A covalent PIN1 inhibitor selectively targets cancer cells by a dual mechanism of action
暂无分享,去创建一个
A. Rosato | P. Carloni | E. Baloglu | G. Del Sal | M. D’Incalci | S. Piazza | A. Rustighi | G. Rossetti | P. Storici | F. Benvenuti | M. Lolli | B. Valsasina | O. Kalid | S. Shacham | Alessandro Zannini | E. Cappuzzello | Y. Ciani | B. Giabbai | E. Bello | A. Pippione | Elena Campaner | U. Cucchi | G. Golan | Alberto Cristiani | Yari Ciani | Silvano Piazza | A. C. Pippione
[1] G. Sal,et al. PIN1 in breast development and cancer: a clinical perspective , 2016, Cell Death and Differentiation.
[2] S. Bicciato,et al. Glucocorticoid receptor signalling activates YAP in breast cancer , 2017, Nature Communications.
[3] A. Rosato,et al. Proteasome machinery is instrumental in a common gain-of-function program of the p53 missense mutants in cancer , 2016, Nature Cell Biology.
[4] Xiao Zhen Zhou,et al. The isomerase PIN1 controls numerous cancer-driving pathways and is a unique drug target , 2016, Nature Reviews Cancer.
[5] M. V. Giuli,et al. Prolyl-isomerase Pin1 controls Notch3 protein expression and regulates T-ALL progression , 2016, Oncogene.
[6] R. Bristow,et al. Radiotherapy-induced miR-223 prevents relapse of breast cancer by targeting the EGF pathway , 2016, Oncogene.
[7] Rachel M. Webster. Combination therapies in oncology , 2016, Nature Reviews Drug Discovery.
[8] Jennifer L. Knight,et al. OPLS3: A Force Field Providing Broad Coverage of Drug-like Small Molecules and Proteins. , 2016, Journal of chemical theory and computation.
[9] R. Amaravadi,et al. Emerging strategies to effectively target autophagy in cancer , 2016, Oncogene.
[10] A. Gautam,et al. STATE , 2016, Intell. Serv. Robotics.
[11] S. Hanes. Prolyl isomerases in gene transcription. , 2015, Biochimica et biophysica acta.
[12] C. Brandl,et al. Peroxide-mediated oxidation and inhibition of the peptidyl-prolyl isomerase Pin1. , 2015, Biochimica et biophysica acta.
[13] Christopher L. Warren,et al. Peptidylprolyl Isomerase Pin1 Directly Enhances the DNA Binding Functions of Estrogen Receptor α* , 2015, The Journal of Biological Chemistry.
[14] P. Pandolfi,et al. Active Pin1 is a key target of all-trans retinoic acid in acute promyelocytic leukemia and breast cancer , 2015, Nature Medicine.
[15] D. Butterfield,et al. Pin1 cysteine-113 oxidation inhibits its catalytic activity and cellular function in Alzheimer's disease , 2015, Neurobiology of Disease.
[16] J. Lieberman,et al. The Rab2A GTPase Promotes Breast Cancer Stem Cells and Tumorigenesis via Erk Signaling Activation , 2015, Cell reports.
[17] Jing-Zhang Wang,et al. Pin1-based diagnostic and therapeutic strategies for breast cancer. , 2015, Pharmacological research.
[18] Yingyan Yu,et al. Pin1 is Overexpressed and Correlates with Poor Prognosis in Gastric Cancer , 2014, Cell Biochemistry and Biophysics.
[19] T. Hunter,et al. Prolyl isomerase Pin1 in cancer , 2014, Cell Research.
[20] G. Poon,et al. Prodrug Applications for Targeted Cancer Therapy , 2014, The AAPS Journal.
[21] J. Lieberman,et al. Prolyl isomerase Pin1 acts downstream of miR200c to promote cancer stem-like cell traits in breast cancer. , 2014, Cancer research.
[22] Kai Zhu,et al. Structure-Based Virtual Screening Approach for Discovery of Covalently Bound Ligands , 2014, J. Chem. Inf. Model..
[23] D. Rimm,et al. Pin1 modulates ERα levels in breast cancer through inhibition of phosphorylation-dependent ubiquitination and degradation , 2014, Oncogene.
[24] A. Krešo,et al. Evolution of the cancer stem cell model. , 2014, Cell stem cell.
[25] Matthias Dobbelstein,et al. Targeting tumour-supportive cellular machineries in anticancer drug development , 2014, Nature Reviews Drug Discovery.
[26] S. Dimmeler,et al. EMBO Molecular Medicine: Fast Forward , 2014, EMBO molecular medicine.
[27] S. Bicciato,et al. Prolyl-isomerase Pin1 controls normal and cancer stem cells of the breast , 2013, EMBO molecular medicine.
[28] T. Mak,et al. Modulation of oxidative stress as an anticancer strategy , 2013, Nature Reviews Drug Discovery.
[29] Zhihua Liu,et al. Regulation of the MicroRNA 200b (miRNA-200b) by Transcriptional Regulators PEA3 and ELK-1 Protein Affects Expression of Pin1 Protein to Control Anoikis* , 2013, The Journal of Biological Chemistry.
[30] Corbin E. Meacham,et al. Tumour heterogeneity and cancer cell plasticity , 2013, Nature.
[31] David A. Scott,et al. Double Nicking by RNA-Guided CRISPR Cas9 for Enhanced Genome Editing Specificity , 2013, Cell.
[32] Andrew Potter,et al. Pin1 inhibitors: Pitfalls, progress and cellular pharmacology. , 2013, Bioorganic & medicinal chemistry letters.
[33] H. Shih,et al. SENP1 deSUMOylates and regulates Pin1 protein activity and cellular function. , 2013, Cancer research.
[34] B. Posner,et al. Identification of DNMT1 Selective Antagonists Using a Novel Scintillation Proximity Assay* , 2013, The Journal of Biological Chemistry.
[35] M. Kuro-o,et al. Pin1 Null Mice Exhibit Low Bone Mass and Attenuation of BMP Signaling , 2013, PloS one.
[36] Colin J. Daniel,et al. Pin1 Regulates the Dynamics of c-Myc DNA Binding To Facilitate Target Gene Regulation and Oncogenesis , 2013, Molecular and Cellular Biology.
[37] Kerstin Pingel,et al. 50 Years of Image Analysis , 2012 .
[38] F. D. D. Fagagna,et al. Crosstalk between chromatin state and DNA damage response in cellular senescence and cancer , 2012, Nature Reviews Cancer.
[39] R. Watson,et al. Patented prostate cancer biomarkers , 2012, Nature Reviews Urology.
[40] Kevin W Eliceiri,et al. NIH Image to ImageJ: 25 years of image analysis , 2012, Nature Methods.
[41] N. R. Jena. DNA damage by reactive species: Mechanisms, mutation and repair , 2012, Journal of Biosciences.
[42] Y. Liou,et al. Prolyl isomerase Pin1 stabilizes and activates orphan nuclear receptor TR3 to promote mitogenesis , 2012, Oncogene.
[43] Akihide Ryo,et al. Prolyl Isomerase Pin1 Regulates Neuronal Differentiation via β-Catenin , 2012, Molecular and Cellular Biology.
[44] K. Lu,et al. Mixed-lineage kinase 3 phosphorylates prolyl-isomerase Pin1 to regulate its nuclear translocation and cellular function , 2012, Proceedings of the National Academy of Sciences.
[45] L. Hedstrom,et al. Inhibitor mediated protein degradation. , 2012, Chemistry & biology.
[46] W. Guida,et al. Discovery and synthesis of hydronaphthoquinones as novel proteasome inhibitors. , 2012, Journal of medicinal chemistry.
[47] Wenjun Guo,et al. Slug and Sox9 Cooperatively Determine the Mammary Stem Cell State , 2012, Cell.
[48] A. Klein-Szanto,et al. Retinoblastoma tumor-suppressor protein phosphorylation and inactivation depend on direct interaction with Pin1 , 2012, Cell Death and Differentiation.
[49] Mishal N. Patel,et al. Objective assessment of cancer genes for drug discovery , 2012, Nature Reviews Drug Discovery.
[50] C. Uchida,et al. A critical step for JNK activation: isomerization by the prolyl isomerase Pin1 , 2011, Cell Death and Differentiation.
[51] S. Bicciato,et al. The Hippo Transducer TAZ Confers Cancer Stem Cell-Related Traits on Breast Cancer Cells , 2011, Cell.
[52] S. Haslam,et al. Regulation of Estrogen Receptor (cid:1) N-Terminus Conformation and Function by Peptidyl Prolyl Isomerase Pin1 , 2022 .
[53] Clark C. Chen. Selected Topics in DNA Repair , 2011 .
[54] Y. Liou,et al. Prolyl isomerase Pin1 as a molecular switch to determine the fate of phosphoproteins. , 2011, Trends in biochemical sciences.
[55] P. Chatterjee,et al. Pin1 Deficiency Causes Endothelial Dysfunction and Hypertension , 2011, Hypertension.
[56] Weiwei Yang,et al. Ras-Induced and Extracellular Signal-Regulated Kinase 1 and 2 Phosphorylation-Dependent Isomerization of Protein Tyrosine Phosphatase (PTP)-PEST by PIN1 Promotes FAK Dephosphorylation by PTP-PEST , 2011, Molecular and Cellular Biology.
[57] Antonio Rosato,et al. A Pin1/mutant p53 axis promotes aggressiveness in breast cancer. , 2011, Cancer cell.
[58] A. Bode,et al. Epigallocatechin-gallate Suppresses Tumorigenesis by Directly Targeting Pin1 , 2011, Cancer Prevention Research.
[59] K. Lu,et al. Peptidyl-prolyl cis–trans isomerase Pin1 in ageing, cancer and Alzheimer disease , 2011, Expert Reviews in Molecular Medicine.
[60] A. Goate,et al. Death-associated protein kinase 1 phosphorylates Pin1 and inhibits its prolyl isomerase activity and cellular function. , 2011, Molecular cell.
[61] Varda Rotter,et al. Mutations in the p53 Tumor Suppressor Gene: Important Milestones at the Various Steps of Tumorigenesis. , 2011, Genes & cancer.
[62] Adrian Whitty,et al. The resurgence of covalent drugs , 2011, Nature Reviews Drug Discovery.
[63] Junying Yuan,et al. Cell death assays for drug discovery , 2011, Nature Reviews Drug Discovery.
[64] Neal Rosen,et al. Targeted cancer therapies , 2011, Chinese journal of cancer.
[65] B. Davis,et al. Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution. , 2011, Bioorganic & medicinal chemistry letters.
[66] Xiao Zhen Zhou,et al. The prolyl isomerase Pin1 acts as a novel molecular switch for TNF-alpha-induced priming of the NADPH oxidase in human neutrophils. , 2010, Blood.
[67] A. Balmain,et al. Guidelines for the welfare and use of animals in cancer research , 2010, British Journal of Cancer.
[68] P. Khanal,et al. The Prolyl Isomerase Pin1 Enhances HER-2 Expression and Cellular Transformation via Its Interaction with Mitogen-Activated Protein Kinase/Extracellular Signal-Regulated Kinase Kinase 1 , 2010, Molecular Cancer Therapeutics.
[69] N. Udupa,et al. Juglone, a naphthoquinone from walnut, exerts cytotoxic and genotoxic effects against cultured melanoma tumor cells , 2009, Cell biology international.
[70] T. Uchida,et al. Dipentamethylene thiuram monosulfide is a novel inhibitor of Pin1. , 2009, Biochemical and biophysical research communications.
[71] Peng Huang,et al. Targeting cancer cells by ROS-mediated mechanisms: a radical therapeutic approach? , 2009, Nature Reviews Drug Discovery.
[72] X. Zhou,et al. Peptidyl-prolyl cis/trans isomerase Pin1 is critical for the regulation of PKB/Akt stability and activation phosphorylation , 2009, Oncogene.
[73] A. Ryo,et al. Pinning down HER2-ER crosstalk in SMRT regulation. , 2009, Trends in biochemical sciences.
[74] Ji Luo,et al. Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction , 2009, Cell.
[75] Pier Paolo Di Fiore,et al. The prolyl-isomerase Pin1 is a Notch1 target that enhances Notch1 activation in cancer , 2009, Nature Cell Biology.
[76] K. Lu,et al. Prolyl Isomerase Pin 1 is Highly Expressed in Her 2-Positive Breast Cancer and Regulates erbB 2 Protein Stability , 2009 .
[77] S. Elledge,et al. Principles of Cancer Therapy: Oncogene and Non-oncogene Addiction , 2009, Cell.
[78] K. Lu,et al. Prolyl isomerase Pin1 is highly expressed in Her2-positive breast cancer and regulates erbB2 protein stability , 2008, Molecular Cancer.
[79] R. Reiter,et al. Melatonin combats molecular terrorism at the mitochondrial level , 2008, Interdisciplinary Toxicology.
[80] P. van der Sluijs,et al. Juglone Inactivates Cysteine-rich Proteins Required for Progression through Mitosis* , 2008, Journal of Biological Chemistry.
[81] M. Hung,et al. Down-regulation of myeloid cell leukemia-1 through inhibiting Erk/Pin 1 pathway by sorafenib facilitates chemosensitization in breast cancer. , 2008, Cancer research.
[82] Wenjun Guo,et al. The Epithelial-Mesenchymal Transition Generates Cells with Properties of Stem Cells , 2008, Cell.
[83] A. Regev,et al. An embryonic stem cell–like gene expression signature in poorly differentiated aggressive human tumors , 2008, Nature Genetics.
[84] F. Schmidt. Meta-Analysis , 2008 .
[85] Charlotte Kuperwasser,et al. Human breast cancer cell lines contain stem-like cells that self-renew, give rise to phenotypically diverse progeny and survive chemotherapy , 2008, Breast Cancer Research.
[86] J. Manley,et al. New Insights into Mitotic Chromosome Condensation: A Role for the Prolyl Isomerase Pin1 , 2007, Cell cycle.
[87] J. Manley,et al. Pin1 modulates RNA polymerase II activity during the transcription cycle. , 2007, Genes & development.
[88] Xiao Zhen Zhou,et al. The prolyl isomerase PIN1: a pivotal new twist in phosphorylation signalling and disease , 2007, Nature Reviews Molecular Cell Biology.
[89] H. Akiyama,et al. Ablation of a peptidyl prolyl isomerase Pin1 from p53-null mice accelerated thymic hyperplasia by increasing the level of the intracellular form of Notch1 , 2007, Oncogene.
[90] Elisabeth S Yeh,et al. PIN1, the cell cycle and cancer , 2007, Nature Reviews Cancer.
[91] N. Sagata,et al. Mechanism for inactivation of the mitotic inhibitory kinase Wee1 at M phase , 2007, Proceedings of the National Academy of Sciences.
[92] J. Labbé,et al. Pin1 stabilizes Emi1 during G2 phase by preventing its association with SCFβtrcp , 2007, EMBO reports.
[93] Matthew P. Repasky,et al. Extra precision glide: docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes. , 2006, Journal of medicinal chemistry.
[94] Y. Kwong,et al. PIN1 expression contributes to hepatic carcinogenesis , 2006, The Journal of pathology.
[95] L. Nicholson,et al. The prolyl isomerase Pin1 regulates amyloid precursor protein processing and amyloid-β production , 2006, Nature.
[96] A. Ryo,et al. Pin1 Regulates Centrosome Duplication, and Its Overexpression Induces Centrosome Amplification, Chromosome Instability, and Oncogenesis , 2006, Molecular and Cellular Biology.
[97] G. Collins. The next generation. , 2006, Scientific American.
[98] K. Saxena,et al. Polo-like Kinase 1-mediated Phosphorylation Stabilizes Pin1 by Inhibiting Its Ubiquitination in Human Cells* , 2005, Journal of Biological Chemistry.
[99] A. Means,et al. Peptidyl-Prolyl Isomerase 1 (Pin1) Serves as a Coactivator of Steroid Receptor by Regulating the Activity of Phosphorylated Steroid Receptor Coactivator 3 (SRC-3/AIB1) , 2005, Molecular and Cellular Biology.
[100] F. Studier,et al. Protein production by auto-induction in high density shaking cultures. , 2005, Protein expression and purification.
[101] A. Means,et al. A role for Pin1 in mammalian germ cell development and spermatogenesis. , 2004, Frontiers in bioscience : a journal and virtual library.
[102] G. Fischer,et al. Insights into the catalytic mechanism of peptidyl prolyl cis/trans isomerases. , 2004, Frontiers in bioscience : a journal and virtual library.
[103] Priti Garg,et al. Modeling breast cancer in vivo and ex vivo reveals an essential role of Pin1 in tumorigenesis , 2004, The EMBO journal.
[104] J. Sowadski,et al. Prevalent overexpression of prolyl isomerase Pin1 in human cancers. , 2004, The American journal of pathology.
[105] Hege S. Beard,et al. Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening. , 2004, Journal of medicinal chemistry.
[106] Matthew P. Repasky,et al. Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy. , 2004, Journal of medicinal chemistry.
[107] A. Means,et al. Spermatogonial Depletion in Adult Pin1-Deficient Mice1 , 2003, Biology of reproduction.
[108] A. Ryo,et al. Regulation of NF-kappaB signaling by Pin1-dependent prolyl isomerization and ubiquitin-mediated proteolysis of p65/RelA. , 2003, Molecular cell.
[109] Anna Frolov,et al. The prolyl isomerase Pin1 is a novel prognostic marker in human prostate cancer. , 2003, Cancer research.
[110] Tony Hunter,et al. Role of the prolyl isomerase Pin1 in protecting against age-dependent neurodegeneration , 2003, Nature.
[111] Y. Matsuo,et al. Pin1 and Par14 peptidyl prolyl isomerase inhibitors block cell proliferation. , 2003, Chemistry & biology.
[112] M. Ahmad,et al. Molecular mechanisms of N-acetylcysteine actions , 2003, Cellular and Molecular Life Sciences CMLS.
[113] S. Volinia,et al. The prolyl isomerase Pin1 reveals a mechanism to control p53 functions after genotoxic insults , 2002, Nature.
[114] Sam W. Lee,et al. PIN1 Is an E2F Target Gene Essential for Neu/Ras-Induced Transformation of Mammary Epithelial Cells , 2002, Molecular and Cellular Biology.
[115] J. Noel,et al. Critical Role of WW Domain Phosphorylation in Regulating Phosphoserine Binding Activity and Pin1 Function* , 2002, The Journal of Biological Chemistry.
[116] T. Hunter,et al. Loss of Pin1 function in the mouse causes phenotypes resembling cyclin D1-null phenotypes , 2002, Proceedings of the National Academy of Sciences of the United States of America.
[117] Tianhua Niu,et al. Pin1 is overexpressed in breast cancer and cooperates with Ras signaling in increasing the transcriptional activity of c‐Jun towards cyclin D1 , 2001, The EMBO journal.
[118] T. Hsu,et al. Drosophila Pin1 prolyl isomerase Dodo is a MAP kinase signal responder during oogenesis , 2001, Nature Cell Biology.
[119] M. Kirschner,et al. Pin1 acts catalytically to promote a conformational change in Cdc25. , 2001, Molecular cell.
[120] Masafumi Nakamura,et al. Pin1 regulates turnover and subcellular localization of β-catenin by inhibiting its interaction with APC , 2001, Nature Cell Biology.
[121] R. Reiter. Melatonin: Lowering the High Price of Free Radicals. , 2000, News in physiological sciences : an international journal of physiology produced jointly by the International Union of Physiological Sciences and the American Physiological Society.
[122] G Fischer,et al. Pin1-dependent prolyl isomerization regulates dephosphorylation of Cdc25C and tau proteins. , 2000, Molecular cell.
[123] C. Uchida,et al. Mice lacking Pin1 develop normally, but are defective in entering cell cycle from G(0) arrest. , 1999, Biochemical and biophysical research communications.
[124] G. Fischer,et al. Selective inactivation of parvulin-like peptidyl-prolyl cis/trans isomerases by juglone. , 1998, Biochemistry.
[125] G. Fischer,et al. Semiautomated microtiter plate assay for monitoring peptidylprolyl cis/trans isomerase activity in normal and pathological human sera. , 1998, Clinical chemistry.
[126] M. Kirschner,et al. The essential mitotic peptidyl-prolyl isomerase Pin1 binds and regulates mitosis-specific phosphoproteins. , 1998, Genes & development.
[127] M. Kirschner,et al. Sequence-specific and phosphorylation-dependent proline isomerization: a potential mitotic regulatory mechanism. , 1997, Science.
[128] R. Ranganathan,et al. Structural and Functional Analysis of the Mitotic Rotamase Pin1 Suggests Substrate Recognition Is Phosphorylation Dependent , 1997, Cell.
[129] T. Hunter,et al. A human peptidyl–prolyl isomerase essential for regulation of mitosis , 1996, Nature.
[130] J. Kofron,et al. Determination of kinetic constants for peptidyl prolyl cis-trans isomerases by an improved spectrophotometric assay. , 1991, Biochemistry.
[131] G. Fischer,et al. [Determination of enzymatic catalysis for the cis-trans-isomerization of peptide binding in proline-containing peptides]. , 1984, Biomedica biochimica acta.
[132] S. Shaughnessy,et al. Do No Harm: Health Systems’ Duty to Promote Clinician Well-Being , 2022, American Journal of Hospital Medicine.