[HTML][HTML] Clinical development of galunisertib (LY2157299 monohydrate), a small molecule inhibitor of transforming growth factor-beta signaling pathway
S Herbertz, JS Sawyer, AJ Stauber… - Drug design …, 2015 - Taylor & Francis
Transforming growth factor-beta (TGF-β) signaling regulates a wide range of biological
processes. TGF-β plays an important role in tumorigenesis and contributes to the hallmarks …
processes. TGF-β plays an important role in tumorigenesis and contributes to the hallmarks …
[HTML][HTML] Targeting the TGFβ pathway with galunisertib, a TGFβRI small molecule inhibitor, promotes anti-tumor immunity leading to durable, complete responses, as …
RB Holmgaard, DA Schaer, Y Li, SP Castaneda… - … for immunotherapy of …, 2018 - Springer
Background TGFβ signaling plays a pleotropic role in tumor biology, promoting tumor
proliferation, invasion and metastasis, and escape from immune surveillance. Inhibiting …
proliferation, invasion and metastasis, and escape from immune surveillance. Inhibiting …
[HTML][HTML] Preclinical assessment of galunisertib (LY2157299 monohydrate), a first-in-class transforming growth factor-β receptor type I inhibitor
JM Yingling, WT McMillen, L Yan, H Huang… - Oncotarget, 2018 - ncbi.nlm.nih.gov
Transforming growth factor-β (TGFβ) is an important driver of tumor growth via intrinsic and
extrinsic mechanisms, and is therefore an attractive target for developing cancer …
extrinsic mechanisms, and is therefore an attractive target for developing cancer …
TGFβ receptor inhibitor galunisertib is linked to inflammation-and remodeling-related proteins in patients with pancreatic cancer
D Melisi, R Garcia-Carbonero, T Macarulla… - Cancer chemotherapy …, 2019 - Springer
Purpose Galunisertib, the first small molecule transforming growth factor beta (TGFβ)
receptor inhibitor, plus gemcitabine resulted in the improvement of survival in patients with …
receptor inhibitor, plus gemcitabine resulted in the improvement of survival in patients with …
Targeting TGF βR2‐mutant tumors exposes vulnerabilities to stromal TGF β blockade in pancreatic cancer
TGF β is important during pancreatic ductal adenocarcinoma (PDA) progression. Canonical
TGF β signaling suppresses epithelial pancreatic cancer cell proliferation; as a result …
TGF β signaling suppresses epithelial pancreatic cancer cell proliferation; as a result …
Autocrine TGFβ is a survival factor for monocytes and drives immunosuppressive lineage commitment
A Gonzalez-Junca, KE Driscoll, I Pellicciotta, S Du… - Cancer immunology …, 2019 - AACR
Transforming growth factor β (TGFβ) is an effector of immune suppression and contributes to
a permissive tumor microenvironment that compromises effective immunotherapy. We …
a permissive tumor microenvironment that compromises effective immunotherapy. We …
The molecular basis of blocking the TIM-3 checkpoint with the LY3321367 mAb in cancer immunotherapy
The anti-T-cell immunoglobulin and mucin-domain containing-3 (TIM-3) antibody
LY3321367 is a promising immune-checkpoint inhibitor that is being clinically tested for the …
LY3321367 is a promising immune-checkpoint inhibitor that is being clinically tested for the …
[HTML][HTML] A herpesvirus transactivator and cellular POU proteins extensively regulate DNA binding of the host Notch signaling protein RBP-Jκ to the virus genome
O Gonzalez-Lopez, J DeCotiis, C Goyeneche… - Journal of Biological …, 2019 - ASBMB
Reactivation of Kaposi's sarcoma-associated herpesvirus (KSHV) from latency requires the
viral transactivator Rta to contact the host protein Jκ recombination signal-binding protein …
viral transactivator Rta to contact the host protein Jκ recombination signal-binding protein …
Abstract B68: Targeted inhibition of Tgfβr2 reduces IL-6 production from cancer-associated fibroblasts, suppresses Stat3 activation in pancreatic cancer cells and …
Pancreatic cancer is characterized by dense stroma consisting of myofibroblasts, abundant
extracellular matrix (ECM) and inflammatory/immune cells. Elevated levels of transforming …
extracellular matrix (ECM) and inflammatory/immune cells. Elevated levels of transforming …
[PDF][PDF] Rikke B. Holmgaard2, David A. Schaer2, Yanxia Li2, Stephen P. Castaneda2, Mary Y. Murphy2, Xiaohong Xu2, Ivan Inigo2, Julie Dobkin2, Jason R. Manro1 …
RD Novosiadly, KA Benhadji, GD Plowman, M Kalos… - 2018 - jitc.biomedcentral.com
Background: TGFβ signaling plays a pleotropic role in tumor biology, promoting tumor
proliferation, invasion and metastasis, and escape from immune surveillance. Inhibiting …
proliferation, invasion and metastasis, and escape from immune surveillance. Inhibiting …