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675576-98-4 | 4-[[(4S,5R)-4,5-Bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone
CAS No: 675576-98-4 Catalog No: AG003APZ MDL No:MFCD14636430
Product Description
Catalog Number:
AG003APZ
Chemical Name:
4-[[(4S,5R)-4,5-Bis(4-chlorophenyl)-4,5-dihydro-2-[4-methoxy-2-(1-methylethoxy)phenyl]-1H-imidazol-1-yl]carbonyl]-2-piperazinone
CAS Number:
675576-98-4
Molecular Formula:
C30H30Cl2N4O4
Molecular Weight:
581.4896
MDL Number:
MFCD14636430
IUPAC Name:
4-[(4S,5R)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]piperazin-2-one
InChI:
InChI=1S/C30H30Cl2N4O4/c1-18(2)40-25-16-23(39-3)12-13-24(25)29-34-27(19-4-8-21(31)9-5-19)28(20-6-10-22(32)11-7-20)36(29)30(38)35-15-14-33-26(37)17-35/h4-13,16,18,27-28H,14-15,17H2,1-3H3,(H,33,37)/t27-,28+/m0/s1
InChI Key:
BDUHCSBCVGXTJM-WUFINQPMSA-N
SMILES:
COc1ccc(c(c1)OC(C)C)C1=N[C@H]([C@H](N1C(=O)N1CCNC(=O)C1)c1ccc(cc1)Cl)c1ccc(cc1)Cl
UNII:
L7C92IOE65
Properties
Complexity:
919
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1
Defined Atom Stereocenter Count:
2
Defined Bond Stereocenter Count:
0
Exact Mass:
580.164g/mol
Formal Charge:
0
Heavy Atom Count:
40
Hydrogen Bond Acceptor Count:
5
Hydrogen Bond Donor Count:
1
Isotope Atom Count:
0
Molecular Weight:
581.494g/mol
Monoisotopic Mass:
580.164g/mol
Rotatable Bond Count:
6
Topological Polar Surface Area:
83.5A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
5.2
Literature
| Title | Journal |
|---|---|
| p53 and NF-κB coregulate proinflammatory gene responses in human macrophages. | Cancer research 20140415 |
| Nutlin-3 overcomes arsenic trioxide resistance and tumor metastasis mediated by mutant p53 in Hepatocellular Carcinoma. | Molecular cancer 20140101 |
| Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development. | ACS medicinal chemistry letters 20130509 |
| SOCS1 is significantly up-regulated in Nutlin-3-treated p53wild-type B chronic lymphocytic leukemia (B-CLL) samples and shows an inverse correlation with miR-155. | Investigational new drugs 20121201 |
| An iTRAQ proteomics screen reveals the effects of the MDM2 binding ligand Nutlin-3 on cellular proteostasis. | Journal of proteome research 20121102 |
| The sorafenib plus nutlin-3 combination promotes synergistic cytotoxicity in acute myeloid leukemic cells irrespectively of FLT3 and p53 status. | Haematologica 20121101 |
| DNA damage response by single-strand breaks in terminally differentiated muscle cells and the control of muscle integrity. | Cell death and differentiation 20121101 |
| A novel combination therapy approach for the treatment of acute myeloid leukemia: the multi-kinase inhibitor sorafenib and the HDM2 inhibitor nutlin-3. | Haematologica 20121101 |
| Discovery of novel dihydroimidazothiazole derivatives as p53-MDM2 protein-protein interaction inhibitors: synthesis, biological evaluation and structure-activity relationships. | Bioorganic & medicinal chemistry letters 20121015 |
| Combination treatment in vitro with Nutlin, a small-molecule antagonist of MDM2, and pegylated interferon-α 2a specifically targets JAK2V617F-positive polycythemia vera cells. | Blood 20121011 |
| Structure-activity relationship and antitumor activity of thio-benzodiazepines as p53-MDM2 protein-protein interaction inhibitors. | European journal of medicinal chemistry 20121001 |
| Differential regulation of p21 (waf1) protein half-life by DNA damage and Nutlin-3 in p53 wild-type tumors and its therapeutic implications. | Cancer biology & therapy 20120901 |
| A novel function of p53: a gatekeeper of retinal detachment. | The American journal of pathology 20120901 |
| Ras homolog gene family, member A promotes p53 degradation and vascular endothelial growth factor-dependent angiogenesis through an interaction with murine double minute 2 under hypoxic conditions. | Cancer 20120901 |
| Competitive binding between dynamic p53 transactivation subdomains to human MDM2 protein: implications for regulating the p53·MDM2/MDMX interaction. | The Journal of biological chemistry 20120831 |
| MDM2 overexpression deregulates the transcriptional control of RB/E2F leading to DNA methyltransferase 3A overexpression in lung cancer. | Clinical cancer research : an official journal of the American Association for Cancer Research 20120815 |
| Nutlin-3 differentially modulates miRNA34a and miRNA181 versus miR26a and miR155 in p53 proficient and p53 deficient B chronic lymphocytic leukemia (B-CLL) samples. | Investigational new drugs 20120801 |
| The tumour suppressor p53 is frequently nonfunctional in Sézary syndrome. | The British journal of dermatology 20120801 |
| Inauhzin and Nutlin3 synergistically activate p53 and suppress tumor growth. | Cancer biology & therapy 20120801 |
| The over-expression of miR-34a fails to block DoHH2 lymphoma cell proliferation by reducing p53 via c-MYC down-regulation. | Nucleic acid therapeutics 20120801 |
| Integrin α5β1 plays a critical role in resistance to temozolomide by interfering with the p53 pathway in high-grade glioma. | Cancer research 20120715 |
| Pharmacological activation of the p53 pathway by nutlin-3 exerts anti-tumoral effects in medulloblastomas. | Neuro-oncology 20120701 |
| ATM and MET kinases are synthetic lethal with nongenotoxic activation of p53. | Nature chemical biology 20120701 |
| The histone acetyltransferase PCAF regulates p21 transcription through stress-induced acetylation of histone H3. | Cell cycle (Georgetown, Tex.) 20120701 |
| Comparison of the antitumor effects of an MDM2 inhibitor, nutlin-3, in feline lymphoma cell lines with or without p53 mutation. | Veterinary immunology and immunopathology 20120630 |
| Structure-based design of novel inhibitors of the MDM2-p53 interaction. | Journal of medicinal chemistry 20120614 |
| Ink4a and Arf are crucial factors in the determination of the cell of origin and the therapeutic sensitivity of Myc-induced mouse lymphoid tumor. | Oncogene 20120607 |
| Chk2 mediates RITA-induced apoptosis. | Cell death and differentiation 20120601 |
| Alpha-melanocyte-stimulating hormone suppresses oxidative stress through a p53-mediated signaling pathway in human melanocytes. | Molecular cancer research : MCR 20120601 |
| The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction. | Bioorganic & medicinal chemistry letters 20120515 |
| Pharmacological inhibition of Mdm2 triggers growth arrest and promotes DNA breakage in mouse colon tumors and human colon cancer cells. | Molecular carcinogenesis 20120501 |
| Activation of the p53 pathway induces α-smooth muscle actin expression in both myeloid leukemic cells and normal macrophages. | Journal of cellular physiology 20120501 |
| Synergistic induction of p53 mediated apoptosis by valproic acid and nutlin-3 in acute myeloid leukemia. | Leukemia 20120501 |
| p53 and MDM2 are involved in the regulation of osteocalcin gene expression. | Experimental cell research 20120501 |
| An evaluation of small-molecule p53 activators as chemoprotectants ameliorating adverse effects of anticancer drugs in normal cells. | Cell cycle (Georgetown, Tex.) 20120501 |
| Reversible induction of PARP1 degradation by p53-inducible cis-imidazoline compounds. | Biochemical and biophysical research communications 20120427 |
| The MDM2 inhibitor Nutlin-3 modulates dendritic cell-induced T cell proliferation. | Human immunology 20120401 |
| Nutlin-3 induces apoptosis, disrupts viral latency and inhibits expression of angiopoietin-2 in Kaposi sarcoma tumor cells. | Cell cycle (Georgetown, Tex.) 20120401 |
| Human neuroblastoma cells with acquired resistance to the p53 activator RITA retain functional p53 and sensitivity to other p53 activating agents. | Cell death & disease 20120401 |
| Structural insights into the dual-targeting mechanism of Nutlin-3. | Biochemical and biophysical research communications 20120330 |
| MDM2 antagonism by nutlin-3 induces death in human medulloblastoma cells. | Neuroscience letters 20120328 |
| Synergistic growth inhibition based on small-molecule p53 activation as treatment for intraocular melanoma. | Oncogene 20120301 |
| Decreased sensitivity of 17p-deleted chronic lymphocytic leukemia cells to a small molecule BCL-2 antagonist ABT-737. | Cancer 20120215 |
| MYCN sensitizes neuroblastoma to the MDM2-p53 antagonists Nutlin-3 and MI-63. | Oncogene 20120209 |
| Histone deacetylase inhibitors enhance the anticancer activity of nutlin-3 and induce p53 hyperacetylation and downregulation of MDM2 and MDM4 gene expression. | Investigational new drugs 20120201 |
| p53 rescue through HDM2 antagonism suppresses melanoma growth and potentiates MEK inhibition. | The Journal of investigative dermatology 20120201 |
| Inability of p53-reactivating compounds Nutlin-3 and RITA to overcome p53 resistance in tumor cells deficient in p53Ser46 phosphorylation. | Biochemical and biophysical research communications 20120120 |
| Fibroid explants reveal a higher sensitivity against MDM2-inhibitor nutlin-3 than matching myometrium. | BMC women's health 20120101 |
| Folate decorated dual drug loaded nanoparticle: role of curcumin in enhancing therapeutic potential of nutlin-3a by reversing multidrug resistance. | PloS one 20120101 |
| p53 modulation as a therapeutic strategy in gastrointestinal stromal tumors. | PloS one 20120101 |
| Binding of Translationally Controlled Tumour Protein to the N-terminal domain of HDM2 is inhibited by nutlin-3. | PloS one 20120101 |
| HDM2 antagonist MI-219 (spiro-oxindole), but not Nutlin-3 (cis-imidazoline), regulates p53 through enhanced HDM2 autoubiquitination and degradation in human malignant B-cell lymphomas. | Journal of hematology & oncology 20120101 |
| MEK-ERK signaling dictates DNA-repair gene MGMT expression and temozolomide resistance of stem-like glioblastoma cells via the MDM2-p53 axis. | Stem cells (Dayton, Ohio) 20111201 |
| Synchronized release of Doxil and Nutlin-3 by remote degradation of polysaccharide matrices and its possible use in the local treatment of colorectal cancer. | Journal of drug targeting 20111201 |
| Adaptation of cancer cells from different entities to the MDM2 inhibitor nutlin-3 results in the emergence of p53-mutated multi-drug-resistant cancer cells. | Cell death & disease 20111201 |
| Acquisition of p53 mutations in response to the non-genotoxic p53 activator Nutlin-3. | Oncogene 20111117 |
| MDM2-p53 protein-protein interaction inhibitors: a-ring substituted isoindolinones. | Bioorganic & medicinal chemistry letters 20111001 |
| Inhibition of MDM2 attenuates neointimal hyperplasia via suppression of vascular proliferation and inflammation. | Cardiovascular research 20110901 |
| Nutlin-3 downregulates the expression of the oncogene TCL1 in primary B chronic lymphocytic leukemic cells. | Clinical cancer research : an official journal of the American Association for Cancer Research 20110901 |
| The power of chemotherapeutic engineering: arresting cell cycle and suppressing senescence to protect from mitotic inhibitors. | Cell cycle (Georgetown, Tex.) 20110715 |
| MDM2 antagonist nutlin-3a reverses mitoxantrone resistance by inhibiting breast cancer resistance protein mediated drug transport. | Biochemical pharmacology 20110701 |
| A small-molecule p53 activator induces apoptosis through inhibiting MDMX expression in breast cancer cells. | Neoplasia (New York, N.Y.) 20110701 |
| Treatment with a BH3 mimetic overcomes the resistance of latency III EBV (+) cells to p53-mediated apoptosis. | Cell death & disease 20110701 |
| Targeting the p53 pathway in retinoblastoma with subconjunctival Nutlin-3a. | Cancer research 20110615 |
| Anticancer effects of the p53 activator nutlin-3 in Ewing's sarcoma cells. | European journal of cancer (Oxford, England : 1990) 20110601 |
| Functional analysis of the p53 pathway in neuroblastoma cells using the small-molecule MDM2 antagonist nutlin-3. | Molecular cancer therapeutics 20110601 |
| Mechanism-specific signatures for small-molecule p53 activators. | Cell cycle (Georgetown, Tex.) 20110515 |
| Understanding small-molecule binding to MDM2: insights into structural effects of isoindolinone inhibitors from NMR spectroscopy. | Chemical biology & drug design 20110501 |
| Inhibition of Mdm2 sensitizes human retinal pigment epithelial cells to apoptosis. | Investigative ophthalmology & visual science 20110501 |
| miR-34a induces the downregulation of both E2F1 and B-Myb oncogenes in leukemic cells. | Clinical cancer research : an official journal of the American Association for Cancer Research 20110501 |
| Activation of the p53 pathway by the MDM2 inhibitor nutlin-3a overcomes BCL2 overexpression in a preclinical model of diffuse large B-cell lymphoma associated with t(14;18)(q32;q21). | Leukemia 20110501 |
| Blockade of Hsp90 by 17AAG antagonizes MDMX and synergizes with Nutlin to induce p53-mediated apoptosis in solid tumors. | Cell death & disease 20110501 |
| Synthetic protocol published for promising anticancer compound. | Future medicinal chemistry 20110501 |
| An Mdm2 antagonist, Nutlin-3a, induces p53-dependent and proteasome-mediated poly(ADP-ribose) polymerase1 degradation in mouse fibroblasts. | Biochemical and biophysical research communications 20110415 |
| Disruption of the MDM2-p53 interaction strongly potentiates p53-dependent apoptosis in cisplatin-resistant human testicular carcinoma cells via the Fas/FasL pathway. | Cell death & disease 20110401 |
| Targeted nutlin-3a loaded nanoparticles inhibiting p53-MDM2 interaction: novel strategy for breast cancer therapy. | Nanomedicine (London, England) 20110401 |
| Isoindolinone inhibitors of the murine double minute 2 (MDM2)-p53 protein-protein interaction: structure-activity studies leading to improved potency. | Journal of medicinal chemistry 20110310 |
| Haploinsufficiency for ribosomal protein genes causes selective activation of p53 in human erythroid progenitor cells. | Blood 20110303 |
| Potent in vitro and in vivo antitumor effects of MDM2 inhibitor nutlin-3 in gastric cancer cells. | Cancer science 20110301 |
| Exploring long-term protection of normal human fibroblasts and epithelial cells from chemotherapy in cell culture. | Oncotarget 20110301 |
| HMGA2 and p14Arf: major roles in cellular senescence of fibroids and therapeutic implications. | Anticancer research 20110301 |
| Suppression of p53 activity through the cooperative action of Ski and histone deacetylase SIRT1. | The Journal of biological chemistry 20110225 |
| Dasatinib plus Nutlin-3 shows synergistic antileukemic activity in both p53 wild-type and p53 mutated B chronic lymphocytic leukemias by inhibiting the Akt pathway. | Clinical cancer research : an official journal of the American Association for Cancer Research 20110215 |
| Molecular mimicry-based repositioning of nutlin-3 to anti-apoptotic Bcl-2 family proteins. | Journal of the American Chemical Society 20110209 |
| Nutlin-3a is a potential therapeutic for ewing sarcoma. | Clinical cancer research : an official journal of the American Association for Cancer Research 20110201 |
| MDM2 antagonist can inhibit tumor growth in hepatocellular carcinoma with different types of p53 in vitro. | Journal of gastroenterology and hepatology 20110201 |
| Epithelial cell adhesion molecule targeted nutlin-3a loaded immunonanoparticles for cancer therapy. | Acta biomaterialia 20110101 |
| Mdm2 inhibition induces apoptosis in p53 deficient human colon cancer cells by activating p73- and E2F1-mediated expression of PUMA and Siva-1. | Apoptosis : an international journal on programmed cell death 20110101 |
| p53-Reactivating small molecules induce apoptosis and enhance chemotherapeutic cytotoxicity in head and neck squamous cell carcinoma. | Oral oncology 20110101 |
| Treatment of ovarian cancer cells with nutlin-3 and resveratrol combination leads to apoptosis via caspase activation. | Journal of medicinal food 20110101 |
| A p53-independent role for the MDM2 antagonist Nutlin-3 in DNA damage response initiation. | BMC cancer 20110101 |
| Pharmacologic activation of p53 by small-molecule MDM2 antagonists. | Current pharmaceutical design 20110101 |
| Recent advances in the therapeutic perspectives of Nutlin-3. | Current pharmaceutical design 20110101 |
| Activation of p53 by nutlin-3a induces apoptosis and cellular senescence in human glioblastoma multiforme. | PloS one 20110101 |
| MDM2 antagonists boost antitumor effect of androgen withdrawal: implications for therapy of prostate cancer. | Molecular cancer 20110101 |
| MDM2 antagonist Nutlin-3a potentiates antitumour activity of cytotoxic drugs in sarcoma cell lines. | BMC cancer 20110101 |
| Transcriptional and post-transcriptional mechanisms for oncogenic overexpression of ether à go-go K+ channel. | PloS one 20110101 |
| Oncogenic functions of hMDMX in in vitro transformation of primary human fibroblasts and embryonic retinoblasts. | Molecular cancer 20110101 |
| Elimination of proliferating cells unmasks the shift from senescence to quiescence caused by rapamycin. | PloS one 20110101 |
| MDM2 antagonist Nutlin-3 enhances bortezomib-mediated mitochondrial apoptosis in TP53-mutated mantle cell lymphoma. | Cancer letters 20101228 |
| p53 prevents progression of nevi to melanoma predominantly through cell cycle regulation. | Pigment cell & melanoma research 20101201 |
| mTOR and its link to the picture of Dorian Gray - re-activation of mTOR promotes aging. | Aging 20101201 |
| Contrasting effects of nutlin-3 on TRAIL- and docetaxel-induced apoptosis due to upregulation of TRAIL-R2 and Mcl-1 in human melanoma cells. | Molecular cancer therapeutics 20101201 |
| DNA damaging agents and p53 do not cause senescence in quiescent cells, while consecutive re-activation of mTOR is associated with conversion to senescence. | Aging 20101201 |
| Hypoxia downregulates p53 but induces apoptosis and enhances expression of BAD in cultures of human syncytiotrophoblasts. | American journal of physiology. Cell physiology 20101101 |
| Shifting senescence into quiescence by turning up p53. | Cell cycle (Georgetown, Tex.) 20101101 |
| Weak p53 permits senescence during cell cycle arrest. | Cell cycle (Georgetown, Tex.) 20101101 |
| p53: The pivot between cell cycle arrest and senescence. | Cell cycle (Georgetown, Tex.) 20101101 |
| The p53 inducing drug dosage may determine quiescence or senescence. | Aging 20101101 |
| Evaluation of an Actinomycin D/VX-680 aurora kinase inhibitor combination in p53-based cyclotherapy. | Oncotarget 20101101 |
| p53-dependent repression of polo-like kinase-1 (PLK1). | Cell cycle (Georgetown, Tex.) 20101015 |
| Nutlin-3 cooperates with doxorubicin to induce apoptosis of human hepatocellular carcinoma cells through p53 or p73 signaling pathways. | Journal of cancer research and clinical oncology 20101001 |
| HDMX-L is expressed from a functional p53-responsive promoter in the first intron of the HDMX gene and participates in an autoregulatory feedback loop to control p53 activity. | The Journal of biological chemistry 20100917 |
| Molecular mechanisms of nutlin-induced apoptosis in multiple myeloma: evidence for p53-transcription-dependent and -independent pathways. | Cancer biology & therapy 20100915 |
| Combination of nutlin-3 and VX-680 selectively targets p53 mutant cells with reversible effects on cells expressing wild-type p53. | Cell death and differentiation 20100901 |
| Disruption of p73-MDM2 binding synergizes with gemcitabine to induce apoptosis in HuCCT1 cholangiocarcinoma cell line with p53 mutation. | Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine 20100801 |
| The C terminus of p53 binds the N-terminal domain of MDM2. | Nature structural & molecular biology 20100801 |
| Characterization and optimization of a novel protein-protein interaction biosensor high-content screening assay to identify disruptors of the interactions between p53 and hDM2. | Assay and drug development technologies 20100801 |
| Nutlin-3, the small-molecule inhibitor of MDM2, promotes senescence and radiosensitises laryngeal carcinoma cells harbouring wild-type p53. | British journal of cancer 20100713 |
| MDM4 (MDMX) is overexpressed in chronic lymphocytic leukaemia (CLL) and marks a subset of p53wild-type CLL with a poor cytotoxic response to Nutlin-3. | British journal of haematology 20100701 |
| Low-dose mithramycin exerts its anticancer effect via the p53 signaling pathway and synergizes with nutlin-3 in gynecologic cancers. | Cancer science 20100601 |
| Decision-making by p53 and mTOR. | Aging 20100601 |
| The choice between p53-induced senescence and quiescence is determined in part by the mTOR pathway. | Aging 20100601 |
| Enhancement of imatinib-induced apoptosis of BCR/ABL-expressing cells by nutlin-3 through synergistic activation of the mitochondrial apoptotic pathway. | Apoptosis : an international journal on programmed cell death 20100501 |
| 1,25-dihydroxyvitamin D3 enhances the apoptotic activity of MDM2 antagonist nutlin-3a in acute myeloid leukemia cells expressing wild-type p53. | Molecular cancer therapeutics 20100501 |
| Role of Mdm4 in drug sensitivity of breast cancer cells. | Oncogene 20100422 |
| Therapeutic potential of Mdm2 inhibition in malignant germ cell tumours. | European urology 20100401 |
| Inactivation of p53 signaling by p73 or PTEN ablation results in a transformed phenotype that remains susceptible to Nutlin-3 mediated apoptosis. | Cell cycle (Georgetown, Tex.) 20100401 |
| Motexafin gadolinium enhances p53-Mdm2 interactions, reducing p53 and downstream targets in lymphoma cell lines. | Anticancer research 20100401 |
| The oncogene DEK promotes leukemic cell survival and is downregulated by both Nutlin-3 and chlorambucil in B-chronic lymphocytic leukemic cells. | Clinical cancer research : an official journal of the American Association for Cancer Research 20100315 |
| Foxp3 expression in p53-dependent DNA damage responses. | The Journal of biological chemistry 20100312 |
| Determination of nutlin-3a in murine plasma by liquid chromatography electrospray ionization tandem mass spectrometry (LC-ESI-MS/MS). | Journal of pharmaceutical and biomedical analysis 20100311 |
| Phosphorylation of serine 392 in p53 is a common and integral event during p53 induction by diverse stimuli. | Cellular signalling 20100301 |
| Perifosine plus nutlin-3 combination shows a synergistic anti-leukaemic activity. | British journal of haematology 20100301 |
| Differential sensitivity of the inner ear sensory cell populations to forced cell cycle re-entry and p53 induction. | Journal of neurochemistry 20100301 |
| DNA damage response to the Mdm2 inhibitor nutlin-3. | Biochemical pharmacology 20100215 |
| The expression levels of the pro-apoptotic XAF-1 gene modulate the cytotoxic response to Nutlin-3 in B chronic lymphocytic leukemia. | Leukemia 20100201 |
| Nutlin-3 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL)-induced apoptosis through up-regulation of death receptor 5 (DR5) in human sarcoma HOS cells and human colon cancer HCT116 cells. | Cancer letters 20100101 |
| Selective FLT3 inhibitor FI-700 neutralizes Mcl-1 and enhances p53-mediated apoptosis in AML cells with activating mutations of FLT3 through Mcl-1/Noxa axis. | Leukemia 20100101 |
| Protection of p53 wild type cells from taxol by nutlin-3 in the combined lung cancer treatment. | BMC cancer 20100101 |
| Activation of endogenous p53 by combined p19Arf gene transfer and nutlin-3 drug treatment modalities in the murine cell lines B16 and C6. | BMC cancer 20100101 |
| High level MycN expression in non-MYCN amplified neuroblastoma is induced by the combination treatment nutlin-3 and doxorubicin and enhances chemosensitivity. | Oncology reports 20091201 |
| Interactions of the Hdm2/p53 and proteasome pathways may enhance the antitumor activity of bortezomib. | Clinical cancer research : an official journal of the American Association for Cancer Research 20091201 |
| Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction. | Journal of medicinal chemistry 20091126 |
| Antitumor activity of the selective MDM2 antagonist nutlin-3 against chemoresistant neuroblastoma with wild-type p53. | Journal of the National Cancer Institute 20091118 |
| Differential microRNA-34a expression and tumor suppressor function in retinoblastoma cells. | Investigative ophthalmology & visual science 20091001 |
| Nutlin-3, an Hdm2 antagonist, inhibits tumor adaptation to hypoxia by stimulating the FIH-mediated inactivation of HIF-1alpha. | Carcinogenesis 20091001 |
| Awakening p53 in senescent cells using nutlin-3. | Aging 20091001 |
| Reduced transcriptional activity in the p53 pathway of senescent cells revealed by the MDM2 antagonist nutlin-3. | Aging 20091001 |
| Nutlin-3 affects expression and function of retinoblastoma protein: role of retinoblastoma protein in cellular response to nutlin-3. | The Journal of biological chemistry 20090925 |
| Activation of p53 by MDM2 antagonists has differential apoptotic effects on Epstein-Barr virus (EBV)-positive and EBV-negative Burkitt's lymphoma cells. | Leukemia 20090901 |
| Specific activation of the p53 pathway by low dose actinomycin D: a new route to p53 based cyclotherapy. | Cell cycle (Georgetown, Tex.) 20090901 |
| MI-63: a novel small-molecule inhibitor targets MDM2 and induces apoptosis in embryonal and alveolar rhabdomyosarcoma cells with wild-type p53. | British journal of cancer 20090901 |
| Correcting miR-15a/16 genetic defect in New Zealand Black mouse model of CLL enhances drug sensitivity. | Molecular cancer therapeutics 20090901 |
| HIPK2 regulation by MDM2 determines tumor cell response to the p53-reactivating drugs nutlin-3 and RITA. | Cancer research 20090801 |
| Identification of a disruptor of the MDM2-p53 protein-protein interaction facilitated by high-throughput in silico docking. | Bioorganic & medicinal chemistry letters 20090715 |
| Restoration of p53 pathway by nutlin-3 induces cell cycle arrest and apoptosis in human rhabdomyosarcoma cells. | Clinical cancer research : an official journal of the American Association for Cancer Research 20090615 |
| Exposure of B cell chronic lymphocytic leukemia (B-CLL) cells to nutlin-3 induces a characteristic gene expression profile, which correlates with nutlin-3-mediated cytotoxicity. | Current cancer drug targets 20090601 |
| The MDM2 antagonist nutlin-3 sensitizes p53-null neuroblastoma cells to doxorubicin via E2F1 and TAp73. | International journal of oncology 20090501 |
| Nutlin-3 up-regulates the expression of Notch1 in both myeloid and lymphoid leukemic cells, as part of a negative feedback antiapoptotic mechanism. | Blood 20090430 |
| Stabilization and activation of p53 downregulates mTOR signaling through AMPK in mantle cell lymphoma. | Leukemia 20090401 |
| Depletion of guanine nucleotides leads to the Mdm2-dependent proteasomal degradation of nucleostemin. | Cancer research 20090401 |
| Reactivation of p53 function in synovial sarcoma cells by inhibition of p53-HDM2 interaction. | Cancer letters 20090318 |
| Parthenolide promotes the ubiquitination of MDM2 and activates p53 cellular functions. | Molecular cancer therapeutics 20090301 |
| MDM2 antagonist nutlin-3 displays antiproliferative and proapoptotic activity in mantle cell lymphoma. | Clinical cancer research : an official journal of the American Association for Cancer Research 20090201 |
| Reversal of P-glycoprotein-mediated multidrug resistance by the murine double minute 2 antagonist nutlin-3. | Cancer research 20090115 |
| Small-molecule inhibitors of the MDM2-p53 protein-protein interaction to reactivate p53 function: a novel approach for cancer therapy. | Annual review of pharmacology and toxicology 20090101 |
| Syntaxin 6, a regulator of the protein trafficking machinery and a target of the p53 family, is required for cell adhesion and survival. | The Journal of biological chemistry 20081107 |
| Involvement of p53 and Raf/MEK/ERK pathways in hematopoietic drug resistance. | Leukemia 20081101 |
| MDM2 E3 ubiquitin ligase mediates UT-A1 urea transporter ubiquitination and degradation. | American journal of physiology. Renal physiology 20081101 |
| RHAMM is differentially expressed in the cell cycle and downregulated by the tumor suppressor p53. | Cell cycle (Georgetown, Tex.) 20081101 |
| Concomitant inhibition of Mdm2-p53 interaction and Aurora kinases activates the p53-dependent postmitotic checkpoints and synergistically induces p53-mediated mitochondrial apoptosis along with reduced endoreduplication in acute myelogenous leukemia. | Blood 20081001 |
| E2F-1 transcriptional activity is a critical determinant of Mdm2 antagonist-induced apoptosis in human tumor cell lines. | Oncogene 20080911 |
| The dual PI3 kinase/mTOR inhibitor PI-103 prevents p53 induction by Mdm2 inhibition but enhances p53-mediated mitochondrial apoptosis in p53 wild-type AML. | Leukemia 20080901 |
| NMR screening for lead compounds using tryptophan-mutated proteins. | Journal of medicinal chemistry 20080828 |
| Multiple p53-independent gene silencing mechanisms define the cellular response to p53 activation. | Cell cycle (Georgetown, Tex.) 20080801 |
| A novel functional assay using etoposide plus nutlin-3a detects and distinguishes between ATM and TP53 mutations in CLL. | Leukemia 20080701 |
| BH3 activation blocks Hdmx suppression of apoptosis and cooperates with Nutlin to induce cell death. | Cell cycle (Georgetown, Tex.) 20080701 |
| Hdm2 and nitric oxide radicals contribute to the p53-dependent radioadaptive response. | International journal of radiation oncology, biology, physics 20080601 |
| Quantitative lid dynamics of MDM2 reveals differential ligand binding modes of the p53-binding cleft. | Journal of the American Chemical Society 20080521 |
| Differential effects of chemotherapeutic drugs versus the MDM-2 antagonist nutlin-3 on cell cycle progression and induction of apoptosis in SKW6.4 lymphoblastoid B-cells. | Journal of cellular biochemistry 20080515 |
| Nutlin-3a activates p53 to both down-regulate inhibitor of growth 2 and up-regulate mir-34a, mir-34b, and mir-34c expression, and induce senescence. | Cancer research 20080501 |
| Inhibition of the Akt/survivin pathway synergizes the antileukemia effect of nutlin-3 in acute lymphoblastic leukemia cells. | Molecular cancer therapeutics 20080501 |
| Triptolide sensitizes AML cells to TRAIL-induced apoptosis via decrease of XIAP and p53-mediated increase of DR5. | Blood 20080401 |
| MDM2 antagonist nutlin-3 is a potent inducer of apoptosis in pediatric acute lymphoblastic leukemia cells with wild-type p53 and overexpression of MDM2. | Leukemia 20080401 |
| Nutlin-3 radiosensitizes hypoxic prostate cancer cells independent of p53. | Molecular cancer therapeutics 20080401 |
| HDM2 antagonist Nutlin-3 disrupts p73-HDM2 binding and enhances p73 function. | Oncogene 20080207 |
| Combined treatment of CpG-oligodeoxynucleotide with Nutlin-3 induces strong immune stimulation coupled to cytotoxicity in B-chronic lymphocytic leukemic (B-CLL) cells. | Journal of leukocyte biology 20080201 |
| Activation of the p53 pathway down-regulates the osteoprotegerin expression and release by vascular endothelial cells. | Blood 20080201 |
| Disruption of the p53-Mdm2 complex by Nutlin-3 reveals different cancer cell phenotypes. | Ethnicity & disease 20080101 |
| Exploration of liquid and supercritical fluid chromatographic chiral separation and purification of Nutlin-3--a small molecule antagonist of MDM2. | Journal of pharmaceutical and biomedical analysis 20071221 |
| p53-mediated growth suppression in response to Nutlin-3 in cyclin D1 transformed cells occurs independently of p21. | Cancer research 20071015 |
| MDM2 antagonist Nutlin-3 suppresses the proliferation and differentiation of human pre-osteoclasts through a p53-dependent pathway. | Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 20071001 |
| The MDM-2 antagonist nutlin-3 promotes the maturation of acute myeloid leukemic blasts. | Neoplasia (New York, N.Y.) 20071001 |
| Respiratory syncytial virus decreases p53 protein to prolong survival of airway epithelial cells. | Journal of immunology (Baltimore, Md. : 1950) 20070901 |
| Nutlin-3 inhibits the NFkappaB pathway in a p53-dependent manner: implications in lung cancer therapy. | Cell cycle (Georgetown, Tex.) 20070901 |
| Hyperubiquitylation of wild-type p53 contributes to cytoplasmic sequestration in neuroblastoma. | Cell death and differentiation 20070701 |
| Analysis of the MDM2 antagonist nutlin-3 in human prostate cancer cells. | The Prostate 20070601 |
| Inhibition of p53-murine double minute 2 interaction by nutlin-3A stabilizes p53 and induces cell cycle arrest and apoptosis in Hodgkin lymphoma. | Clinical cancer research : an official journal of the American Association for Cancer Research 20070601 |
| Synergistic cytotoxic activity of recombinant TRAIL plus the non-genotoxic activator of the p53 pathway nutlin-3 in acute myeloid leukemia cells. | Current drug metabolism 20070501 |
| Pharmacologic activation of p53-dependent and p53-independent apoptotic pathways in Hodgkin/Reed-Sternberg cells. | Leukemia 20070401 |
| Mitogen-activated protein kinase kinase inhibition enhances nuclear proapoptotic function of p53 in acute myelogenous leukemia cells. | Cancer research 20070401 |
| [TP53 and RB tumor suppressor pathways collaborate in retinoblastoma genesis]. | Medecine sciences : M/S 20070401 |
| Nutlin-3 protects kidney cells during cisplatin therapy by suppressing Bax/Bak activation. | The Journal of biological chemistry 20070126 |
| Antiangiogenic activity of the MDM2 antagonist nutlin-3. | Circulation research 20070105 |
| Mdm2 is critically and continuously required to suppress lethal p53 activity in vivo. | Cancer cell 20061201 |
| Concomitant inhibition of MDM2 and Bcl-2 protein function synergistically induce mitochondrial apoptosis in AML. | Cell cycle (Georgetown, Tex.) 20061201 |
| Hdmx modulates the outcome of p53 activation in human tumor cells. | The Journal of biological chemistry 20061103 |
| Cancer biology: second step to retinal tumours. | Nature 20061102 |
| Inactivation of the p53 pathway in retinoblastoma. | Nature 20061102 |
| Nongenotoxic p53 activation protects cells against S-phase-specific chemotherapy. | Cancer research 20061101 |
| Circumvention and reactivation of the p53 oncogene checkpoint in mouse colon tumors. | Biochemical pharmacology 20061016 |
| Small-molecule MDM2 antagonists as a new therapy concept for neuroblastoma. | Cancer research 20061001 |
| Small molecule inhibition of HDM2 leads to p53-mediated cell death in retinoblastoma cells. | Archives of ophthalmology (Chicago, Ill. : 1960) 20060901 |
| MDM2 inhibition sensitizes neuroblastoma to chemotherapy-induced apoptotic cell death. | Molecular cancer therapeutics 20060901 |
| Mdm2 inhibitor Nutlin-3a induces p53-mediated apoptosis by transcription-dependent and transcription-independent mechanisms and may overcome Atm-mediated resistance to fludarabine in chronic lymphocytic leukemia. | Blood 20060801 |
| A second p53 binding site in the central domain of Mdm2 is essential for p53 ubiquitination. | Biochemistry 20060801 |
| (R)-roscovitine (CYC202, Seliciclib) sensitizes SH-SY5Y neuroblastoma cells to nutlin-3-induced apoptosis. | Experimental cell research 20060715 |
| Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy. | Journal of medicinal chemistry 20060629 |
| The epithelial cell transforming sequence 2, a guanine nucleotide exchange factor for Rho GTPases, is repressed by p53 via protein methyltransferases and is required for G1-S transition. | Cancer research 20060615 |
| Functional integrity of the p53-mediated apoptotic pathway induced by the nongenotoxic agent nutlin-3 in B-cell chronic lymphocytic leukemia (B-CLL). | Blood 20060515 |
| MDM2 antagonists activate p53 and synergize with genotoxic drugs in B-cell chronic lymphocytic leukemia cells. | Blood 20060515 |
| An shRNA barcode screen provides insight into cancer cell vulnerability to MDM2 inhibitors. | Nature chemical biology 20060401 |
| Levels of HdmX expression dictate the sensitivity of normal and transformed cells to Nutlin-3. | Cancer research 20060315 |
| WOX1 is essential for tumor necrosis factor-, UV light-, staurosporine-, and p53-mediated cell death, and its tyrosine 33-phosphorylated form binds and stabilizes serine 46-phosphorylated p53. | The Journal of biological chemistry 20051230 |
| Nongenotoxic activation of the p53 pathway as a therapeutic strategy for multiple myeloma. | Blood 20051115 |
| MDM2 antagonists induce p53-dependent apoptosis in AML: implications for leukemia therapy. | Blood 20051101 |
| Monitoring the effects of antagonists on protein-protein interactions with NMR spectroscopy. | Journal of the American Chemical Society 20050928 |
| Phosphorylation of p53 on key serines is dispensable for transcriptional activation and apoptosis. | The Journal of biological chemistry 20041217 |
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