Discovery of a new class of integrin antibodies for fibrosis

[1]  Saburo Ito,et al.  Cryo-EM Reveals Integrin-Mediated TGF-β Activation without Release from Latent TGF-β , 2020, Cell.

[2]  Benjamin B. Sun,et al.  New genetic signals for lung function highlight pathways and chronic obstructive pulmonary disease associations across multiple ancestries. , 2018, Nature Genetics.

[3]  W. Fahy,et al.  Safety, tolerability and pharmacokinetics of GSK3008348, a novel integrin αvβ6 inhibitor, in healthy participants , 2018, European Journal of Clinical Pharmacology.

[4]  D. Veesler,et al.  The Therapeutic Antibody LM609 Selectively Inhibits Ligand Binding to Human αVβ3 Integrin via Steric Hindrance. , 2017, Structure.

[5]  Shirly Pinto,et al.  An integrin antagonist (MK‐0429) decreases proteinuria and renal fibrosis in the ZSF1 rat diabetic nephropathy model , 2017, Pharmacology research & perspectives.

[6]  A. Sivasubramanian,et al.  Broad epitope coverage of a human in vitro antibody library , 2016, mAbs.

[7]  R. Slack,et al.  Characterisation of a novel, high affinity and selective αvβ6 integrin RGD-mimetic radioligand. , 2016, Biochemical pharmacology.

[8]  M. Breyer,et al.  The next generation of therapeutics for chronic kidney disease , 2016, Nature Reviews Drug Discovery.

[9]  K. Sekiguchi,et al.  Molecular Basis of the Ligand Binding Specificity of αvβ8 Integrin* , 2016, The Journal of Biological Chemistry.

[10]  G. Raghu,et al.  The 2015 guidelines for idiopathic pulmonary fibrosis: an important chapter in the evolution of the management of patients with IPF , 2015, European Respiratory Journal.

[11]  W. DeGrado,et al.  The αvβ1 integrin plays a critical in vivo role in tissue fibrosis , 2015, Science Translational Medicine.

[12]  Don C Rockey,et al.  Fibrosis--a common pathway to organ injury and failure. , 2015, The New England journal of medicine.

[13]  Alexander Pautsch,et al.  Mode of action of nintedanib in the treatment of idiopathic pulmonary fibrosis , 2015, European Respiratory Journal.

[14]  G. Raghu,et al.  Nintedanib and pirfenidone. New antifibrotic treatments indicated for idiopathic pulmonary fibrosis offer hopes and raises questions. , 2015, American journal of respiratory and critical care medicine.

[15]  C. Bokemeyer,et al.  Abituzumab combined with cetuximab plus irinotecan versus cetuximab plus irinotecan alone for patients with KRAS wild-type metastatic colorectal cancer: the randomised phase I/II POSEIDON trial. , 2015 .

[16]  T. Springer,et al.  Structural determinants of integrin β-subunit specificity for latent TGF-β , 2014, Nature Structural &Molecular Biology.

[17]  O. Brand,et al.  Selective Targeting of TGF-β Activation to Treat Fibroinflammatory Airway Disease , 2014, Science Translational Medicine.

[18]  J. Duffield Cellular and molecular mechanisms in kidney fibrosis. , 2014, The Journal of clinical investigation.

[19]  M. Mofrad,et al.  Atomic basis for the species-specific inhibition of alpha V integrins by monoclonal antibody 17E6 is revealed by the crystal structure of alpha V beta 3 ectodomain-17E6 Fab complex. , 2014 .

[20]  M. Mofrad,et al.  Atomic Basis for the Species-specific Inhibition of αV Integrins by Monoclonal Antibody 17E6 Is Revealed by the Crystal Structure of αVβ3 Ectodomain-17E6 Fab Complex* , 2014, The Journal of Biological Chemistry.

[21]  T. Kijima,et al.  Efficacy and safety of pirfenidone for idiopathic pulmonary fibrosis , 2014, Patient preference and adherence.

[22]  D. Griggs,et al.  Selective αv integrin depletion identifies a core, targetable molecular pathway that regulates fibrosis across solid organs , 2013, Nature Network Boston.

[23]  T. Oury,et al.  Animal models of fibrotic lung disease. , 2013, American journal of respiratory cell and molecular biology.

[24]  D. Sheppard,et al.  Integrin-mediated regulation of TGFβ in fibrosis. , 2013, Biochimica et biophysica acta.

[25]  D. Griggs,et al.  OC-001 The Impact of the Introduction of Formalised Polypectomy Assessment on Training in the United Kingdom , 2013, Gut.

[26]  A. Hata,et al.  Targeting the TGFβ signalling pathway in disease , 2012, Nature Reviews Drug Discovery.

[27]  Y. Sugita,et al.  Crystal structure of α5β1 integrin ectodomain: Atomic details of the fibronectin receptor , 2012, The Journal of cell biology.

[28]  P. Wolters,et al.  Mouse and human lung fibroblasts regulate dendritic cell trafficking, airway inflammation, and fibrosis through integrin αvβ8-mediated activation of TGF-β. , 2011, The Journal of clinical investigation.

[29]  M. Campone,et al.  Evaluation of the safety, pharmacokinetics and treatment effects of an ανβ3 integrin inhibitor on bone turnover and disease activity in men with hormone‐refractory prostate cancer and bone metastases , 2010, Asia-Pacific journal of clinical oncology.

[30]  M. Humphries,et al.  Anti-integrin monoclonal antibodies , 2009, Journal of Cell Science.

[31]  Fan Wang,et al.  Integrin αvβ3-Targeted Radioimmunotherapy of Glioblastoma Multiforme , 2008, Clinical Cancer Research.

[32]  H. Bolte,et al.  Standardized quantification of pulmonary fibrosis in histological samples. , 2008, BioTechniques.

[33]  D. Brooks,et al.  Inhibition of Gene Markers of Fibrosis with a Novel Inhibitor of Transforming Growth Factor-β Type I Receptor Kinase in Puromycin-Induced Nephritis , 2005, Journal of Pharmacology and Experimental Therapeutics.

[34]  R. Recker,et al.  Effect of L-000845704, an αVβ3 integrin antagonist, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women , 2005 .

[35]  M. Humphries,et al.  Dual Functionality of the Anti-β1 Integrin Antibody, 12G10, Exemplifies Agonistic Signalling from the Ligand Binding Pocket of Integrin Adhesion Receptors* , 2005, Journal of Biological Chemistry.

[36]  P. Coleman,et al.  Nonpeptide αvβ3 Antagonists. Part 11: Discovery and Preclinical Evaluation of Potent αvβ3 Antagonists for the Prevention and Treatment of Osteoporosis , 2004 .

[37]  Mark P. Lewis,et al.  αv integrins play an important role in myofibroblast differentiation , 2004, Wound repair and regeneration : official publication of the Wound Healing Society [and] the European Tissue Repair Society.

[38]  K. Simon,et al.  Function-blocking Integrin αvβ6 Monoclonal Antibodies , 2004, Journal of Biological Chemistry.

[39]  P. Coleman,et al.  Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. , 2003, Journal of medicinal chemistry.

[40]  Richard O Hynes,et al.  Integrins Bidirectional, Allosteric Signaling Machines , 2002, Cell.

[41]  D. Sheppard,et al.  The integrin αvβ8 mediates epithelial homeostasis through MT1-MMP–dependent activation of TGF-β1 , 2002, The Journal of cell biology.

[42]  Thilo Stehle,et al.  Crystal Structure of the Extracellular Segment of Integrin αVβ3 , 2001, Science.

[43]  E. Topol,et al.  Comparison of two platelet glycoprotein IIb/IIIa inhibitors, tirofiban and abciximab, for the prevention of ischemic events with percutaneous coronary revascularization. , 2001, The New England journal of medicine.

[44]  T. N. Campbell,et al.  Targeted antiangiogenic therapy for cancer using Vitaxin: a humanized monoclonal antibody to the integrin alphavbeta3. , 2000, Clinical cancer research : an official journal of the American Association for Cancer Research.

[45]  H. Lodish,et al.  Specificity in transforming growth factor beta-induced transcription of the plasminogen activator inhibitor-1 gene: interactions of promoter DNA, transcription factor muE3, and Smad proteins. , 1999, Proceedings of the National Academy of Sciences of the United States of America.

[46]  N. Kaminski,et al.  The integrin alpha v beta 6 binds and activates latent TGF beta 1: a mechanism for regulating pulmonary inflammation and fibrosis. , 1999, Cell.

[47]  N. Kaminski,et al.  A Mechanism for Regulating Pulmonary Inflammation and Fibrosis: The Integrin αvβ6 Binds and Activates Latent TGF β1 , 1999, Cell.

[48]  M. Hensler,et al.  Stepwise in vitro affinity maturation of Vitaxin, an αvβ3-specific humanized mAb , 1998 .

[49]  Xiao-Fan Wang,et al.  Tumor suppressor Smad4 is a transforming growth factor beta-inducible DNA binding protein , 1997, Molecular and cellular biology.

[50]  M. Humphries,et al.  Identification of a novel anti‐integrin monoclonal antibody that recognises a ligand‐induced binding site epitope on the β1 subunit , 1995, FEBS letters.

[51]  R. Juliano,et al.  The alpha 5 beta 1 integrin fibronectin receptor, but not the alpha 5 cytoplasmic domain, functions in an early and essential step in fibronectin matrix assembly. , 1993, The Journal of biological chemistry.

[52]  D. Vestweber,et al.  A monoclonal antibody against an activation epitope on mouse integrin chain beta 1 blocks adhesion of lymphocytes to the endothelial integrin alpha 6 beta 1. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[53]  E. Ruoslahti,et al.  The alpha v beta 1 integrin functions as a fibronectin receptor but does not support fibronectin matrix assembly and cell migration on fibronectin , 1993, The Journal of cell biology.

[54]  E. Ruoslahti,et al.  A novel integrin specificity exemplified by binding of the alpha v beta 5 integrin to the basic domain of the HIV Tat protein and vitronectin , 1993, The Journal of cell biology.

[55]  R J Lynch,et al.  Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors. , 1992, Journal of medicinal chemistry.

[56]  J M Simpson,et al.  Simple method of estimating severity of pulmonary fibrosis on a numerical scale. , 1988, Journal of clinical pathology.

[57]  V. Harris,et al.  Protein detection by Simple Western™ analysis. , 2015, Methods in molecular biology.

[58]  Nicola J. Rinaldi,et al.  Partial inhibition of integrin alpha(v)beta6 prevents pulmonary fibrosis without exacerbating inflammation. , 2008, American journal of respiratory and critical care medicine.

[59]  Nicola J. Rinaldi,et al.  Partial Inhibition of Integrin αvβ6 Prevents Pulmonary Fibrosis without Exacerbating Inflammation , 2008 .

[60]  K. Simon,et al.  Alphav beta6 integrin regulates renal fibrosis and inflammation in Alport mouse. , 2007, The American journal of pathology.

[61]  K. Simon,et al.  Epithelial and Mesenchymal Cell Biology v 6 Integrin Regulates Renal Fibrosis and Inflammation in Alport Mouse , 2006 .

[62]  R. Recker,et al.  Effect of L-000845704, an alphaVbeta3 integrin antagonist, on markers of bone turnover and bone mineral density in postmenopausal osteoporotic women. , 2005, The Journal of clinical endocrinology and metabolism.

[63]  K. Simon,et al.  Function-blocking integrin alphavbeta6 monoclonal antibodies: distinct ligand-mimetic and nonligand-mimetic classes. , 2004, The Journal of biological chemistry.

[64]  P. Coleman,et al.  Nonpeptide alphavbeta3 antagonists. Part 11: discovery and preclinical evaluation of potent alphavbeta3 antagonists for the prevention and treatment of osteoporosis. , 2004, Journal of medicinal chemistry.

[65]  D. Rifkin,et al.  Measurement of active TGF-beta generated by cultured cells. , 2000, Methods in molecular biology.

[66]  D. Rifkin,et al.  Measurements of Active TGFβ Generated by Culture Cells , 2000 .

[67]  M. Hensler,et al.  Stepwise in vitro affinity maturation of Vitaxin, an alphav beta3-specific humanized mAb. , 1998, Proceedings of the National Academy of Sciences of the United States of America.

[68]  F. Himmelsbach,et al.  Nonpeptidic fibrinogen receptor antagonists , 1994 .