Targeting cancer-associated fibroblasts: Challenges, opportunities and future directions
Cancer-associated fibroblasts (CAFs) are a common cell in the tumour microenvironment
with diverse tumour-promoting functions. Their presence in tumours is commonly associated …
with diverse tumour-promoting functions. Their presence in tumours is commonly associated …
Designing dual inhibitors of autotaxin-lpar gpcr axis
S Banerjee, S Lee, DD Norman, GJ Tigyi - Molecules, 2022 - mdpi.com
The ATX-LPA-LPAR1 signaling pathway plays a universal role in stimulating diverse cellular
responses, including cell proliferation, migration, survival, and invasion in almost every cell …
responses, including cell proliferation, migration, survival, and invasion in almost every cell …
Discovery of a novel orally active, selective LPA receptor type 1 antagonist, 4-(4-(2-isopropylphenyl)-4-((2-methoxy-4-methylphenyl) carbamoyl) piperidin-1-yl)-4 …
C Lescop, C Brotschi, JT Williams… - Journal of Medicinal …, 2024 - ACS Publications
Lysophosphatidic acid receptor 1 (LPAR1) antagonists show promise as potentially novel
antifibrotic treatments. In a human LPAR1 β-arrestin recruitment-based high-throughput …
antifibrotic treatments. In a human LPAR1 β-arrestin recruitment-based high-throughput …
Integration of an LPAR1 antagonist into liposomes enhances their internalization and tumor accumulation in an animal model of human metastatic breast cancer
Lysophosphatidic acid receptor 1 (LPAR1) is elevated in breast cancer. The deregulation of
LPAR1, including the function and level of expression, is linked to cancer initiation …
LPAR1, including the function and level of expression, is linked to cancer initiation …
Endothelial specific deletion of autotaxin improves stroke outcomes
Autotaxin (ATX) is an extracellular secretory enzyme (lysophospholipase D) that catalyzes
the hydrolysis of lysophosphatidyl choline to lysophosphatidic acid (LPA). The ATX–LPA …
the hydrolysis of lysophosphatidyl choline to lysophosphatidic acid (LPA). The ATX–LPA …
Identification of genetic fingerprint of type I interferon therapy in visceral metastases of melanoma
L Vízkeleti, O Papp, V Doma, J Gil, G Markó-Varga… - Scientific Reports, 2024 - nature.com
Malignant melanoma is a difficult-to-treat skin cancer with increasing incidence worldwide.
Although type-I interferon (IFN) is no longer part of guidelines, several melanoma patients …
Although type-I interferon (IFN) is no longer part of guidelines, several melanoma patients …
LPA suppresses HLA-DR expression in human melanoma cells: a potential immune escape mechanism involving LPAR1 and DR6-mediated release of IL-10
While immune checkpoint inhibitors (ICIs) are promising in the treatment of metastatic
melanoma, about half of patients do not respond well to them. Low levels of human …
melanoma, about half of patients do not respond well to them. Low levels of human …
Design, synthesis and promising anti-tumor efficacy of novel imidazo [1, 2-a] pyridine derivatives as potent autotaxin allosteric inhibitors
H Lei, X Wang, G Zhao, T Li, Y Cui, H Wu… - European Journal of …, 2022 - Elsevier
Aiming to track the potential antitumor effect of novel allosteric autotaxin (ATX) inhibitors, a
hybrid strategy was utilized by merging ATX inhibitors PF-8380 and GLPG1690, while the …
hybrid strategy was utilized by merging ATX inhibitors PF-8380 and GLPG1690, while the …
The LPA3 Receptor: Regulation and Activation of Signaling Pathways
KH Solís, MT Romero-Ávila, A Guzmán-Silva… - International journal of …, 2021 - mdpi.com
The lysophosphatidic acid 3 receptor (LPA3) participates in different physiological actions
and in the pathogenesis of many diseases through the activation of different signal …
and in the pathogenesis of many diseases through the activation of different signal …
BBT-877, a Novel Autotaxin Inhibitor, Abrogates Drug Resistance in Epithelial Ovarian Cancer Stem Cells
JS Kim, MJ Shin, SY Lee, SM Choi, K Choi… - Anticancer …, 2024 - ar.iiarjournals.org
Background/Aim: Cancer stem cells (CSCs) contribute significantly to the poor prognosis of
patients with epithelial ovarian cancer (EOC) due to their roles in drug resistance and tumor …
patients with epithelial ovarian cancer (EOC) due to their roles in drug resistance and tumor …