dimerization.

Nabet B, Gray NS.

Biochemistry. 2018 Apr 24;57(16):2289-2290. doi: 10.1021/acs.biochem.8b00376. Epub 2018 Apr 12. No abstract available.

PMID:
29648795
49.

The dTAG system for immediate and target-specific protein degradation.

Nabet B, Roberts JM, Buckley DL, Paulk J, Dastjerdi S, Yang A, Leggett AL, Erb MA, Lawlor MA, Souza A, Scott TG, Vittori S, Perry JA, Qi J, Winter GE, Wong KK, Gray NS, Bradner JE.

Nat Chem Biol. 2018 May;14(5):431-441. doi: 10.1038/s41589-018-0021-8. Epub 2018 Mar 26.

50.

Kinase inhibitors: the road ahead.

Ferguson FM, Gray NS.

Nat Rev Drug Discov. 2018 May;17(5):353-377. doi: 10.1038/nrd.2018.21. Epub 2018 Mar 16. Review.

PMID:
29545548

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