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Rena S. Lapidus, PhD

Academic Title:

Associate Professor

Primary Appointment:

Medicine

Administrative Title:

Assistant Director of the UMGCCC Shared Services

Additional Title:

Director, Translational Laboratory Shared Service

Location:

655 West Baltimore Street

Phone (Primary):

410-328-8092

Fax:

410-328-6559

Education and Training

Bachelor of Arts – Chemistry, Boston University, Boston, MA

Ph.D., University of Maryland School of Medicine, Baltimore MD, Department of Pharmacology

Post-Doctoral Fellowship, The Johns Hopkins Oncology Center

Biosketch

The Translational Laboratory Shared Service (TLSS) at UMGCC plays a critical role in ‘translating’ novel drugs from bench to bedside. We interact with clinicians and pre-clinical investigators to produce preclinical data both in vitro and in vivo in order to generate grants for research or LOIs for clinical trials. In vitro studies include proliferation and cell death assays, IC50 generation, apoptotic assays, Western analysis among others.  In vivo studies include maximum tolerated dose studies, pharmacokinetic studies (dosing of mice/plasma isolation) and cancer efficacy and pharmacodynamic studies.  Specifically, this laboratory has tested novel agents alone and in combination both in vitro and in vivo.   We have developed many novel flank, orthotopic and primary xenografts models to test novel compounds in cancer. Our laboratory is equipped with the tools necessary to generate in vivo oncology data for preclinical investigators. The TLSS also possesses an umbrella Animal Use protocol that is approved for oncology studies with UMBs  IACUC. Overall, the goal is to develop novel compounds that may lead to a Phase I clinical trial.

I am uniquely suited for this position having spent twelve years in industry working on small molecule drug development and 7 years as the Director of the TLSS.   In industry, I worked as the representative ‘biologist’ on many multi-disciplinary project teams being exposed to many of the other ‘disciplines’ including toxicology and pharmacokinetics.  My responsibilities included testing novel anti-cancer compounds in in vitro and in vivo cancer efficacy models as well as doing the ‘in-life’ for pharmacokinetic and pharmacodynamic assays.  The skills that I learned in industry are highly valuable to the researchers at UMGCC.   

Research/Clinical Keywords

Cancer Drug Development, Translational Research, Pre-clinical,In Vivo Studies for Cancer

Highlighted Publications

Muvarak NM, Chowdhury K, Robert C, Choi EY, Xia L, Cai Y, Bellani M, Singh Z, Duong V, Rutherford T, Seidman M, Baer MR, Lapidus RG, Baylin SB, Rassool FV. Effects of PARP inhibitors by DNA demethylating agents – a potential therapy for cancer. Cancer Cell 30(4): 637-650, 2016 

Lapidus RG, Carter-Cooper BA, Sadowska M, Choi E, Wonodi O, Muvarak N, Natarajan K, Pidugu LS, Jaiswal An, Toth EA, Rassool FV, Etemadi A, Sausville EA, Baer MR, Emadi A. Hydroxylated dimeric naphthoquinones increase generation of reactive oxygen species, induce apoptosis of acute myeloid leukemia cells and are not substrates of the multidrug resistance proteins ABCB1 and ABCG2  Pharmaceuticals 9(1): pii: E4 2016 

Kim MS, Gernapudi R, Choi EY, Lapidus RG, Passaniti A. Characterization of CADD522, a small molecule that inhibits RUNX2-DNA binding that exhibits antitumor activity.  Oncotarget 8(41): 70916-70940, 2017

Xie M, Lapidus RG, Sadowska M, Edelman MJ and Hosmane RS.  Synthesis, anticancer activity and SAR analyses of compounds containing the 5:7-fused 4,6,8-triaminoimidazo[4,5-e][1,3]diazepiene ring system.  Biorg Med Chem 24(12): 2595-2602, 2016.

Edelman MJ, Lapidus RG, Feliciano J, Styblo M, Beumer JH, Liu T, Gobbru J. Phase I and pharmacokinetic evaluation of the anti-telomerase agent KML001 with cisplatin in advanced solid tumors.  Cancer Chemo Pharmacol.  78(5): 959-967, 2016.

Additional Publication Citations

Lapidus RG and Sokolove PM  Inhibition of spermine of the inner membrane permeability transition of isolated rat heart mitochondria.  FEBS Lett. 313:314-318, 1992.

Streicher-Scott J, Lapidus RG and Sokolove PM  Use of carboxyatractylate and tight binding inhibitor theory to determine the concentration of functional mitochondrial adenine nucleotide translocators in a reconstituted system.  Anal. Biochem. 210:69-76, 1993.

Lapidus RG and Sokolove PM  Spermine inhibition of the permeability transition of isolated rat liver mitochondria: an investigation of mechanism.  Arch. Biochem. Biophys. 306:246-253, 1993.

Streicher-Scott J, Lapidus RG and Sokolove PM  The reconstituted mitochondrial adenine nucleotide translocator: effects of lipid polymorphism.  Arch. Biochem. Biophys. 315(2): 548-554, 1994.

Lapidus RG and Sokolove PM  The mitochondrial permeability transition: interactions of spermine, ADP and inorganic phosphate.  J. Biol. Chem., 269(29):18931-18936, 1994.

Ferguson AT, Lapidus RG, Baylin SB and Davidson NE  Demethylation of the estrogen receptor gene in estrogen receptor-negative breast cancer cells can reactivate estrogen receptor gene expression.  Cancer Res.  55: 2279-2283, 1995

Herman JG, Merlo A, Mao L, Lapidus RG, Issa J-P J, Davidson NE., Sidransky D and Baylin SB Inactivation of the CDKN2/p16/MTS1 gene is frequently associated with aberrant DNA methylation in all common human cancers.  Cancer Res. 55: 4525-4530, 1995.

Graff JR, Herman JG, Lapidus RG, Chopra H, Xu R, Jarrard DF, Isaacs WB, Pitha PM. Davidson NE and Baylin SB E-cadherin expression is silenced by DNA hypermethylation in human breast and prostate carcinomas.  Cancer Res. 55: 5195-5199, 1995.

Lapidus RG, Ferguson AT, Ottoviano YL, Parl FF, Smith HS, Weitzman SA, Issa J-P and Davidson NE Methylation of estrogen and progesterone receptor genes 5' CpG islands correlates with lack of ER and PR gene expression in breast tumors.  Clin. Cancer Res.  2(5): 805-810, 1996.

Lapidus RG, Nass SS, and Davidson NE  Loss of estrogen and progesterone receptor gene expression in breast cancer.  J. of Mammary Gland Biology and Neoplasia 3(1): 85-94, 1998 

Lapidus RG, Nass SJ, Butash KA, Parl FF, Weitzman SA,  Graff JG, Herman JG, and Davidson NE Mapping the ER gene CpG island by methylation specific PCR Cancer Res. 58(12):2515-2519, 1998.

Ferguson AT, Lapidus RG and Davidson NE Demethylation of the progesterone receptor CpG island is not required for progesterone receptor gene expression.  Oncogene 17: 577-583, 1998.

Tiffany CW, Lapidus RG, Merion A, Calvin DC and Slusher BS  Characterization of the enzymatic activity of PSM: comparison with brain NAALADase.  The Prostate 39: 28-35, 1999.

Harper EA, Dang W, Lapidus RG, and Garver RI  Enhanced efficacy of a novel controlled release paclitaxel formulation (Paclimer TM Delivery System) for local-regional therapy of lung cancer tumor nodules in mice.  Clin Cancer Research  5:4242-4248, 1999.

Slusher BS, Tiffany CW, Lapidus RG, and Jackson PF.  Suramin potently inhibits the enzymatic activity of PSM.  The Prostate  44:55-60, 2000

Lapidus RG, Tiffany CW, Isaacs JT, Slusher BS. Prostate specific membrane antigen (PSMA) enzyme activity is elevated in prostate cancer cells.  The Prostate 45:350-354, 2000.

Lapidus RG, Dang W, Rosen M, Gady AM, Zabelinka Y, O’Meally R, DeWeese TL, Denmeade SR. Antitumor effect of combination therapy with intratumoral controlled-release paclitaxel (PACLIMER´âĺ Microspheres) and radiation.  The Prostate  58(3): 291-298, 2004.

Tentori L, Leonetti C, Scarsella M, Vergai M, Xu W, Calvin D, Morgan L, Tang Z, Wozniak K, Alemu C, Hoover R, Lapidus RG,  Zhang J, Graziani G.  Brain distribution and efficacy as chemosensitizer of oral formulations of PARP-1 inhibitor GPI 15427 in experimental models of CNS.  Int J. Oncol  26: 415-432, 2005.

Tentori L, Leonetti C, Scarsella M, Muzi A, Mazzon E, Vergati M, Forini O, Lapidus R, Xu W, Dorio AS, Zhang J, Cuzzocrea S, Graziani G.  Inhibition of poly(ADP-ribose) polymerase prevents irinotecan-induced intestinal damage and enhances irinotecan/temozolomide efficacy against colon carcinoma.  FASEB J. 20(10): 1709-1711, 2005.

Humblet V, Lapidus RG, Williams LR, Tsukamot T, Rojas C, Majer P, Ohnishi S, De Grand AM, Zaheer A, Renze JT, Nakayama A, Slusher BS and Frangioni JV.  High Affinity Near-Infrared flurorescent small molecule contrast agent for in vivo imaging of prostate-specific membrane antigen.  Molecular Imaging  4(4):  448-462, 2005.

Khan K, Li G, Li X, Zhang J, Xu W, Hoover RK,  O'Malley Jr BW, Lapidus RG  and Li D.  GPI-15427, a novel poly(ADP-ribose) polymerase-1 inhibitor, enhances the tumoricidal effect of radiation in head and neck cancer.  Head Neck 32(3):  381-391, 2010.

Carozzi VA, Chiorazzi A, Canta A, Lapidus RG, Slusher BS, Wozniak KM, Cavaletti G.   Glutamate carboxypeptidase inhibition reduces the severity of chemotherapy-induced peripheral neurotoxicity in rat. Neurotox Res  17: 380-391, 2010.

Xie M, Ujjinamatada RK, Sadowska M, Lapidus RG, Edelman M and Hosmane RS. A novel, broad spectrum anti-cancer compound containing the Imidazo[4,5-e][1,3]diazepine Ring System.  Bioorganic and Medicinal Chemistry Letters 20(15):4386-9 2010

Kondaskar A, Kondaskar S, Kumar R, Muvarak N, Lapidus RG, Sadowska M, Edelman MJ, Bol GM, Raman V and Hosmane RS  A Series of Novel, Broad Spectrum Anti-Cancer AgentsContaining the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System  ACS Med Chem Letters  2(3):  252-256, 2010.

Wozniak KM, Nomoto K, Lapidus RG, Wu Y, Carozzi V, Cavaletti G, Hayakawa K, Hosokawa S, Towle MJ, Littlefield BA, Slusher BS. Comparison of neuropathy-inducing effects of eribulin mesylate, paclitaxel and exabepilone in mice.  Cancer Res. 71(11): 3952-3962, 2011.

Wozniak KM, Wu Y, Vornov JJ, Lapidus R, Rais R, Rojas C, Tsukamoto T, Slusher BS. The orally active glutamate carboxypeptidase II inhibitor E2072 exhibits sustained nerve exposure and attenuates peripheral neuropathy. J Pharmacol Exp Ther 343(3): 746-754, 2012.

Lee TY, Ezelle HJ, Venkataraman T, Lapidus RG, Scheibner K, Hassel BA: Regulation of human RNase L by the miR-29 family reveals a novel oncogenic role in chronic myelogenous leukemia  J Interferon and Cytokine Res  33(1): 34-42, 2013

Kondaskar A, Kondaskar S, Fishbein JC, Carter-Cooper, BA, Lapidus RG, Sadowska M, Edelman MJ and Hosmane RS.  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.  Biorg Med Chem 21(3): 618-631, 2013

Zimmer DB, Lapidus RG, Weber DJ. In vivo screening of S100B inhibitors for melanoma therapy Methods Mol Biol. 963:303-17, 2013.

Gojo I, Tan M, Fang H-B, Sadowska M, Lapidus R, Baer MR, Carrier F, Beumer JH, Anyang BN, Holleran JL, Srivastava RK, Espinoza-Delgado I, Ross DD. Translational phase I trial of vorinostat combined with cytarabine and etoposide in patients with relapsed, refractory, or high-risk acute myeloid leukemia  Clin Cancer Res 19(7):1838-1851 2013

Gojo I, Sadowska M, Walker A, Cooper M, Feldman EJ, Padmanabhan W, Baer MR, Sausville EA, Lapidus RG, Zhang D, Zhu Y, Jou Y-M, Poon J, Small K and Bannerji R. Clinical and laboratory studies of the novel cyclin-dependent kinase inhibitor dinaciclib (SCH 727965) in acute leukemias.   Cancer Chemotherapy and Pharmacology 72(4): 897-908, 2013

Bao T, Goloubeva O, Porter N, Primrose j, Wang L, Hester L, Sadowska M, Lapidus RG, Medeiros M, Lao L, Dorsey S, Badros AZ. A Pilot Study of Acupuncture in Treating Bortezomib-Induced Peripheral Neuropathy in Multiple Myeloma Patients  Integr Cancer Ther 13(5): 396-404, 2013

Yu KH, Sangar V, Ricigliano M, Hidalgo M, O’Reilly EM, Abou-Alfa GK, Lowery M, Saltz LB, Crotty J, Gary K, Cooper B, Lapidus R, Sadowska M.  Pharmacogenomic Modeling of Circulating Tumor and Invasive Cells for Prediction of Chemotherapy Response and Resistance in Pancreatic Cancer Clin Cancer Res 20(20): 5281-5289, 2014. PMCID: Not listed

Emadi A, Faramand R, Carter-Cooper B, Tolu S, Ford LA, Lapidus RG, Wetzler M, Wang ES, Etemadi A, Griffiths EA. Presence of Isocitrate dehydrogenase may predict clinical response to hypo-methylating agents with acute myeloid leukemia (AML)   Am J Hematology 90(5);  E77-E79, 2015

Emadi A, Sadowska M, Carter-Cooper B, Bhatnagar V, van der Merwe I, Levis MJ, Sausville EA, Lapidus RG.  Perturbation of cellular oxidative stress induced by dichloroacetate and arsenic trioxide for treatment of acute myeloid leukemia.    Leukemia Res  39(7): 719-729, 2015.

Gao Y, Gartenhaus R, Lapidus RG, Hussain A, Zhang Y, Wang X., Dan HC  Differential IKK/NF-kB activity  by TSC2 through mTORC1 in PTEN loss prostate cancer and tuberous sclerosis complex tumor cells. Mol Cancer Res 13(12): 1602-1614, 2015

Dan,  HC, Li Z, Lapidus, RG, Liu X, Cullen KJ and Yang, Z.  IKKβ phosphorylatiom of NF-κB at serine 536 contributes to acquired cisplatin resistance in head and neck squamous cell cancer. Am J Cancer Res 5(10): 3098-3110, 2015

Lapidus RG, Carter-Cooper BA, Sadowska M, Choi E, Wonodi O, Muvarak N, Natarajan K, Pidugu LS, Jaiswal An, Toth EA, Rassool FV, Etemadi A, Sausville EA, Baer MR, Emadi A. Hydroxylated dimeric naphthoquinones increase generation of reactive oxygen species, induce apoptosis of acute myeloid leukemia cells and are not substrates of the multidrug resistance proteins ABCB1 and ABCG2  Pharmaceuticals 9(1): pii: E4 2016

Li Z, Yang Z, Passaniti A, Lapidus RG, Liu X, Cullen KJ, Dan HC. A positive feedback loop involving EGFR/Akt/mTORC1 and IKK/NF-kB regulated head and neck squamous cell carcinoma proliferation.  Oncotarget 7(22): 31892-31906, 2016.

Babakoohi S, Lapidus RG, Faramand R, Sausville EA, Emadi A. Comparative analysis of methods for detectingisocitrate dehydrogenase 1 and 2 mutations and their metabolic consequence, 2-hydroxyglutarate, in different neoplasms.  Appl Imunohistochem Mol Morphol.  2016.  Epub ahead of print.

Zhang y, Lapidus RG, Liu P, Choi EY, Adediran S, Hussain A, Wang X, Liu X, Dan HC. Targeting IkB kinase b/NF-KB signaling in human prostate cancer by a novel IkB kinase b inhibitor CmpdA.  Mol Cancer Ther  15(7): 1504-1514, 2016

Wang C, Carter-Cooper B, Du Y, Zhou J, Saeed M, Liu J, Roembke BT, Mikek C, Lewis EA, Lapidus RG and Sintim HO. Alkyne-substituted diminazene as G-quadraplex binders with anti-cancer activities.  Eur J Med Chem  118: 266-275, 2016

Muvarak NM, Chowdhury K, Robert C, Choi EY, Xia L, Cai Y, Bellani M, Singh Z, Duong V, Rutherford T, Seidman M, Baer MR, Lapidus RG, Baylin SB, Rassool FV. Effects of PARP inhibitors by DNA demethylating agents – a potential therapy for cancer. Cancer Cell 30(4): 637-650, 2016

Xie M, Lapidus RG, Sadowska M, Edelman MJ and Hosmane RS.  Synthesis, anticancer activity and SAR analyses of compounds containing the 5:7-fused 4,6,8-triaminoimidazo[4,5-e][1,3]diazepiene ring system.  Biorg Med Chem 24(12): 2595-2602, 2016.

Edelman MJ, Lapidus RG, Feliciano J, Styblo M, Beumer JH, Liu T, Gobbru J. Phase I and pharmacokinetic evaluation of the anti-telomerase agent KML001 with cisplatin in advanced solid tumors.  Cancer Chemo Pharmacol.  78(5): 959-967, 2016.

Carter-Cooper BA, Fletcher S, Ferraris D, Choi EY, Kronfli D, Dash S, Truong P, Sausville EA, Lapidus RG, Emadi A.  Synthesis, characterization and anti-neoplastic activity of bis-aziridine dimeric naphthoquinone – a novel class of compounds with potent activity against acute myeloid leukemia cells. Bioorg Med Chem Lett 27(1); 6-10, 2016

Ma X, Zhou J, Wang C, Carter-Cooper B, Yang F, Larocque E, Fine J, Tsuji G, Chopra G, Lapidus RG, Sintim HO.  Identification of new FLT3 inhibitors that potently inhibits AML cell lines, via a click-it-staple-it approach. ACS Medicinal Chemistry Letters 8: 492-497, 2017

Larocque E, Naganna N, Max X, Opoku-Temeng C, Carter-Cooper B, Chopra G, Lapidus RG, Sintim HO. Aminoisoquinoline benzamides, FLT3 and Src-family kinase inhibitors, potently inhibit proliferation of acute myeloid leukemia cell lines.  Future Med Chem 9(11): 1213-1225, 2017

Li Z, Li D, Choi EY, Lapidus RG, Zhang L, Huang S-M, Raman CS, Shaprio P, Wang H. Silencing of solute carrier family 13 member 5 disrupts energy homeostasis and inhibits proliferation of human hepatocarcinoma.  J Biol Chem  292(33): 13890-13901, 2017

Emadi AE and Lapidus RG  Breaking the mitochondrial fasting for cancer treatment:  Old wine in new bottles.  JNCI 109 (11) Nov 2017 

Kapoor S, Natarajan K, Baldwin P, Doshi K, Lapidus R, Mathia T, Scarpa M, Trotta R, Davila E, Kraus M, Huszar D, Tron A, Perrotti D and Baer M.  Concurrent inhibition of Pim and FLT3 kinases enhances apoptosis of FLT3-ITD acute myeloid leukemia cells through increased Mcl-1 proteasomal degradation Clin Cancer Res 2017 epub ahead of print

Kim MS, Gernapudi R, Choi EY, Lapidus RG, Passaniti A. Characterization of CADD522, a small molecule that inhibits RUNX2-DNA binding that exhibits antitumor activity.  Oncotarget 8(41): 70916-70940, 2017

Research Interests

Development of novel treatments for acute myeloid leukemia.

  1. Gojo I, Tan M, Fang HB, Sadowska M, Lapidus R, Baer MR, Carrier F, Beumer JH, Anyang BN, Srivastava RK, Espinoza-Delgado I, Ross DD. Translational phase I trial of vorinostat (suberoylanilide hydroxamic acid) combined with cytarabine and etoposide in patients with relapsed, refractory, or high-risk acute myeloid leukemia. Clin Cancer Res. 2013 Apr 1;19(7):1838-51. PubMed PMID: 23403629; PubMed Central PMCID: PMC4332848.
  2. 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. Clinical and laboratory studies of the novel cyclin-dependent kinase inhibitor dinaciclib (SCH 727965) in acute leukemias. Cancer Chemother Pharmacol. 2013 Oct;72(4):897-908. PubMed PMID: 23949430; PubMed Central PMCID: PMC3784060.
  3. Emadi A, Faramand R, Carter-Cooper B, Tolu S, Ford LA, Lapidus RG, Wetzler M, Wang ES, Etemadi A, Griffiths EA. Presence of isocitrate dehydrogenase mutations may predict clinical response to hypomethylating agents in patients with acute myeloid leukemia. Am J Hematol. 2015 May;90(5):E77-9. PubMed PMID: 25651001.
  4. Lapidus RG, Carter-Cooper BA, Sadowska M, Choi E, Wonodi O, Muvarak N, Natarajan K, Pidugu LS, Jaiswal An, Toth EA, Rassool FV, Etemadi A, Sausville EA, Baer MR, Emadi A. Hydroxylated dimeric naphthoquinones increase generation of reactive oxygen species, induce apoptosis of acute myeloid leukemia cells and are not substrates of the multidrug resistance proteins ABCB1 and ABCG2  Pharmaceuticals 2016 Jan; 9(10): pii  PMID: 26797621

 Studied the role of epigenetic silencing of genes in breast cancer

 Herman JG, Merlo A, Mao L, Lapidus RG, Issa JP, Davidson NE, Sidransky D, Baylin SB. Inactivation of the CDKN2/p16/MTS1 gene is frequently associated with aberrant DNA methylation in all common human cancers. Cancer Res. 1995 Oct 15;55(20):4525-30. PubMed PMID: 7553621.

  1. Lapidus RG, Ferguson AT, Ottaviano YL, Parl FF, Smith HS, Weitzman SA, Baylin SB, Issa JP, Davidson NE. Methylation of estrogen and progesterone receptor gene 5' CpG islands correlates with lack of estrogen and progesterone receptor gene expression in breast tumors. Clin Cancer Res. 1996 May;2(5):805-10. PubMed PMID: 9816234.
  2. Lapidus RG, Nass SJ, Davidson NE. The loss of estrogen and progesterone receptor gene expression in human breast cancer. J Mammary Gland Biol Neoplasia. 1998 Jan;3(1):85-94. PubMed PMID: 10819507.
  3. Lapidus RG, Nass SJ, Butash KA, Parl FF, Weitzman SA, Graff JG, Herman JG, Davidson NE. Mapping of ER gene CpG island methylation-specific polymerase chain reaction. Cancer Res. 1998 Jun 15;58(12):2515-9. PubMed PMID: 9635570

Discovery and research of PARP inhibitors as chemo-sensitizers

  1. Tentori L, Leonetti C, Scarsella M, Vergati M, Xu W, Calvin D, Morgan L, Tang Z, Woznizk K, Alemu C, Hoover R, Lapidus R, Zhang J, Graziani G. Brain distribution and efficacy as chemosensitizer of an oral formulation of PARP-1 inhibitor GPI 15427 in experimental models of CNS tumors. Int J Oncol. 2005 Feb;26(2):415-22. PubMed PMID: 15645126.
  2. Tentori L, Leonetti C, Scarsella M, Muzi A, Mazzon E, Vergati M, Forini O, Lapidus R, Xu W, Dorio AS, Zhang J, Cuzzocrea S, Graziani G. Inhibition of poly(ADP-ribose) polymerase prevents irinotecan-induced intestinal damage and enhances irinotecan/temozolomide efficacy against colon carcinoma. FASEB J. 2006 Aug;20(10):1709-11. PubMed PMID: 16809434.
  3. 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 and neck cancer radiosensitization by the novel poly(ADP-ribose) polymerase inhibitor GPI-15427. Head Neck. 2010 Mar;32(3):381-91. PubMed PMID: 19672867

Spermine inhibition of the mitochondrial permeability transition.

  1. Lapidus RG, Sokolove PM. Inhibition by spermine of the inner membrane permeability transition of isolated rat heart mitochondria. FEBS Lett. 1992 Nov 30;313(3):314-8. PubMed PMID: 1446752.
  2. Lapidus RG, Sokolove PM. Spermine inhibition of the permeability transition of isolated rat liver mitochondria: an investigation of mechanism. Arch Biochem Biophys. 1993 Oct;306(1):246-53. PubMed PMID: 8215411.
  3. Lapidus RG, Sokolove PM. The mitochondrial permeability transition. Interactions of spermine, ADP, and inorganic phosphate. J Biol Chem. 1994 Jul 22;269(29):18931-6. PubMed PMID: 8034650

Development of novel Glutamate Carboxypeptidase II inhibitors to protect against chemotherapy induced neuropathy

  1. Carozzi VA, Chiorazzi A, Canta A, Lapidus RG, Slusher BS, Wozniak KM, Cavaletti G. Glutamate carboxypeptidase inhibition reduces the severity of chemotherapy-induced peripheral neurotoxicity in rat. Neurotox Res. 2010 May;17(4):380-91. PubMed PMID: 19763734.
  2. Wozniak KM, Nomoto K, Lapidus RG, Wu Y, Carozzi V, Cavaletti G, Hayakawa K, Hosokawa S, Towle MJ, Littlefield BA, Slusher BS. Comparison of neuropathy-inducing effects of eribulin mesylate, paclitaxel, and ixabepilone in mice. Cancer Res. 2011 Jun 1;71(11):3952-62. PubMed PMID: 21498637.
  3. Wozniak KM, Wu Y, Vornov JJ, Lapidus R, Rais R, Rojas C, Tsukamoto T, Slusher BS. The orally active glutamate carboxypeptidase II inhibitor E2072 exhibits sustained nerve exposure and attenuates peripheral neuropathy. J Pharmacol Exp Ther. 2012 Dec;343(3):746-54. PubMed PMID: 22988061

 

Links of Interest

http://www.umm.edu/programs/cancer/