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Items: 10

1.

Rational Targeting of Cooperating Layers of the Epigenome Yields Enhanced Therapeutic Efficacy against AML.

Duy C, Teater M, Garrett-Bakelman FE, Lee TC, Meydan C, Glass JL, Li M, Hellmuth JC, Mohammad HP, Smitheman KN, Shih AH, Abdel-Wahab O, Tallman MS, Guzman ML, Muench D, Grimes HL, Roboz GJ, Kruger RG, Creasy CL, Paietta EM, Levine RL, Carroll M, Melnick AM.

Cancer Discov. 2019 May 10. doi: 10.1158/2159-8290.CD-19-0106. [Epub ahead of print]

PMID:
31076479
2.

Lysine specific demethylase 1 inactivation enhances differentiation and promotes cytotoxic response when combined with all-trans retinoic acid in acute myeloid leukemia across subtypes.

Smitheman KN, Severson TM, Rajapurkar SR, McCabe MT, Karpinich N, Foley J, Pappalardi MB, Hughes A, Halsey W, Thomas E, Traini C, Federowicz KE, Laraio J, Mobegi F, Ferron-Brady G, Prinjha RK, Carpenter CL, Kruger RG, Wessels L, Mohammad HP.

Haematologica. 2019 Jun;104(6):1156-1167. doi: 10.3324/haematol.2018.199190. Epub 2018 Dec 4.

3.

LSD1 inhibition exerts its antileukemic effect by recommissioning PU.1- and C/EBPα-dependent enhancers in AML.

Cusan M, Cai SF, Mohammad HP, Krivtsov A, Chramiec A, Loizou E, Witkin MD, Smitheman KN, Tenen DG, Ye M, Will B, Steidl U, Kruger RG, Levine RL, Rienhoff HY Jr, Koche RP, Armstrong SA.

Blood. 2018 Apr 12;131(15):1730-1742. doi: 10.1182/blood-2017-09-807024. Epub 2018 Feb 16.

4.

A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC.

Mohammad HP, Smitheman KN, Kamat CD, Soong D, Federowicz KE, Van Aller GS, Schneck JL, Carson JD, Liu Y, Butticello M, Bonnette WG, Gorman SA, Degenhardt Y, Bai Y, McCabe MT, Pappalardi MB, Kasparec J, Tian X, McNulty KC, Rouse M, McDevitt P, Ho T, Crouthamel M, Hart TK, Concha NO, McHugh CF, Miller WH, Dhanak D, Tummino PJ, Carpenter CL, Johnson NW, Hann CL, Kruger RG.

Cancer Cell. 2015 Jul 13;28(1):57-69. doi: 10.1016/j.ccell.2015.06.002.

5.

BET inhibition silences expression of MYCN and BCL2 and induces cytotoxicity in neuroblastoma tumor models.

Wyce A, Ganji G, Smitheman KN, Chung CW, Korenchuk S, Bai Y, Barbash O, Le B, Craggs PD, McCabe MT, Kennedy-Wilson KM, Sanchez LV, Gosmini RL, Parr N, McHugh CF, Dhanak D, Prinjha RK, Auger KR, Tummino PJ.

PLoS One. 2013 Aug 23;8(8):e72967. doi: 10.1371/journal.pone.0072967. eCollection 2013.

6.

Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions.

King AJ, Arnone MR, Bleam MR, Moss KG, Yang J, Fedorowicz KE, Smitheman KN, Erhardt JA, Hughes-Earle A, Kane-Carson LS, Sinnamon RH, Qi H, Rheault TR, Uehling DE, Laquerre SG.

PLoS One. 2013 Jul 3;8(7):e67583. doi: 10.1371/journal.pone.0067583. Print 2013.

7.

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.

Rheault TR, Stellwagen JC, Adjabeng GM, Hornberger KR, Petrov KG, Waterson AG, Dickerson SH, Mook RA Jr, Laquerre SG, King AJ, Rossanese OW, Arnone MR, Smitheman KN, Kane-Carson LS, Han C, Moorthy GS, Moss KG, Uehling DE.

ACS Med Chem Lett. 2013 Feb 7;4(3):358-62. doi: 10.1021/ml4000063. eCollection 2013 Mar 14.

8.

Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations.

Greger JG, Eastman SD, Zhang V, Bleam MR, Hughes AM, Smitheman KN, Dickerson SH, Laquerre SG, Liu L, Gilmer TM.

Mol Cancer Ther. 2012 Apr;11(4):909-20. doi: 10.1158/1535-7163.MCT-11-0989. Epub 2012 Mar 2.

9.

Mutation of A677 in histone methyltransferase EZH2 in human B-cell lymphoma promotes hypertrimethylation of histone H3 on lysine 27 (H3K27).

McCabe MT, Graves AP, Ganji G, Diaz E, Halsey WS, Jiang Y, Smitheman KN, Ott HM, Pappalardi MB, Allen KE, Chen SB, Della Pietra A 3rd, Dul E, Hughes AM, Gilbert SA, Thrall SH, Tummino PJ, Kruger RG, Brandt M, Schwartz B, Creasy CL.

Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):2989-94. doi: 10.1073/pnas.1116418109. Epub 2012 Feb 8.

10.

Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.

Stellwagen JC, Adjabeng GM, Arnone MR, Dickerson SH, Han C, Hornberger KR, King AJ, Mook RA Jr, Petrov KG, Rheault TR, Rominger CM, Rossanese OW, Smitheman KN, Waterson AG, Uehling DE.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4436-40. doi: 10.1016/j.bmcl.2011.06.021. Epub 2011 Jun 16.

PMID:
21733693

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