Development of TGF-β signalling inhibitors for cancer therapy

New Guidelines to Evaluate the Response to Treatment in Solid Tumors

Therasse, P., Arbuck, S. G., Eisenhauer, E. A., Wanders, J., Kaplan, R. S., Rubinstein, L., Verweij, J., Van Glabbeke, M., van Oosterom, A. T., Christian, M. C., et al. (2000) · JNCI: Journal of the National Cancer Institute · doi:10.1093/jnci/92.3.205 · Cited by 15,660

Use of chemotherapy plus a monoclonal antibody against HER2 for metastatic breast cancer that overexpresses HER2

Slamon, D. J., Leyland-Jones, B., Shak, S., Fuchs, H., Paton, V., Bajamonde, A., Fleming, T., Eiermann, W., Wolter, J., Pegram, M., et al. (2001) · New England Journal of Medicine · doi:10.1056/nejm200103153441101 · Cited by 11,500

Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib

Lynch, T. J., Bell, D. W., Sordella, R., Gurubhagavatula, S., Okimoto, R. A., Brannigan, B. W., Harris, P. L., Haserlat, S. M., Supko, J. G., Haluska, F. G., et al. (2004) · New England Journal of Medicine · doi:10.1056/nejmoa040938 · Cited by 11,486

EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy

Paez, J. G., Jänne, P. A., Lee, J. C., Tracy, S., Greulich, H., Gabriel, S., Herman, P., Kaye, F. J., Lindeman, N., Boggon, T. J., et al. (2004) · Science · doi:10.1126/science.1099314 · Cited by 9,368

Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification

Gorre, M. E., Mohammed, M., Ellwood, K., Hsu, N., Paquette, R., Rao, P. N., & Sawyers, C. L. (2001) · Science · doi:10.1126/science.1062538 · Cited by 3,104

Transforming growth factor beta 1 null mutation in mice causes excessive inflammatory response and early death.

Kulkarni, A. B., Huh, C. G., Becker, D., Geiser, A., Lyght, M., Flanders, K. C., Roberts, A. B., Sporn, M. B., Ward, J. M., & Karlsson, S. (1993) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.90.2.770 · Cited by 1,967

Efficacy and Safety of Trastuzumab as a Single Agent in First-Line Treatment of HER2-Overexpressing Metastatic Breast Cancer

Vogel, C. L., Cobleigh, M. A., Tripathy, D., Gutheil, J. C., Harris, L. N., Fehrenbacher, L., Slamon, D. J., Murphy, M., Novotny, W. F., Burchmore, M., et al. (2002) · Journal of Clinical Oncology · doi:10.1200/jco.2002.20.3.719 · Cited by 1,860

TGF-ß Signaling in Fibroblasts Modulates the Oncogenic Potential of Adjacent Epithelia

Bhowmick, N. A., Chytil, A., Plieth, D., Gorska, A. E., Dumont, N., Shappell, S., Washington, M. K., Neilson, E. G., & Moses, H. L. (2004) · Science · doi:10.1126/science.1090922 · Cited by 1,401

Immune-mediated eradication of tumors through the blockade of transforming growth factor-β signaling in T cells

Gorelik, L., & Flavell, R. A. (2001) · Nature Medicine · doi:10.1038/nm1001-1118 · Cited by 770

TGFβ1 Inhibits the Formation of Benign Skin Tumors, but Enhances Progression to Invasive Spindle Carcinomas in Transgenic Mice

Cui, W., Fowlis, D. J., Bryson, S., Duffie, E., Ireland, H., Balmain, A., & Akhurst, R. J. (1996) · Cell · doi:10.1016/s0092-8674(00)80127-0 · Cited by 628

Targeting the TGFβ signalling pathway in disease

Akhurst, R. J., & Hata, A. (2012) · Nature Reviews Drug Discovery · doi:10.1038/nrd3810 · Cited by 1,466

TGF-β directly targets cytotoxic T cell functions during tumor evasion of immune surveillance

Thomas, D. A., & Massagué, J. (2005) · Cancer Cell · doi:10.1016/j.ccr.2005.10.012 · Cited by 1,355

To exploit the tumor microenvironment: Since the EPR effect fails in the clinic, what is the future of nanomedicine?

Danhier, F. (2016) · Journal of Controlled Release · doi:10.1016/j.jconrel.2016.11.015 · Cited by 1,288

Dependency of Colorectal Cancer on a TGF-β-Driven Program in Stromal Cells for Metastasis Initiation

Calon, A., Espinet, E., Palomo-Ponce, S., Tauriello, D. V. F., Iglesias, M., Céspedes, M. V., Sevillano, M., Nadal, C., Jung, P., Zhang, X. H.-F., et al. (2012) · Cancer Cell · doi:10.1016/j.ccr.2012.08.013 · Cited by 1,060

Modern pathogenetic concepts of liver fibrosis suggest stellate cells and TGF-β as major players and therapeutic targets

Gressner, A. M., & Weiskirchen, R. (2006) · Journal of Cellular and Molecular Medicine · doi:10.1111/j.1582-4934.2006.tb00292.x · Cited by 718

TGF-β in progression of liver disease

Dooley, S., & ten Dijke, P. (2012) · Cell and Tissue Research · doi:10.1007/s00441-011-1246-y · Cited by 718

Signaling Receptors for TGF-β Family Members

Heldin, C.-H., & Moustakas, A. (2016) · Cold Spring Harbor Perspectives in Biology · doi:10.1101/cshperspect.a022053 · Cited by 711

T cell‐targeting nanoparticles focus delivery of immunotherapy to improve antitumor immunity

Schmid, D., Park, C. G., Hartl, C. A., Subedi, N., Cartwright, A. N., Puerto, R. B., Zheng, Y., Maiarana, J., Freeman, G. J., Wucherpfennig, K. W., et al. (2017) · Nature Communications · doi:10.1038/s41467-017-01830-8 · Cited by 449

Transforming growth factor‐β in stem cells and tissue homeostasis

Xu, X., Zheng, L., Yuan, Q., Zhen, G., Crane, J. L., Zhou, X., & Cao, X. (2018) · Bone Research · doi:10.1038/s41413-017-0005-4 · Cited by 414

Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as monotherapy and in combination with checkpoint blockade

Holmgaard, R. B., Schaer, D. A., Li, Y., Castaneda, S. P., Murphy, M. Y., Xu, X., Inigo, I., Dobkin, J., Manro, J. R., Iversen, P. W., et al. (2018) · Journal for ImmunoTherapy of Cancer · doi:10.1186/s40425-018-0356-4 · Cited by 356

What's wrong with our cancer models?

Kamb, A. (2005) · Nature Reviews Drug Discovery · doi:10.1038/nrd1635 · Cited by 335

Signaling by the Matrix Proteoglycan Decorin Controls Inflammation and Cancer Through PDCD4 and MicroRNA-21

Merline, R., Moreth, K., Beckmann, J., Nastase, M. V., Zeng-Brouwers, J., Tralhão, J. G., Lemarchand, P., Pfeilschifter, J., Schaefer, R. M., Iozzo, R. V., et al. (2011) · Science Signaling · doi:10.1126/scisignal.2001868 · Cited by 333

Hepatic fibrosis: molecular mechanisms and drug targets

Lotersztajn, S., Julien, B., Teixeira-Clerc, F., Grenard, P., & Mallat, A. (2005) · Annual Review of Pharmacology and Toxicology · doi:10.1146/annurev.pharmtox.45.120403.095906 · Cited by 325

TGFβ inhibition restores a regenerative response in acute liver injury by suppressing paracrine senescence

Bird, T. G., Müller, M., Boulter, L., Vincent, D. F., Ridgway, R. A., Lopez-Guadamillas, E., Lu, W.-Y., Jamieson, T., Govaere, O., Campbell, A. D., et al. (2018) · Science Translational Medicine · doi:10.1126/scitranslmed.aan1230 · Cited by 261

Targeted tumor therapy with the TGF-β2 antisense compound AP 12009

SCHLINGENSIEPEN, K., SCHLINGENSIEPEN, R., STEINBRECHER, A., HAU, P., BOGDAHN, U., FISCHERBLASS, B., & JACHIMCZAK, P. (2006) · Cytokine & Growth Factor Reviews · doi:10.1016/j.cytogfr.2005.09.002 · Cited by 195

M7824, a novel bifunctional anti-PD-L1/TGFβ Trap fusion protein, promotes anti-tumor efficacy as monotherapy and in combination with vaccine

Knudson, K. M., Hicks, K. C., Luo, X., Chen, J.-Q., Schlom, J., & Gameiro, S. R. (2018) · OncoImmunology · doi:10.1080/2162402x.2018.1426519 · Cited by 195

Preclinical assessment of galunisertib (LY2157299 monohydrate), a first‐in‐class transforming growth factor‐β receptor type I inhibitor

Yingling, J. M., McMillen, W. T., Yan, L., Huang, H., Sawyer, J. S., Graff, J., Clawson, D. K., Britt, K. S., Anderson, B. D., Beight, D. W., et al. (2018) · Oncotarget · doi:10.18632/oncotarget.23795 · Cited by 187

Antibody-Mediated Blockade of Integrin αvβ6 Inhibits Tumor Progression In vivo by a Transforming Growth Factor-β–Regulated Mechanism

Koopman Van Aarsen, L. A., Leone, D. R., Ho, S., Dolinski, B. M., McCoon, P. E., LePage, D. J., Kelly, R., Heaney, G., Rayhorn, P., Reid, C., et al. (2008) · Cancer Research · doi:10.1158/0008-5472.can-07-2307 · Cited by 146

Anti–Transforming Growth Factor β Receptor II Antibody Has Therapeutic Efficacy against Primary Tumor Growth and Metastasis through Multieffects on Cancer, Stroma, and Immune Cells

Zhong, Z., Carroll, K. D., Policarpio, D., Osborn, C., Gregory, M., Bassi, R., Jimenez, X., Prewett, M., Liebisch, G., Persaud, K., et al. (2010) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-09-1634 · Cited by 123

A Novel Small-Molecule Inhibitor of Transforming Growth Factor β Type I Receptor Kinase (SM16) Inhibits Murine Mesothelioma Tumor Growth In vivo and Prevents Tumor Recurrence after Surgical Resection

Suzuki, E., Kim, S., Cheung, H.-K., Corbley, M. J., Zhang, X., Sun, L., Shan, F., Singh, J., Lee, W.-C., Albelda, S. M., et al. (2007) · Cancer Research · doi:10.1158/0008-5472.can-06-2389 · Cited by 113

Outgrowth of Drug-Resistant Carcinomas Expressing Markers of Tumor Aggression after Long-term TβRI/II Kinase Inhibition with LY2109761

Connolly, E. C., Saunier, E. F., Quigley, D., Luu, M. T., De Sapio, A., Hann, B., Yingling, J. M., & Akhurst, R. J. (2011) · Cancer Research · doi:10.1158/0008-5472.can-10-2941 · Cited by 82

TGF-beta: a master switch in tumor immunity

Gigante, M., Gesualdo, L., & Ranieri, E. (2012) · Current Pharmaceutical Design · doi:10.2174/138161212802430378 · Cited by 45

An engineered transforming growth factor β (TGF-β) monomer that functions as a dominant negative to block TGF-β signaling

Kim, S. K., Barron, L., Hinck, C. S., Petrunak, E. M., Cano, K. E., Thangirala, A., Iskra, B., Brothers, M., Vonberg, M., Leal, B., et al. (2017) · Journal of Biological Chemistry · doi:10.1074/jbc.m116.768754 · Cited by 43

Gene Expression Patterns Associated With Histopathology in Toxic Liver Fibrosis

Ippolito, D. L., AbdulHameed, M. D. M., Tawa, G. J., Baer, C. E., Permenter, M. G., McDyre, B. C., Dennis, W. E., Boyle, M. H., Hobbs, C. A., Streicker, M. A., et al. (2016) · Toxicological Sciences · doi:10.1093/toxsci/kfv214 · Cited by 43

A phase I dose-escalation study to a predefined dose of a transforming growth factor-β1 monoclonal antibody (TβM1) in patients with metastatic cancer

COHN, A., LAHN, M. M., WILLIAMS, K. E., CLEVERLY, A. L., PITOU, C., KADAM, S. K., FARMEN, M. W., DESAIAH, D., RAJU, R., CONKLING, P., et al. (2014) · International Journal of Oncology · doi:10.3892/ijo.2014.2679 · Cited by 43

Evaluation of antitumor activity of a TGF-beta receptor I inhibitor (SD-208) on human colon adenocarcinoma

Akbari, A., Amanpour, S., Muhammadnejad, S., Ghahremani, M. H., Ghaffari, S. H., Dehpour, A. R., Mobini, G. R., Shidfar, F., Abastabar, M., Khoshzaban, A., et al. (2014) · DARU Journal of Pharmaceutical Sciences · doi:10.1186/2008-2231-22-47 · Cited by 33

The impact of stress on tumor growth: peripheral CRF mediates tumor-promoting effects of stress

Arranz, A., Venihaki, M., Mol, B., Androulidaki, A., Dermitzaki, E., Rassouli, O., Ripoll, J., Stathopoulos, E. N., Gomariz, R. P., Margioris, A. N., et al. (2010) · Molecular Cancer · doi:10.1186/1476-4598-9-261 · Cited by 30