[HTML][HTML] Autotaxin in the crosshairs: taking aim at cancer and other inflammatory conditions

MGK Benesch, YM Ko, TPW McMullen, DN Brindley - FEBS letters, 2014 - Elsevier
Autotaxin is a secreted enzyme that produces most of the extracellular lysophosphatidate
from lysophosphatidylcholine, the most abundant phospholipid in blood plasma …

Autotaxin inhibitors: a patent review

E Barbayianni, V Magrioti… - Expert opinion on …, 2013 - Taylor & Francis
Introduction: Autotaxin (ATX) is a lysophospholipase D enzyme that hydrolyzes
lysophosphatidylcholine to lysophosphatidic acid (LPA) and choline. LPA is a bioactive lipid …

Highly potent non-carboxylic acid autotaxin inhibitors reduce melanoma metastasis and chemotherapeutic resistance of breast cancer stem cells

S Banerjee, DD Norman, SC Lee… - Journal of medicinal …, 2017 - ACS Publications
Autotaxin (ATX, aka. ENPP2) is the main source of the lipid mediator lysophosphatidic acid
(LPA) in biological fluids. This study reports on inhibitors of ATX derived by lead optimization …

Hits of a high-throughput screen identify the hydrophobic pocket of autotaxin/lysophospholipase D as an inhibitory surface

JI Fells, SC Lee, Y Fujiwara, DD Norman, KG Lim… - Molecular …, 2013 - ASPET
Autotaxin (ATX), a lysophospholipase D, plays an important role in cancer invasion,
metastasis, tumor progression, tumorigenesis, neuropathic pain, fibrotic diseases …

Identification of novel phosphodiesterase-4D inhibitors prescreened by molecular dynamics-augmented modeling and validated by bioassay

Z Li, YH Cai, YK Cheng, X Lu, YX Shao… - Journal of chemical …, 2013 - ACS Publications
Phosphodiesterase-4D (PDE4D) has been proved to be a potential therapeutic target
against strokes. In the present study, a procedure of integrating pharmacophore, molecular …

Autotaxin inhibition: development and application of computational tools to identify site-selective lead compounds

DD Norman, A Ibezim, WE Scott, S White… - Bioorganic & medicinal …, 2013 - Elsevier
Autotaxin (ATX) catalyzes the conversion of lysophosphatidyl choline (LPC) to
lysophosphatidic acid (LPA). Both ATX and LPA have been linked to pathophysiologies …

Development of lysophosphatidic acid pathway modulators as therapies for fibrosis

DC Budd, Y Qian - Future medicinal chemistry, 2013 - Future Science
Lysophosphatidic acid (LPA) is a class of bioactive phospholipid that displays a wide range
of cellular effects via LPA receptors, of which six have been identified (LPAR1–6). In serum …

In silico design of anti-atherogenic biomaterials

DR Lewis, V Kholodovych, MD Tomasini… - Biomaterials, 2013 - Elsevier
Atherogenesis, the uncontrolled deposition of modified lipoproteins in inflamed arteries,
serves as a focal trigger of cardiovascular disease (CVD). Polymeric biomaterials have been …

Autotaxin-an enzymatic augmenter of malignant progression linked to inflammation

DN Brindley, MGK Benesch… - … Clinical Management and …, 2015 - books.google.com
Malignant melanoma cells are incredibly hardy, stemming from their intrinsic defensive
nature. These cells inherit unique characteristics, which allowed their non-malignant prede …

ANN-QSAR model for virtual screening of androstenedione C-skeleton containing phytomolecules and analogues for cytotoxic activity against human breast cancer …

O Prakash, F Khan, RS Sangwan… - … Chemistry & High …, 2013 - ingentaconnect.com
The present study deals with the development of an artificial neural network based
quantitative structure activity relationship (QSAR) model for virtual screening of active …