Wee1 Inhibition by MK-1775 Leads to Tumor Inhibition and Enhances Efficacy of Gemcitabine in Human Sarcomas

PLoS ONE

Volumn 8, Issue 3, 2013, Pages

  Kreahling, Jenny M ^a   Foroutan, Parastou ^a   Reed, Damon ^a   Martinez, Gary ^a   Razabdouski, Tiffany ^b   Bui, Marilyn M ^a   Raghavan, Meera ^a   Letson, Douglas ^a   Gillies, Robert J ^a   Altiok, Soner ^a  

^a H LEE MOFFITT CANCER CENTER AND RESEARCH INSTITUTE   (United States)

^b UNIVERSITY OF SOUTH FLORIDA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GEMCITABINE; MK 1775; PHOSPHOTRANSFERASE; PHOSPHOTRANSFERASE INHIBITOR; PROTEIN P53; UNCLASSIFIED DRUG; WEE1 KINASE;

ADULT; ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; APOPTOSIS; ARTICLE; CANCER CLASSIFICATION; CANCER INHIBITION; CANCER PATIENT; CELL DIFFERENTIATION; CONTROLLED STUDY; CYTOTOXICITY; DRUG EFFICACY; EX VIVO STUDY; FEMALE; HISTOPATHOLOGY; HUMAN; HUMAN TISSUE; IN VITRO STUDY; MITOSIS; MOUSE; NONHUMAN; NUCLEAR MAGNETIC RESONANCE IMAGING; OSTEOSARCOMA; SARCOMA CELL; TREATMENT RESPONSE;

ADOLESCENT; ADULT; ANIMALS; ANTIMETABOLITES, ANTINEOPLASTIC; CELL CYCLE PROTEINS; CELL DEATH; CELL DIFFERENTIATION; CELL LINE, TUMOR; CHILD; CHILD, PRESCHOOL; DEOXYCYTIDINE; DRUG SYNERGISM; FEMALE; FEMORAL NEOPLASMS; HUMANS; MALE; MICE; MICE, SCID; MIDDLE AGED; NEOPLASM TRANSPLANTATION; NUCLEAR PROTEINS; OSTEOSARCOMA; PROTEIN-TYROSINE KINASES; PYRAZOLES; PYRIMIDINES; TRANSPLANTATION, HETEROLOGOUS; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 84874777985     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0057523     Document Type: Article

References (43)

1. Ludwig J, Trent JC (2008) Targeted Therapy in Sarcoma. In: Kurzrock RM M, editor. Targeted Cancer Therapy. Humana Press. 317-329.
2. Blanke CD, Rankin C, Demetri GD, Ryan CW, Von Mehren M, et al. (2008) Phase III randomized, intergroup trial assessing imatinib mesylate at two dose levels in patients with unresectable or metastatic gastrointestinal stromal tumors expressing the kit receptor tyrosine kinase: S0033. Journal of clinical oncology: official journal of the American Society of Clinical Oncology 26: 626-632.
3. Helleday T, Petermann E, Lundin C, Hodgson B, Sharma RA, (2008) DNA repair pathways as targets for cancer therapy. Nature reviews Cancer 8: 193-204.
4. Jin P, Gu Y, Morgan DO, (1996) Role of inhibitory CDC2 phosphorylation in radiation-induced G2 arrest in human cells. The Journal of cell biology 134: 963-970.
5. O'Connell MJ, Raleigh JM, Verkade HM, Nurse P, (1997) Chk1 is a wee1 kinase in the G2 DNA damage checkpoint inhibiting cdc2 by Y15 phosphorylation. The EMBO journal 16: 545-554.
6. Perry JA, Kornbluth S, (2007) Cdc25 and Wee1: analogous opposites? Cell division 2: 12.
7. De Witt Hamer PC, Mir SE, Noske D, Van Noorden CJF, Würdinger T, (2011) WEE1 kinase targeting combined with DNA-damaging cancer therapy catalyzes mitotic catastrophe. Clinical cancer research: an official journal of the American Association for Cancer Research 17: 4200-4207.
8. Merck Sharp & Dohme Corp. aSoMC I (n.d.) Investigator's Brochure, MK-11775.
9. Kiviharju-af Hällström TM, Jäämaa S, Mönkkönen M, Peltonen K, Andersson LC, et al. (2007) Human prostate epithelium lacks Wee1A-mediated DNA damage-induced checkpoint enforcement. Proceedings of the National Academy of Sciences of the United States of America 104: 7211-7216.
10. Rajeshkumar N V, De Oliveira E, Ottenhof N, Watters J, Brooks D, et al. (2011) MK-1775, a potent Wee1 inhibitor, synergizes with gemcitabine to achieve tumor regressions, selectively in p53-deficient pancreatic cancer xenografts. Clinical cancer research: an official journal of the American Association for Cancer Research 17: 2799-2806.
11. Mizuarai S, Yamanaka K, Itadani H, Arai T, Nishibata T, et al. (2009) Discovery of gene expression-based pharmacodynamic biomarker for a p53 context-specific anti-tumor drug Wee1 inhibitor. Molecular cancer 8: 34.
12. Hirai H, Arai T, Okada M, Nishibata T, Kobayashi M, et al. (2010) MK-1775, a small molecule Wee1 inhibitor, enhances anti-tumor efficacy of various DNA-damaging agents, including 5-fluorouracil. Cancer biology & therapy 9: 514-522.
13. Kreahling JM, Gemmer JY, Reed D, Letson D, Bui M, et al. (2012) MK1775, a selective Wee1 inhibitor, shows single-agent antitumor activity against sarcoma cells. Molecular cancer therapeutics 11: 174-182.
14. Ewald B, Sampath D, Plunkett W, (2007) H2AX phosphorylation marks gemcitabine-induced stalled replication forks and their collapse upon S-phase checkpoint abrogation. Molecular cancer therapeutics 6: 1239-1248.
15. Crescenzi E, Chiaviello A, Canti G, Reddi E, Veneziani BM, et al. (2006) Low doses of cisplatin or gemcitabine plus Photofrin/photodynamic therapy: Disjointed cell cycle phase-related activity accounts for synergistic outcome in metastatic non-small cell lung cancer cells (H1299). Molecular cancer therapeutics 5: 776-785.
16. Pauwels B, Korst AEC, Pattyn GGO, Lambrechts HAJ, Van Bockstaele DR, et al. (2003) Cell cycle effect of gemcitabine and its role in the radiosensitizing mechanism in vitro. International journal of radiation oncology, biology, physics 57: 1075-1083.
17. Martín Y, Domínguez-Kelly R, Freire R, (2011) Novel insights into maintaining genomic integrity: Wee1 regulating Mus81/Eme1. Cell division 6: 21.
18. Aarts M, Sharpe R, Garcia-Murillas I, Gevensleben H, Hurd MS, et al. (2012) Forced mitotic entry of S-phase cells as a therapeutic strategy induced by inhibition of WEE1. Cancer discovery 2: 524-539.
19. Murrow LM, Garimella S V, Jones TL, Caplen NJ, Lipkowitz S, (2010) Identification of WEE1 as a potential molecular target in cancer cells by RNAi screening of the human tyrosine kinome. Breast cancer research and treatment 122: 347-357.
20. Yoshida T, Tanaka S, Mogi A, Shitara Y, Kuwano H, (2004) The clinical significance of Cyclin B1 and Wee1 expression in non-small-cell lung cancer. Annals of oncology: official journal of the European Society for Medical Oncology/ESMO 15: 252-256.
21. Hirai H, Iwasawa Y, Okada M, Arai T, Nishibata T, et al. (2009) Small-molecule inhibition of Wee1 kinase by MK-1775 selectively sensitizes p53-deficient tumor cells to DNA-damaging agents. Molecular cancer therapeutics 8: 2992-3000.
22. Indovina P, Giordano A, (2010) Targeting the checkpoint kinase WEE1: selective sensitization of cancer cells to DNA-damaging drugs. Cancer biology & therapy 9: 523-525.
23. Hall PA, Lane DP, (1994) p53 in tumour pathology: can we trust immunohistochemistry? -Revisited! The Journal of pathology 172: 1-4.
24. Lepelley P, Preudhomme C, Vanrumbeke M, Quesnel B, Cosson A, et al. (1994) Detection of p53 mutations in hematological malignancies: comparison between immunocytochemistry and DNA analysis. Leukemia: official journal of the Leukemia Society of America, Leukemia Research Fund, UK 8: 1342-1349.
25. Marks JR, Davidoff AM, Kerns BJ, Humphrey PA, Pence JC, et al. (1991) Overexpression and mutation of p53 in epithelial ovarian cancer. Cancer research 51: 2979-2984.
26. Wynford-Thomas D, (1992) P53 in tumour pathology: can we trust immunocytochemistry? The Journal of pathology 166: 329-330.
27. Levine AJ, (1997) p53, the cellular gatekeeper for growth and division. Cell 88: 323-331.
28. Finlay CA, Hinds PW, Tan TH, Eliyahu D, Oren M, et al. (1988) Activating mutations for transformation by p53 produce a gene product that forms an hsc70-p53 complex with an altered half-life. Molecular and cellular biology 8: 531-539.
29. Kraiss S, Spiess S, Reihsaus E, Montenarh M, (1991) Correlation of metabolic stability and altered quaternary structure of oncoprotein p53 with cell transformation. Experimental cell research 192: 157-164.
30. Fletcher CDM, Unni KK (2002) World Health Organization Classification of Tumours Pathology and Genetics of Tumours of Soft Tissue and Bone.
31. PosthumaDeBoer J, Würdinger T, Graat HCA, Van Beusechem VW, Helder MN, et al. (2011) WEE1 inhibition sensitizes osteosarcoma to radiotherapy. BMC cancer 11: 156.
32. Schellens JH, Leijen S, Shapiro GI, Pavlick AC, Tibes R, et al. (2009) A phase I and pharmacological study of MK-1775, a Wee1 tyrosine kinase inhibitor, in both monotherapy and in combination with gemcitabine, cisplatin, or carboplatin in patients with advanced solid tumors.- ASCO. ASCO Annual Meeting.
33. Rubio-Viqueira B, Mezzadra H, Nielsen ME, Jimeno A, Zhang X, et al. (2007) Optimizing the development of targeted agents in pancreatic cancer: tumor fine-needle aspiration biopsy as a platform for novel prospective ex vivo drug sensitivity assays. Molecular cancer therapeutics 6: 515-523.
34. Bucher N, Britten CD, (2008) G2 checkpoint abrogation and checkpoint kinase-1 targeting in the treatment of cancer. British journal of cancer 98: 523-528.
35. Stein GS, Lian JB, Stein JL, Van Wijnen AJ, Montecino M, (1996) Transcriptional control of osteoblast growth and differentiation. Physiological reviews 76: 593-629.
36. Aubin JE (1998) Bone stem cells. Journal of cellular biochemistry Supplement 30-31: 73-82.
37. Bodine P V, Trailsmith M, Komm BS, (1996) Development and characterization of a conditionally transformed adult human osteoblastic cell line. Journal of bone and mineral research: the official journal of the American Society for Bone and Mineral Research 11: 806-819.
38. Feuerbach D, Loetscher E, Buerki K, Sampath TK, Feyen JH, (1997) Establishment and characterization of conditionally immortalized stromal cell lines from a temperature-sensitive T-Ag transgenic mouse. Journal of bone and mineral research: the official journal of the American Society for Bone and Mineral Research 12: 179-190.
39. Stanford JL, Szklo M, Brinton LA, (1986) Estrogen receptors and breast cancer. Epidemiologic reviews 8: 42-59.
40. Jenster G, (1999) The role of the androgen receptor in the development and progression of prostate cancer. Seminars in oncology 26: 407-421.
41. Housset M, Daniel MT, Degos L, (1982) Small doses of ARA-C in the treatment of acute myeloid leukaemia: differentiation of myeloid leukaemia cells? British journal of haematology 51: 125-129.
42. Fenaux P, Chomienne C, Degos L, (2001) All-trans retinoic acid and chemotherapy in the treatment of acute promyelocytic leukemia. Seminars in hematology 38: 13-25.
43. López-Carballo G, Moreno L, Masiá S, Pérez P, Barettino D, (2002) Activation of the phosphatidylinositol 3-kinase/Akt signaling pathway by retinoic acid is required for neural differentiation of SH-SY5Y human neuroblastoma cells. The Journal of biological chemistry 277: 25297-25304.