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Analysis of the Mechanisms of Action of Naphthoquinone-Based Anti-Acute Myeloid Leukemia Chemotherapeutics.

Lee MH, Lapidus RG, Ferraris D, Emadi A.

Molecules. 2019 Aug 28;24(17). pii: E3121. doi: 10.3390/molecules24173121.


Potently inhibiting cancer cell migration with novel 3H-pyrazolo[4,3-f]quinoline boronic acid ROCK inhibitors.

Dayal N, Mikek CG, Hernandez D, Naclerio GA, Yin Chu EF, Carter-Cooper BA, Lapidus RG, Sintim HO.

Eur J Med Chem. 2019 Oct 15;180:449-456. doi: 10.1016/j.ejmech.2019.06.089. Epub 2019 Jun 29.


Regulation of cisplatin-resistant head and neck squamous cell carcinoma by the SRC/ETS-1 signaling pathway.

Yang Z, Liao J, Carter-Cooper BA, Lapidus RG, Cullen KJ, Dan H.

BMC Cancer. 2019 May 22;19(1):485. doi: 10.1186/s12885-019-5664-7.


Equipotent doses of daunorubicin and idarubicin for AML: a meta-analysis of clinical trials versus in vitro estimation.

Adige S, Lapidus RG, Carter-Cooper BA, Duffy A, Patzke C, Law JY, Baer MR, Ambulos NP, Zou Y, Bentzen SM, Emadi A.

Cancer Chemother Pharmacol. 2019 Jun;83(6):1105-1112. doi: 10.1007/s00280-019-03825-2. Epub 2019 Apr 9.


HER3-Targeted Affibodies with Optimized Formats Reduce Ovarian Cancer Progression in a Mouse Xenograft Model.

Schardt JS, Noonan-Shueh M, Oubaid JM, Pottash AE, Williams SC, Hussain A, Lapidus RG, Lipkowitz S, Jay SM.

AAPS J. 2019 Apr 4;21(3):48. doi: 10.1208/s12248-019-0318-x.


The Novel Mnk1/2 Degrader and Apoptosis Inducer VNLG-152 Potently Inhibits TNBC Tumor Growth and Metastasis.

Ramalingam S, Ramamurthy VP, Gediya LK, Murigi FN, Purushottamachar P, Huang W, Choi EY, Zhang Y, Vasaitis TS, Kane MA, Lapidus RG, Njar VCO.

Cancers (Basel). 2019 Mar 3;11(3). pii: E299. doi: 10.3390/cancers11030299.


Exploiting epigenetically mediated changes: Acute myeloid leukemia, leukemia stem cells and the bone marrow microenvironment.

Kogan AA, Lapidus RG, Baer MR, Rassool FV.

Adv Cancer Res. 2019;141:213-253. doi: 10.1016/bs.acr.2018.12.005. Epub 2019 Jan 21.


Amino alkynylisoquinoline and alkynylnaphthyridine compounds potently inhibit acute myeloid leukemia proliferation in mice.

Naganna N, Opoku-Temeng C, Choi EY, Larocque E, Chang ET, Carter-Cooper BA, Wang M, Torregrosa-Allen SE, Elzey BD, Lapidus RG, Sintim HO.

EBioMedicine. 2019 Feb;40:231-239. doi: 10.1016/j.ebiom.2019.01.012. Epub 2019 Jan 25.


Co-targeting EGFR and IKKβ/NF-κB signalling pathways in head and neck squamous cell carcinoma: a potential novel therapy for head and neck squamous cell cancer.

Li Z, Liao J, Yang Z, Choi EY, Lapidus RG, Liu X, Cullen KJ, Dan H.

Br J Cancer. 2019 Feb;120(3):306-316. doi: 10.1038/s41416-018-0351-z. Epub 2018 Dec 26.


Gamma Delta T Cell Therapy for Cancer: It Is Good to be Local.

Pauza CD, Liou ML, Lahusen T, Xiao L, Lapidus RG, Cairo C, Li H.

Front Immunol. 2018 Jun 8;9:1305. doi: 10.3389/fimmu.2018.01305. eCollection 2018. Review.


Dual FLT3/TOPK inhibitor with activity against FLT3-ITD secondary mutations potently inhibits acute myeloid leukemia cell lines.

Dayal N, Opoku-Temeng C, Hernandez DE, Sooreshjani MA, Carter-Cooper BA, Lapidus RG, Sintim HO.

Future Med Chem. 2018 Apr 1;10(7):823-835. doi: 10.4155/fmc-2017-0298. Epub 2018 Feb 13.


Asparaginase Erwinia chrysanthemi effectively depletes plasma glutamine in adult patients with relapsed/refractory acute myeloid leukemia.

Emadi A, Law JY, Strovel ET, Lapidus RG, Jeng LJB, Lee M, Blitzer MG, Carter-Cooper BA, Sewell D, Van Der Merwe I, Philip S, Imran M, Yu SL, Li H, Amrein PC, Duong VH, Sausville EA, Baer MR, Fathi AT, Singh Z, Bentzen SM.

Cancer Chemother Pharmacol. 2018 Jan;81(1):217-222. doi: 10.1007/s00280-017-3459-6. Epub 2017 Nov 8.


Concurrent Inhibition of Pim and FLT3 Kinases Enhances Apoptosis of FLT3-ITD Acute Myeloid Leukemia Cells through Increased Mcl-1 Proteasomal Degradation.

Kapoor S, Natarajan K, Baldwin PR, Doshi KA, Lapidus RG, Mathias TJ, Scarpa M, Trotta R, Davila E, Kraus M, Huszar D, Tron AE, Perrotti D, Baer MR.

Clin Cancer Res. 2018 Jan 1;24(1):234-247. doi: 10.1158/1078-0432.CCR-17-1629. Epub 2017 Oct 26.


Breaking Mitochondrial Fasting for Cancer Treatment: Old Wine in New Bottles.

Emadi A, Lapidus RG.

J Natl Cancer Inst. 2017 Nov 1;109(11). doi: 10.1093/jnci/djx069. No abstract available.


Characterization of CADD522, a small molecule that inhibits RUNX2-DNA binding and exhibits antitumor activity.

Kim MS, Gernapudi R, Choi EY, Lapidus RG, Passaniti A.

Oncotarget. 2017 Aug 10;8(41):70916-70940. doi: 10.18632/oncotarget.20200. eCollection 2017 Sep 19.


Identification of New FLT3 Inhibitors That Potently Inhibit AML Cell Lines via an Azo Click-It/Staple-It Approach.

Ma X, Zhou J, Wang C, Carter-Cooper B, Yang F, Larocque E, Fine J, Tsuji G, Chopra G, Lapidus RG, Sintim HO.

ACS Med Chem Lett. 2017 Apr 14;8(5):492-497. doi: 10.1021/acsmedchemlett.6b00468. eCollection 2017 May 11.


Aminoisoquinoline benzamides, FLT3 and Src-family kinase inhibitors, potently inhibit proliferation of acute myeloid leukemia cell lines.

Larocque E, Naganna N, Ma X, Opoku-Temeng C, Carter-Cooper B, Chopra G, Lapidus RG, Sintim HO.

Future Med Chem. 2017 Jul;9(11):1213-1225. doi: 10.4155/fmc-2017-0067. Epub 2017 May 11.


Exploring the Concept of Radiation "Booster Shot" in Combination with an Anti-PD-L1 mAb to Enhance Anti-Tumor Immune Effects in Mouse Pancreas Tumors.

Chuong M, Chang ET, Choi EY, Mahmood J, Lapidus RG, Davila E, Carrier F.

J Clin Oncol Res. 2017;5(2). pii: 1058. Epub 2017 Aug 11.


Synthesis, characterization and antineoplastic activity of bis-aziridinyl dimeric naphthoquinone - A novel class of compounds with potent activity against acute myeloid leukemia cells.

Carter-Cooper BA, Fletcher S, Ferraris D, Choi EY, Kronfli D, Dash S, Truong P, Sausville EA, Lapidus RG, Emadi A.

Bioorg Med Chem Lett. 2017 Jan 1;27(1):6-10. doi: 10.1016/j.bmcl.2016.11.045. Epub 2016 Nov 17.


Enhancing the Cytotoxic Effects of PARP Inhibitors with DNA Demethylating Agents - A Potential Therapy for Cancer.

Muvarak NE, Chowdhury K, Xia L, Robert C, Choi EY, Cai Y, Bellani M, Zou Y, Singh ZN, Duong VH, Rutherford T, Nagaria P, Bentzen SM, Seidman MM, Baer MR, Lapidus RG, Baylin SB, Rassool FV.

Cancer Cell. 2016 Oct 10;30(4):637-650. doi: 10.1016/j.ccell.2016.09.002.


Targeting IκB Kinase β/NF-κB Signaling in Human Prostate Cancer by a Novel IκB Kinase β Inhibitor CmpdA.

Zhang Y, Lapidus RG, Liu P, Choi EY, Adediran S, Hussain A, Wang X, Liu X, Dan HC.

Mol Cancer Ther. 2016 Jul;15(7):1504-14. doi: 10.1158/1535-7163.MCT-15-0999. Epub 2016 Apr 8.


Synthesis, anticancer activity, and SAR analyses of compounds containing the 5:7-fused 4,6,8-triaminoimidazo[4,5-e][1,3]diazepine ring system.

Xie M, Lapidus RG, Sadowska M, Edelman MJ, Hosmane RS.

Bioorg Med Chem. 2016 Jun 15;24(12):2595-602. doi: 10.1016/j.bmc.2016.03.015. Epub 2016 Mar 9.


Alkyne-substituted diminazene as G-quadruplex binders with anticancer activities.

Wang C, Carter-Cooper B, Du Y, Zhou J, Saeed MA, Liu J, Guo M, Roembke B, Mikek C, Lewis EA, Lapidus RG, Sintim HO.

Eur J Med Chem. 2016 Aug 8;118:266-75. doi: 10.1016/j.ejmech.2016.04.030. Epub 2016 Apr 20.


Comparative Analysis of Methods for Detecting Isocitrate Dehydrogenase 1 and 2 Mutations and Their Metabolic Consequence, 2-Hydroxyglutarate, in Different Neoplasms.

Babakoohi S, Lapidus RG, Faramand R, Sausville EA, Emadi A.

Appl Immunohistochem Mol Morphol. 2017 May/Jun;25(5):334-337. doi: 10.1097/PAI.0000000000000342. Review.


A positive feedback loop involving EGFR/Akt/mTORC1 and IKK/NF-kB regulates head and neck squamous cell carcinoma proliferation.

Li Z, Yang Z, Passaniti A, Lapidus RG, Liu X, Cullen KJ, Dan HC.

Oncotarget. 2016 May 31;7(22):31892-906. doi: 10.18632/oncotarget.7441.


Hydroxylated Dimeric Naphthoquinones Increase the Generation of Reactive Oxygen Species, Induce Apoptosis of Acute Myeloid Leukemia Cells and Are Not Substrates of the Multidrug Resistance Proteins ABCB1 and ABCG2.

Lapidus RG, Carter-Cooper BA, Sadowska M, Choi EY, Wonodi O, Muvarak N, Natarajan K, Pidugu LS, Jaiswal A, Toth EA, Rassool FV, Etemadi A, Sausville EA, Baer MR, Emadi A.

Pharmaceuticals (Basel). 2016 Jan 19;9(1). pii: E4. doi: 10.3390/ph9010004.


IKK phosphorylation of NF-κB at serine 536 contributes to acquired cisplatin resistance in head and neck squamous cell cancer.

Li Z, Yang Z, Lapidus RG, Liu X, Cullen KJ, Dan HC.

Am J Cancer Res. 2015 Sep 15;5(10):3098-110. eCollection 2015.


Differential IKK/NF-κB Activity Is Mediated by TSC2 through mTORC1 in PTEN-Null Prostate Cancer and Tuberous Sclerosis Complex Tumor Cells.

Gao Y, Gartenhaus RB, Lapidus RG, Hussain A, Zhang Y, Wang X, Dan HC.

Mol Cancer Res. 2015 Dec;13(12):1602-14. doi: 10.1158/1541-7786.MCR-15-0213. Epub 2015 Sep 15.


Perturbation of cellular oxidative state induced by dichloroacetate and arsenic trioxide for treatment of acute myeloid leukemia.

Emadi A, Sadowska M, Carter-Cooper B, Bhatnagar V, van der Merwe I, Levis MJ, Sausville EA, Lapidus RG.

Leuk Res. 2015 Jul;39(7):719-29. doi: 10.1016/j.leukres.2015.04.002. Epub 2015 Apr 30.


Presence of isocitrate dehydrogenase mutations may predict clinical response to hypomethylating agents in patients with acute myeloid leukemia.

Emadi A, Faramand R, Carter-Cooper B, Tolu S, Ford LA, Lapidus RG, Wetzler M, Wang ES, Etemadi A, Griffiths EA.

Am J Hematol. 2015 May;90(5):E77-9. doi: 10.1002/ajh.23965. Epub 2015 Feb 27.


Clinical and laboratory studies of the novel cyclin-dependent kinase inhibitor dinaciclib (SCH 727965) in acute leukemias.

Gojo I, Sadowska M, Walker A, Feldman EJ, Iyer SP, Baer MR, Sausville EA, Lapidus RG, Zhang D, Zhu Y, Jou YM, Poon J, Small K, Bannerji R.

Cancer Chemother Pharmacol. 2013 Oct;72(4):897-908. doi: 10.1007/s00280-013-2249-z. Epub 2013 Aug 15.


In vivo screening of S100B inhibitors for melanoma therapy.

Zimmer DB, Lapidus RG, Weber DJ.

Methods Mol Biol. 2013;963:303-17. doi: 10.1007/978-1-62703-230-8_18.


Structure-based drug design and potent anti-cancer activity of tricyclic 5:7:5-fused diimidazo[4,5-d:4',5'-f][1,3]diazepines.

Kondaskar A, Kondaskar S, Fishbein JC, Carter-Cooper BA, Lapidus RG, Sadowska M, Edelman MJ, Hosmane RS.

Bioorg Med Chem. 2013 Feb 1;21(3):618-31. doi: 10.1016/j.bmc.2012.11.050. Epub 2012 Dec 11.


Regulation of human RNase-L by the miR-29 family reveals a novel oncogenic role in chronic myelogenous leukemia.

Lee TY, Ezelle HJ, Venkataraman T, Lapidus RG, Scheibner KA, Hassel BA.

J Interferon Cytokine Res. 2013 Jan;33(1):34-42. doi: 10.1089/jir.2012.0062. Epub 2012 Oct 31.


Novel, Broad Spectrum Anti-Cancer Agents Containing the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System.

Kondaskar A, Kondaskar S, Kumar R, Fishbein JC, Muvarak N, Lapidus RG, Sadowska M, Edelman MJ, Bol GM, Vesuna F, Raman V, Hosmane RS.

ACS Med Chem Lett. 2010 Dec 31;2(3):252-256.


Comparison of neuropathy-inducing effects of eribulin mesylate, paclitaxel, and ixabepilone in mice.

Wozniak KM, Nomoto K, Lapidus RG, Wu Y, Carozzi V, Cavaletti G, Hayakawa K, Hosokawa S, Towle MJ, Littlefield BA, Slusher BS.

Cancer Res. 2011 Jun 1;71(11):3952-62. doi: 10.1158/0008-5472.CAN-10-4184. Epub 2011 Apr 15.


A novel, broad-spectrum anticancer compound containing the imidazo[4,5-e][1,3]diazepine ring system.

Xie M, Ujjinamatada RK, Sadowska M, Lapidus RG, Edelman MJ, Hosmane RS.

Bioorg Med Chem Lett. 2010 Aug 1;20(15):4386-9. doi: 10.1016/j.bmcl.2010.06.061. Epub 2010 Jun 15.


Glutamate carboxypeptidase inhibition reduces the severity of chemotherapy-induced peripheral neurotoxicity in rat.

Carozzi VA, Chiorazzi A, Canta A, Lapidus RG, Slusher BS, Wozniak KM, Cavaletti G.

Neurotox Res. 2010 May;17(4):380-91. doi: 10.1007/s12640-009-9114-1. Epub 2009 Sep 15.


Head and neck cancer radiosensitization by the novel poly(ADP-ribose) polymerase inhibitor GPI-15427.

Khan K, Araki K, Wang D, Li G, Li X, Zhang J, Xu W, Hoover RK, Lauter S, O'Malley B Jr, Lapidus RG, Li D.

Head Neck. 2010 Mar;32(3):381-91. doi: 10.1002/hed.21195.


Anti-tumor effect of combination therapy with intratumoral controlled-release paclitaxel (PACLIMER microspheres) and radiation.

Lapidus RG, Dang W, Rosen DM, Gady AM, Zabelinka Y, O'Meally R, DeWeese TL, Denmeade SR.

Prostate. 2004 Feb 15;58(3):291-8.


Prostate-specific membrane antigen (PSMA) enzyme activity is elevated in prostate cancer cells.

Lapidus RG, Tiffany CW, Isaacs JT, Slusher BS.

Prostate. 2000 Dec 1;45(4):350-4.


Suramin potently inhibits the enzymatic activity of PSM.

Slusher BS, Tiffany CW, Merion A, Lapidus RG, Jackson PF.

Prostate. 2000 Jun 15;44(1):55-60.


The loss of estrogen and progesterone receptor gene expression in human breast cancer.

Lapidus RG, Nass SJ, Davidson NE.

J Mammary Gland Biol Neoplasia. 1998 Jan;3(1):85-94. Review.


Characterization of the enzymatic activity of PSM: comparison with brain NAALADase.

Tiffany CW, Lapidus RG, Merion A, Calvin DC, Slusher BS.

Prostate. 1999 Apr 1;39(1):28-35.


Mapping of ER gene CpG island methylation-specific polymerase chain reaction.

Lapidus RG, Nass SJ, Butash KA, Parl FF, Weitzman SA, Graff JG, Herman JG, Davidson NE.

Cancer Res. 1998 Jun 15;58(12):2515-9.


The regulation of estrogen receptor expression and function in human breast cancer.

Ferguson AT, Lapidus RG, Davidson NE.

Cancer Treat Res. 1998;94:255-78. Review. No abstract available.


Methylation of estrogen and progesterone receptor gene 5' CpG islands correlates with lack of estrogen and progesterone receptor gene expression in breast tumors.

Lapidus RG, Ferguson AT, Ottaviano YL, Parl FF, Smith HS, Weitzman SA, Baylin SB, Issa JP, Davidson NE.

Clin Cancer Res. 1996 May;2(5):805-10.


E-cadherin expression is silenced by DNA hypermethylation in human breast and prostate carcinomas.

Graff JR, Herman JG, Lapidus RG, Chopra H, Xu R, Jarrard DF, Isaacs WB, Pitha PM, Davidson NE, Baylin SB.

Cancer Res. 1995 Nov 15;55(22):5195-9.

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