Recent research advances in ATX inhibitors: An overview of primary literature.

The autoglobulin gene is the main enzyme for circulating LPA production and has lysophosphatidylcholine D activity, which catalyzes the production of lysophosphatidic acid and choline with lysophosphatidylcholine as substrate. A growing body of experimental evidence suggests that autoglobulin is involved in the pathogenesis of a variety of diseases. This review summarizes the different structural ATX inhibitors classified according to their binding mode to the ATX triple orientation site, and summarizes the conformational relationships and molecular docking of each type with ATX structure, hoping to contribute to the development of novel ATX inhibitors.

• Publication year

  2023

• Venue

  Bioorganic & Medicinal Chemistry

• Publication date

  2023-06-15

• Fields of study

  Medicine, Chemistry

• Identifiers
  DOI 10.1016/j.bmc.2023.117374PMID 37354726
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Design, synthesis and promising anti-tumor efficacy of novel imidazo[1,2-a]pyridine derivatives as potent autotaxin allosteric inhibitors.

  2022cited by this paper
• Structure-Based Design of a Novel Class of Autotaxin Inhibitors Based on Endogenous Allosteric Modulators

  2022cited by this paper
• Discovery of Potent Selective Nonzinc Binding Autotaxin Inhibitor BIO-32546.

  2021cited by this paper
• Novel 4-(piperazin-1-yl)quinolin-2(1H)-one bearing thiazoles with antiproliferative activity through VEGFR-2-TK inhibition.

  2021cited by this paper
• Evaluation of serum ATX and LPA as potential diagnostic biomarkers in patients with pancreatic cancer

  2021cited by this paper
• The Expression Regulation and Biological Function of Autotaxin

  2021cited by this paper
• LPA and Autotaxin: Potential Drug Targets in Asthma?

  2021cited by this paper
• Structure–property correlations in piracetam polytypes

  2021cited by this paper
• Design and Development of Autotaxin Inhibitors

  2021cited by this paper
• Structural and PK-guided identification of indole-based non-acidic autotaxin (ATX) inhibitors exhibiting high in vivo anti-fibrosis efficacy in rodent model.

  2021cited by this paper
• Design, synthesis, and biological evaluation of novel pyrrolidinone small-molecule Formyl peptide receptor 2 agonists.

  2021cited by this paper
• Design, synthesis and anti-fibrosis evaluation of imidazo[1,2-a]pyridine derivatives as potent ATX inhibitors.

  2021cited by this paper
• The correlation between the autotaxin enzyme and pruritus in Egyptian patients suffering from chronic liver disease.

  2021cited by this paper
• Analgesic and Anticancer Activity of Benzoxazole Clubbed 2-Pyrrolidinones as Novel Inhibitors of Monoacylglycerol Lipase

  2021cited by this paper
• Novel imidazo[1,2-a]pyridine derivatives as potent ATX allosteric inhibitors: Design, synthesis and promising in vivo anti-fibrotic efficacy in mice lung model.

  2021cited by this paper
• Design, synthesis and evaluation of hydrazine and acyl hydrazone derivatives of 5-pyrrolidin-2-one as antifungal agents.

  2020cited by this paper
• Structure guided design of potent indole-based ATX inhibitors bearing hydrazone moiety with tumor suppression effects.

  2020cited by this paper
• Molecular modelling guided design, synthesis and QSAR analysis of new small molecule non-lipid autotaxin inhibitors.

  2020cited by this paper
• Structure-based linker exploration: Discovery of 1-ethyl-1H-indole analogs as novel ATX inhibitors.

  2020cited by this paper
• The bioavailability and maturing clearance of doxapram in preterm infants

  2020cited by this paper
• Design, microwave‐assisted synthesis, biological evaluation and molecular modeling studies of 4‐phenylthiazoles as potent fatty acid amide hydrolase inhibitors

  2020cited by this paper
• Identification of potent in vivo autotaxin inhibitors that bind to both hydrophobic pocket and channel in the catalytic domain.

  2020cited by this paper
• Roles for lysophosphatidic acid signaling in vascular development and disease.

  2020cited by this paper
• Discovery of Novel Indole-based Allosteric Highly Potent ATX Inhibitors with Great in vivo Efficacy in Mouse Lung Fibrosis Model.

  2020cited by this paper
• Optimization and evaluation of novel tetrahydropyrido[4,3-d]pyrimidine derivatives as ATX inhibitors for cardiac and hepatic fibrosis.

  2019cited by this paper
• Synthesis of novel 2-pyrrolidinone and pyrrolidine derivatives and study of their inhibitory activity against autotaxin enzyme.

  2019cited by this paper
• O17 The bioavailability and maturing clearance of doxapram in preterm infants

  2019cited by this paper
• Benzoxaboroles—Novel Autotaxin Inhibitors

  2019cited by this paper
• Development of 2-amino-4-phenylthiazole analogues to disrupt myeloid differentiation factor 88 and prevent inflammatory responses in acute lung injury.

  2019cited by this paper
• Substituted 4-phenylthiazoles: Development of potent and selective A1, A3 and dual A1/A3 adenosine receptor antagonists.

  2019cited by this paper
• Autotaxin in Pathophysiology and Pulmonary Fibrosis

  2018cited by this paper
• ATX-LPA axis facilitates estrogen-induced endometrial cancer cell proliferation via MAPK/ERK signaling pathway

  2018cited by this paper
• Discovery and optimization of tetrahydropyrido[4,3-d]pyrimidine derivatives as novel ATX and EGFR dual inhibitors.

  2018cited by this paper
• Discovery and optimization of ATX inhibitors via modeling, synthesis and biological evaluation.

  2018cited by this paper
• Safety, tolerability, pharmacokinetics, and pharmacodynamics of GLPG1690, a novel autotaxin inhibitor, to treat idiopathic pulmonary fibrosis (FLORA): a phase 2a randomised placebo-controlled trial.

  2018cited by this paper
• Pharmacologic targeting of the ATX/LPA axis attenuates bleomycin-induced pulmonary fibrosis.

  2018cited by this paper
• Design, synthesis, and biological evaluation of 2,4‐dihydropyrano[2,3‐c]pyrazole derivatives as autotaxin inhibitors

  2017cited by this paper
• Discovery, Structure-Activity Relationship, and Binding Mode of an Imidazo[1,2-a]pyridine Series of Autotaxin Inhibitors.

  2017cited by this paper
• Selective Inhibition of Autotaxin Is Efficacious in Mouse Models of Liver Fibrosis

  2017cited by this paper
• Design, synthesis, docking and biological evaluation of 4-phenyl-thiazole derivatives as autotaxin (ATX) inhibitors.

  2017cited by this paper
• Highly Potent Non-Carboxylic Acid Autotaxin Inhibitors Reduce Melanoma Metastasis and Chemotherapeutic Resistance of Breast Cancer Stem Cells.

  2017cited by this paper
• Discovery of 2-[[2-Ethyl-6-[4-[2-(3-hydroxyazetidin-1-yl)-2-oxoethyl]piperazin-1-yl]-8-methylimidazo[1,2-a]pyridin-3-yl]methylamino]-4-(4-fluorophenyl)thiazole-5-carbonitrile (GLPG1690), a First-in-Class Autotaxin Inhibitor Undergoing Clinical Evaluation for the Treatment of Idiopathic Pulmonary Fib

  2017cited by this paper
• Discovery of BI-2545: A Novel Autotaxin Inhibitor That Significantly Reduces LPA Levels in Vivo.

  2017cited by this paper
• Autotaxin inhibitors: a patent review (2012-2016)

  2017cited by this paper
• Structure-Activity Relationships of Small Molecule Autotaxin Inhibitors with a Discrete Binding Mode.

  2017cited by this paper
• Autotaxin activity increases locally following lung injury, but is not required for pulmonary lysophosphatidic acid production or fibrosis

  2016cited by this paper
• Discovery of potent inhibitors of the lysophospholipase autotaxin.

  2016cited by this paper
• Structural Basis for Inhibition of Human Autotaxin by Four Potent Compounds with Distinct Modes of Binding

  2015cited by this paper
• Autotaxin, a secreted lysophospholipase D, as a promising therapeutic target in chronic inflammation and cancer.

  2015cited by this paper
• Targeting the hydrophobic pocket of autotaxin with virtual screening of inhibitors identifies a common aromatic sulfonamide structural motif

  2014cited by this paper
• Hits of a High-Throughput Screen Identify the Hydrophobic Pocket of Autotaxin/Lysophospholipase D As an Inhibitory Surface

  2013cited by this paper
• Chemical Evolution of Autotaxin Inhibitors

  2012cited by this paper
• Structure-Based Design of Novel Boronic Acid-Based Inhibitors of Autotaxin

  2011cited by this paper
• Boronic acid-based inhibitor of autotaxin reveals rapid turnover of LPA in the circulation

  2010cited by this paper
• Structural basis for substrate discrimination and integrin binding by autotaxin

  2010cited by this paper
• Discovery and optimization of boronic acid based inhibitors of autotaxin.

  2010cited by this paper
• Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors.

  2007cited by this paper

• Ligand Binding Prediction on Pharmaceutical and Nucleic Acid Targets by the CoDock Group in CASP16

  2025cites this paper
• Structure-Based Discovery of MolPort-137: A Novel Autotaxin Inhibitor That Improves Paclitaxel Efficacy

  2025cites this paper
• Development of potent indole-3-carboxamide autotaxin inhibitors with preferred lipophilicity for in vivo treatment of pulmonary fibrosis.

  2025cites this paper
• Calvatine A and B, pyrrolidone alkaloids as M3 receptor antagonists from Pyrrosia calvata

  2025cites this paper
• Development of Tricyclic 4,5-Dihydro-3H-pyrrolo[2,3-c]quinolin-4-ones as Potent Autotaxin Inhibitors for Pulmonary Fibrosis Treatment In Vivo.

  2025cites this paper
• Amplex red assay, a standardized in vitro protocol to quantify the efficacy of autotaxin inhibitors

  2025cites this paper
• Optimization of a DNA encoded library derived autotaxin inhibitor hit to a potent in vivo LPA lowering quinazolinone compound with a non‑zinc binding mode.

  2025cites this paper
• Design, Synthesis, and Biological Implications of Autotaxin inhibitors with a Three-Point lock binding mode.

  2025cites this paper
• Allosteric inhibitors for the treatment of cancers (2021-): A review from medicinal chemistry perspectives

  2025cites this paper
• Autotaxin and Lysophosphatidate Signaling: Prime Targets for Mitigating Therapy Resistance in Breast Cancer

  2024influential citation
• Virtual screening and molecular dynamics investigations using natural compounds against autotaxin for the treatment of chronic pain

  2024cites this paper
• Experimental autotaxin inhibitors for the treatment of idiopathic pulmonary fibrosis

  2024cites this paper
• Novel Autotaxin Inhibitor ATX-1d Significantly Enhances Potency of Paclitaxel—An In Silico and In Vitro Study

  2024cites this paper
• Design, synthesis and evaluation of 3-(2-(substituted benzyloxy)benzylidene) pyrrolidine-2,5-dione derivatives for novel ATX inhibitor.

  2024cites this paper
• Accurate prediction of protein–ligand interactions by combining physical energy functions and graph-neural networks

  2024cites this paper
• Discovery of Novel 4,5,6,7-Tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one Derivatives as Orally Efficacious ATX Allosteric Inhibitors for the Treatment of Pulmonary Fibrosis.

  2024cites this paper
• A Review of Cyclic Phosphatidic Acid and Other Potential Therapeutic Targets for Treating Osteoarthritis

  2023cites this paper