Drugging the undruggables: exploring the ubiquitin system for drug development
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[1] Toshihiko Ogura,et al. Identification of a Primary Target of Thalidomide Teratogenicity , 2010, Science.
[2] R. Deshaies,et al. Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation , 2001, Proceedings of the National Academy of Sciences of the United States of America.
[3] Brian Raught,et al. A Strategy for Modulation of Enzymes in the Ubiquitin System , 2013, Science.
[4] Christine Yu,et al. Ubiquitin Chain Editing Revealed by Polyubiquitin Linkage-Specific Antibodies , 2008, Cell.
[5] H. Handa,et al. Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogs , 2014, Nature Structural &Molecular Biology.
[6] A. Matouschek,et al. Regulated protein turnover: snapshots of the proteasome in action , 2014, Nature Reviews Molecular Cell Biology.
[7] J. Rizo,et al. Jasmonate perception by inositol phosphate-potentiated COI1-JAZ co-receptor , 2010, Nature.
[8] M. Oren,et al. Mdm2 promotes the rapid degradation of p53 , 1997, Nature.
[9] J. Silke,et al. IAP family of cell death and signaling regulators. , 2014, Methods in enzymology.
[10] R. Young,et al. BET Bromodomain Inhibition as a Therapeutic Strategy to Target c-Myc , 2011, Cell.
[11] Mike Tyers,et al. An Allosteric Inhibitor of the Human Cdc34 Ubiquitin-Conjugating Enzyme , 2011, Cell.
[12] Min Huang,et al. Inactivation of murine Usp1 results in genomic instability and a Fanconi anemia phenotype. , 2009, Developmental cell.
[13] M. Hung,et al. Pharmacological Inactivation of Skp2 SCF Ubiquitin Ligase Restricts Cancer Stem Cell Traits and Cancer Progression , 2013, Cell.
[14] T. Willson,et al. Structural basis for an unexpected mode of SERM-mediated ER antagonism. , 2005, Molecular cell.
[15] M. Rapé,et al. Mechanism of Ubiquitin-Chain Formation by the Human Anaphase-Promoting Complex , 2008, Cell.
[16] Min Jae Lee,et al. Enhancement of Proteasome Activity by a Small-Molecule Inhibitor of Usp14 , 2010, Nature.
[17] J C Reed,et al. IAP family proteins--suppressors of apoptosis. , 1999, Genes & development.
[18] Michele Pagano,et al. SKP2 is required for ubiquitin-mediated degradation of the CDK inhibitor p27 , 1999, Nature Cell Biology.
[19] M. Rapé,et al. Building ubiquitin chains: E2 enzymes at work , 2009, Nature Reviews Molecular Cell Biology.
[20] Ivan Dikic,et al. Ubiquitination in disease pathogenesis and treatment , 2014, Nature Medicine.
[21] S. Hymowitz,et al. Antagonists Induce a Conformational Change in cIAP1 That Promotes Autoubiquitination , 2011, Science.
[22] Jerome Wielens,et al. Oncogenic protein interfaces: small molecules, big challenges , 2014, Nature Reviews Cancer.
[23] D. Esseltine,et al. Multicenter, phase I, dose-escalation trial of lenalidomide plus bortezomib for relapsed and relapsed/refractory multiple myeloma. , 2009, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[24] Christopher E. Berndsen,et al. New insights into ubiquitin E3 ligase mechanism , 2014, Nature Structural &Molecular Biology.
[25] R. Deshaies,et al. RING domain E3 ubiquitin ligases. , 2009, Annual review of biochemistry.
[26] M. Protopopova,et al. Small molecule RITA binds to p53, blocks p53–HDM-2 interaction and activates p53 function in tumors , 2004, Nature Medicine.
[27] D. Esseltine,et al. A phase 2 trial of lenalidomide, bortezomib, and dexamethasone in patients with relapsed and relapsed/refractory myeloma. , 2014, Blood.
[28] A. Levine. p53, the Cellular Gatekeeper for Growth and Division , 1997, Cell.
[29] David A. Agard,et al. The Structural Basis of Estrogen Receptor/Coactivator Recognition and the Antagonism of This Interaction by Tamoxifen , 1998, Cell.
[30] David L. Vaux,et al. IAPs, RINGs and ubiquitylation , 2005, Nature Reviews Molecular Cell Biology.
[31] Xiaodong Wang,et al. Smac, a Mitochondrial Protein that Promotes Cytochrome c–Dependent Caspase Activation by Eliminating IAP Inhibition , 2000, Cell.
[32] H. Walden,et al. RBR E3 ubiquitin ligases: new structures, new insights, new questions , 2014, The Biochemical journal.
[33] I. E. Smith,et al. HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins. , 2015, ACS chemical biology.
[34] David A. Agard,et al. Structural characterization of a subtype-selective ligand reveals a novel mode of estrogen receptor antagonism , 2002, Nature Structural Biology.
[35] M. Pagano,et al. Specific small molecule inhibitors of Skp2-mediated p27 degradation. , 2012, Chemistry & biology.
[36] Simone Fulda,et al. Targeting IAP proteins for therapeutic intervention in cancer , 2012, Nature Reviews Drug Discovery.
[37] Wilhelm Krek,et al. p45SKP2 promotes p27Kip1 degradation and induces S phase in quiescent cells , 1999, Nature Cell Biology.
[38] M. Gerritsen,et al. Novel Inhibitors of Cytokine-induced IκBα Phosphorylation and Endothelial Cell Adhesion Molecule Expression Show Anti-inflammatory Effects in Vivo* , 1997, The Journal of Biological Chemistry.
[39] K. Anderson,et al. Molecular mechanisms mediating antimyeloma activity of proteasome inhibitor PS-341. , 2003, Blood.
[40] Daniel Kaganovich,et al. Protein quality control: chaperones culling corrupt conformations , 2005, Nature Cell Biology.
[41] C. Anfinsen. Principles that govern the folding of protein chains. , 1973, Science.
[42] P. Richardson,et al. In Vitro and In Vivo Selective Antitumor Activity of a Novel Orally Bioavailable Proteasome Inhibitor MLN9708 against Multiple Myeloma Cells , 2011, Clinical Cancer Research.
[43] C. Crews,et al. Epoxomicin, a potent and selective proteasome inhibitor, exhibits in vivo antiinflammatory activity. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[44] V. Jordan,et al. The estrogen receptor: a model for molecular medicine. , 2003, Clinical cancer research : an official journal of the American Association for Cancer Research.
[45] J. Fletcher,et al. USP6 (Tre2) Fusion Oncogenes in Aneurysmal Bone Cyst , 2004, Cancer Research.
[46] Yevgeniy V. Serebrenik,et al. Targeted Protein Destabilization Reveals an Estrogen-mediated ER Stress Response , 2014, Nature chemical biology.
[47] Christopher J. Ott,et al. The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins , 2014, Science.
[48] I. Sanz,et al. Inhibition of proliferation and survival of diffuse large B-cell lymphoma cells by a small-molecule inhibitor of the ubiquitin-conjugating enzyme Ubc13-Uev1A. , 2012, Blood.
[49] A. Ciulli,et al. Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4 , 2015, ACS chemical biology.
[50] R. Brasseur,et al. The hydrophobic effect in protein folding , 1995, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
[51] R. Huber,et al. Crystal Structure of Epoxomicin:20S Proteasome reveals a molecular basis for selectivity of alpha,beta-Epoxyketone Proteasome Inhibitors , 2000 .
[52] Akio Matsuda,et al. Genome-Wide and Functional Annotation of Human E3 Ubiquitin Ligases Identifies MULAN, a Mitochondrial E3 that Regulates the Organelle's Dynamics and Signaling , 2008, PloS one.
[53] P. Elliott,et al. The proteasome inhibitor PS-341 inhibits growth, induces apoptosis, and overcomes drug resistance in human multiple myeloma cells. , 2001, Cancer research.
[54] Parantu K. Shah,et al. A small molecule inhibitor of ubiquitin-specific protease-7 induces apoptosis in multiple myeloma cells and overcomes bortezomib resistance. , 2012, Cancer cell.
[55] David P. Davis,et al. Ubiquitin Ligase RNF146 Regulates Tankyrase and Axin to Promote Wnt Signaling , 2011, PloS one.
[56] Andiliy G. Lai,et al. Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts. , 2015, Journal of medicinal chemistry.
[57] René Bernards,et al. A Genomic and Functional Inventory of Deubiquitinating Enzymes , 2005, Cell.
[58] J. Pruneda,et al. Allosteric Activation of the RNF146 Ubiquitin Ligase by a Poly(ADP-ribosyl)ation Signal , 2014, Nature.
[59] A. Levine,et al. Structure of the MDM2 Oncoprotein Bound to the p53 Tumor Suppressor Transactivation Domain , 1996, Science.
[60] S. Elledge,et al. Structure of the Cul1–Rbx1–Skp1–F boxSkp2 SCF ubiquitin ligase complex , 2002, Nature.
[61] H. Li,et al. USP37 directly deubiquitinates and stabilizes c-Myc in lung cancer , 2014, Oncogene.
[62] J. Moffat,et al. The ubiquitin-activating enzyme E1 as a therapeutic target for the treatment of leukemia and multiple myeloma. , 2010, Blood.
[63] S. Grant,et al. Synergistic Induction of Oxidative Injury and Apoptosis in Human Multiple Myeloma Cells by the Proteasome Inhibitor Bortezomib and Histone Deacetylase Inhibitors , 2004, Clinical Cancer Research.
[64] Yili Yang,et al. Inhibitors of ubiquitin-activating enzyme (E1), a new class of potential cancer therapeutics. , 2007, Cancer research.
[65] J. Gervais,et al. Human CUL-1 associates with the SKP1/SKP2 complex and regulates p21(CIP1/WAF1) and cyclin D proteins. , 1998, Proceedings of the National Academy of Sciences of the United States of America.
[66] Amanda Doucette,et al. An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer , 2009, Nature.
[67] S. Minoshima,et al. Mutations in the parkin gene cause autosomal recessive juvenile parkinsonism , 1998, Nature.
[68] C. Pace,et al. Forces contributing to the conformational stability of proteins , 1996, FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
[69] J. Wade Harper,et al. Ubiquitin-like protein activation by E1 enzymes: the apex for downstream signalling pathways , 2009, Nature Reviews Molecular Cell Biology.
[70] Christoph H. Emmerich,et al. The anti-inflammatory drug BAY 11-7082 suppresses the MyD88-dependent signalling network by targeting the ubiquitin system , 2013, The Biochemical journal.
[71] P. Hasselgren,et al. Molecular regulation of muscle cachexia: it may be more than the proteasome. , 2002, Biochemical and biophysical research communications.
[72] M. Estelle,et al. The TIR1 protein of Arabidopsis functions in auxin response and is related to human SKP2 and yeast grr1p. , 1998, Genes & development.
[73] I. Wertz,et al. Toward understanding ubiquitin-modifying enzymes: from pharmacological targeting to proteomics. , 2014, Trends in pharmacological sciences.
[74] Edward L. Huttlin,et al. Systematic and quantitative assessment of the ubiquitin-modified proteome. , 2011, Molecular cell.
[75] M. Ladanyi,et al. MDM2 gene amplification in metastatic osteosarcoma. , 1993, Cancer research.
[76] Zhiwei Wang,et al. Roles of F-box proteins in cancer , 2014, Nature Reviews Cancer.
[77] T. Corson,et al. Small-Molecule Hydrophobic Tagging Induced Degradation of HaloTag Fusion Proteins , 2011, Nature Chemical Biology.
[78] Mårten Fryknäs,et al. Inhibition of proteasome deubiquitinating activity as a new cancer therapy , 2011, Nature Medicine.
[79] A. Bauer,et al. RNF146 is a poly(ADP-ribose)-directed E3 ligase that regulates axin degradation and Wnt signalling , 2011, Nature Cell Biology.
[80] Jeremy L. Jenkins,et al. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide , 2014, Nature.
[81] J. Gribben,et al. Bortezomib blocks Bax degradation in malignant B cells during treatment with TRAIL. , 2008, Blood.
[82] T. Nagykálnai,et al. [Cachexia in cancer patients]. , 2016, Magyar onkologia.
[83] Jan Bergman,et al. PRIMA-1 reactivates mutant p53 by covalent binding to the core domain. , 2009, Cancer cell.
[84] F. Bazan,et al. Deubiquitinase USP9X stabilizes MCL1 and promotes tumour cell survival , 2010, Nature.
[85] Chun Cheng,et al. The Expression and Prognosis of FOXO3a and Skp2 in Human Hepatocellular Carcinoma , 2009, Pathology & Oncology Research.
[86] Javed Siddiqui,et al. Activating ESR1 mutations in hormone-resistant metastatic breast cancer , 2013, Nature Genetics.
[87] William B. Smith,et al. Selective inhibition of BET bromodomains , 2010, Nature.
[88] A. Levine,et al. The mdm-2 oncogene product forms a complex with the p53 protein and inhibits p53-mediated transactivation , 1992, Cell.
[89] B. Quesnel,et al. Over‐expression of the MDM2 gene is found in some cases of haematological malignancies , 1994, British journal of haematology.
[90] Steven P. Gygi,et al. Dynamics of Cullin-RING Ubiquitin Ligase Network Revealed by Systematic Quantitative Proteomics , 2010, Cell.
[91] I. E. Smith,et al. Catalytic in vivo protein knockdown by small-molecule PROTACs. , 2015, Nature chemical biology.
[92] S. Gygi,et al. Dual E1 activation systems for ubiquitin differentially regulate E2 enzyme charging , 2007, Nature.
[93] B. O’Malley,et al. Proteasome-dependent degradation of the human estrogen receptor. , 1999, Proceedings of the National Academy of Sciences of the United States of America.
[94] P. Jänne,et al. Pharmacological Targeting of the Pseudokinase Her3 , 2014, Nature chemical biology.
[95] L. Lam,et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets , 2013, Nature Medicine.
[96] M. Rapé,et al. K11-linked ubiquitin chains as novel regulators of cell division. , 2011, Trends in cell biology.
[97] Jia-qing Li,et al. Correlation of Skp2 with carcinogenesis, invasion, metastasis, and prognosis in colorectal tumors. , 2004, International journal of oncology.
[98] A. Wakeling,et al. A potent specific pure antiestrogen with clinical potential. , 1991, Cancer research.
[99] S. Demo,et al. Antitumor activity of PR-171, a novel irreversible inhibitor of the proteasome. , 2007, Cancer research.
[100] K. Iwai,et al. Generation and physiological roles of linear ubiquitin chains , 2012, BMC Biology.
[101] L. Hedstrom,et al. Inhibitor mediated protein degradation. , 2012, Chemistry & biology.
[102] Ping Li,et al. Substrate-assisted inhibition of ubiquitin-like protein-activating enzymes: the NEDD8 E1 inhibitor MLN4924 forms a NEDD8-AMP mimetic in situ. , 2010, Molecular cell.
[103] D. Germain,et al. Differential expression of the F-box proteins Skp2 and Skp2B in breast cancer , 2005, Oncogene.
[104] Zhijian J. Chen,et al. Activation of the IκB Kinase Complex by TRAF6 Requires a Dimeric Ubiquitin-Conjugating Enzyme Complex and a Unique Polyubiquitin Chain , 2000, Cell.
[105] V. Battaglia,et al. Discovery of specific inhibitors of human USP7/HAUSP deubiquitinating enzyme. , 2012, Chemistry & biology.
[106] K. Anderson,et al. Proteasome inhibitor therapy in multiple myeloma , 2005, Molecular Cancer Therapeutics.
[107] K. Shokat,et al. Targeting the cancer kinome through polypharmacology , 2010, Nature Reviews Cancer.
[108] David Chen,et al. ESR1 ligand binding domain mutations in hormone-resistant breast cancer , 2013, Nature Genetics.
[109] K. Vousden,et al. Ubiquitination and Degradation of Mutant p53 , 2007, Molecular and Cellular Biology.
[110] Vishva M Dixit,et al. IAP antagonists induce autoubiquitination of c-IAPs, NF-kappaB activation, and TNFalpha-dependent apoptosis. , 2007, Cell.
[111] C. Lima,et al. Structural and functional insights to ubiquitin-like protein conjugation. , 2014, Annual review of biophysics.
[112] K. Ohshima,et al. Prognostic significance of S-phase kinase-associated protein 2 and p27kip1 in patients with diffuse large B-cell lymphoma: effects of rituximab. , 2010, Annals of oncology : official journal of the European Society for Medical Oncology.
[113] M. Dimopoulos,et al. Current treatment landscape for relapsed and/or refractory multiple myeloma , 2015, Nature Reviews Clinical Oncology.
[114] Michael J. Emanuele,et al. Global Identification of Modular Cullin-RING Ligase Substrates , 2011, Cell.
[115] J. Hazle,et al. The Skp2-SCF E3 Ligase Regulates Akt Ubiquitination, Glycolysis, Herceptin Sensitivity, and Tumorigenesis , 2012, Cell.
[116] B. Ruggeri,et al. Novel, orally active, proteasome inhibitor, delanzomib (CEP-18770), ameliorates disease symptoms and glomerulonephritis in two preclinical mouse models of SLE. , 2012, International immunopharmacology.
[117] Daniel C. Scott,et al. Structural Insights into NEDD8 Activation of Cullin-RING Ligases: Conformational Control of Conjugation , 2008, Cell.
[118] S. Carr,et al. Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells , 2014, Science.
[119] C. Crews,et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. , 2015, Chemistry & biology.
[120] J. Mestan,et al. Skp2 is oncogenic and overexpressed in human cancers , 2001, Proceedings of the National Academy of Sciences of the United States of America.
[121] James E. Bradner,et al. Phthalimide conjugation as a strategy for in vivo target protein degradation , 2015, Science.
[122] Ottoline Leyser,et al. Auxin regulates SCFTIR1-dependent degradation of AUX/IAA proteins , 2001, Nature.
[123] Bo Yang,et al. Lenalidomide Treatment for Multiple Myeloma: Systematic Review and Meta-Analysis of Randomized Controlled Trials , 2013, PloS one.
[124] N. Gray,et al. Targeting cancer with small molecule kinase inhibitors , 2009, Nature Reviews Cancer.
[125] Robert L Moritz,et al. Identification of DIABLO, a Mammalian Protein that Promotes Apoptosis by Binding to and Antagonizing IAP Proteins , 2000, Cell.
[126] D. Carney,et al. Amplification of the MDM2 gene in human breast cancer and its association with MDM2 and p53 protein status. , 1995, British Journal of Cancer.
[127] Dajun Yang,et al. Temporal activation of p53 by a specific MDM2 inhibitor is selectively toxic to tumors and leads to complete tumor growth inhibition , 2008, Proceedings of the National Academy of Sciences.
[128] M. Rapé,et al. The Ubiquitin Code , 2012, Annual review of biochemistry.
[129] L. Vassilev,et al. In Vivo Activation of the p53 Pathway by Small-Molecule Antagonists of MDM2 , 2004, Science.
[130] V. Dixit,et al. Deubiquitinase USP37 is activated by CDK2 to antagonize APC(CDH1) and promote S phase entry. , 2011, Molecular cell.
[131] David Komander,et al. Breaking the chains: structure and function of the deubiquitinases , 2009, Nature Reviews Molecular Cell Biology.
[132] J. Adams. The development of proteasome inhibitors as anticancer drugs. , 2004, Cancer cell.