Lung-restricted ALK5 inhibition avoids systemic toxicities associated with TGFβ pathway inhibition.
暂无分享,去创建一个
Jitendra Kanodia | K. Nikula | P. Brassil | E. Harstad | Kimberly Perkins | G. Palanisamy | J. Maher | Hart S. Dengler | Rui Zhang | A. Mcnamara | Lynda Liu | Adam Hughes | A. Lo | A. McNamara | A. Scandurra | S. Kulyk | I. Lua | J. Kanodia
[1] J. Tabernero,et al. Clinical development of therapies targeting TGFβ: current knowledge and future perspectives. , 2020, Annals of oncology : official journal of the European Society for Medical Oncology.
[2] S. Turley,et al. A Potent Pan-TGFβ Neutralizing Monoclonal Antibody Elicits Cardiovascular Toxicity in Mice and Cynomolgus Monkeys. , 2020, Toxicological sciences : an official journal of the Society of Toxicology.
[3] Gregory D Rak,et al. Intermittent dosing of the transforming growth factor beta receptor 1 inhibitor, BMS‐986260, mitigates class‐based cardiovascular toxicity in dogs but not rats , 2020, Journal of applied toxicology : JAT.
[4] K. Pradhan,et al. Phase II Study of the ALK5 Inhibitor Galunisertib in Very Low-, Low-, and Intermediate-Risk Myelodysplastic Syndromes , 2019, Clinical Cancer Research.
[5] M. Yoshikawa,et al. Small-scale panel comprising diverse gene family targets to evaluate compound promiscuity. , 2019, Chemical research in toxicology.
[6] M. Yokoyama,et al. Attenuation of pulmonary fibrosis in type I collagen-targeted reporter mice with ALK-5 inhibitors. , 2019, Pulmonary pharmacology & therapeutics.
[7] Xuedong Zhou,et al. Transforming growth factor-β in stem cells and tissue homeostasis , 2018, Bone Research.
[8] J. Zhang,et al. Galunisertib (LY2157299), a transforming growth factor-β receptor I kinase inhibitor, attenuates acute pancreatitis in rats , 2016, Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas.
[9] Yi-Ping Li,et al. TGF-β and BMP signaling in osteoblast, skeletal development, and bone formation, homeostasis and disease , 2016, Bone Research.
[10] R. Chambers,et al. The anti-fibrotic effect of inhibition of TGFβ-ALK5 signalling in experimental pulmonary fibrosis in mice is attenuated in the presence of concurrent γ-herpesvirus infection , 2015, Disease Models & Mechanisms.
[11] S. Estrem,et al. Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway , 2015, Drug design, development and therapy.
[12] M. Abdullah,et al. Inhibition of transforming growth factor-β via the activin receptor-like kinase-5 inhibitor attenuates pulmonary fibrosis. , 2015, Molecular medicine reports.
[13] M. Pirmohamed,et al. Physiological, pharmacological and toxicological considerations of drug‐induced structural cardiac injury , 2015, British journal of pharmacology.
[14] J. Baselga,et al. Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-β receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer , 2014, Investigational New Drugs.
[15] J. Baselga,et al. Cardiac Safety of TGF-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study , 2014, Cardiovascular Toxicology.
[16] J. Baselga,et al. First-in-Human Dose Study of the Novel Transforming Growth Factor-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Patients with Advanced Cancer and Glioma , 2014, Clinical Cancer Research.
[17] Pirjo Spuul,et al. ALK5 and ALK1 Play Antagonistic Roles in Transforming Growth Factor β-Induced Podosome Formation in Aortic Endothelial Cells , 2014, Molecular and Cellular Biology.
[18] K. Credille,et al. Nonclinical Safety Evaluation of a Transforming Growth Factor β Receptor I Kinase Inhibitor in Fischer 344 Rats and Beagle Dogs , 2014 .
[19] M. Anderton,et al. Induction of Heart Valve Lesions by Small-Molecule ALK5 Inhibitors , 2011, Toxicologic pathology.
[20] C. Elangbam,et al. Drug-induced Valvulopathy: An Update , 2010, Toxicologic pathology.
[21] K. Garber. Companies waver in efforts to target transforming growth factor beta in cancer. , 2009, Journal of the National Cancer Institute.
[22] A. Kulkarni,et al. Critical roles of the TGF-beta type I receptor ALK5 in perichondrial formation and function, cartilage integrity, and osteoblast differentiation during growth plate development. , 2009, Developmental biology.
[23] M. Goumans,et al. Poor vessel formation in embryos from knock-in mice expressing ALK5 with L45 loop mutation defective in Smad activation , 2009, Laboratory Investigation.
[24] R. Schwartz,et al. Signaling via the Tgf-beta type I receptor Alk5 in heart development. , 2008, Developmental biology.
[25] D. J. Alexander,et al. Association of Inhalation Toxicologists (AIT) Working Party Recommendation for Standard Delivered Dose Calculation and Expression in Non-Clinical Aerosol Inhalation Toxicology Studies with Pharmaceuticals , 2008 .
[26] M. Goumans,et al. Compensatory signalling induced in the yolk sac vasculature by deletion of TGFβ receptors in mice , 2007, Journal of Cell Science.
[27] H. Kikkawa,et al. Inhibition of activin receptor-like kinase 5 attenuates bleomycin-induced pulmonary fibrosis. , 2007, Experimental and molecular pathology.
[28] R. Mirabile,et al. Inhibition of ALK5 Signaling Induces Physeal Dysplasia in Rats , 2007, Toxicologic pathology.
[29] M. Kolb,et al. Progressive transforming growth factor beta1-induced lung fibrosis is blocked by an orally active ALK5 kinase inhibitor. , 2005, American journal of respiratory and critical care medicine.
[30] A. Roberts,et al. SB-505124 is a selective inhibitor of transforming growth factor-beta type I receptors ALK4, ALK5, and ALK7. , 2004, Molecular pharmacology.
[31] Jonas Larsson,et al. Activin receptor-like kinase (ALK)1 is an antagonistic mediator of lateral TGFbeta/ALK5 signaling. , 2003, Molecular cell.
[32] C. Lisboa,et al. Bleomycin-induced chronic lung damage does not resemble human idiopathic pulmonary fibrosis. , 2001, American journal of respiratory and critical care medicine.
[33] M. Goumans,et al. Abnormal angiogenesis but intact hematopoietic potential in TGF‐β type I receptor‐deficient mice , 2001, The EMBO journal.
[34] T. Mak,et al. Normal B lymphocyte development but impaired T cell maturation in CD45-Exon6 protein tyrosine phosphatase-deficient mice , 1993, Cell.
[35] A. Wakeham,et al. Profound block in thymocyte development in mice lacking p56lck , 1992, Nature.