4.7 Article

Discovery of Clinical Candidate ACT-777991, a Potent CXCR3 Antagonist for Antigen-Driven and Inflammatory Pathologies

相关参考文献

注意:仅列出部分参考文献,下载原文获取全部文献信息。
Article Chemistry, Medicinal

Design, Synthesis, and Pharmacological Evaluation of Benzimidazolo-thiazoles as Potent CXCR3 Antagonists with Therapeutic Potential in Autoimmune Diseases: Discovery of ACT-672125

Eva Caroff et al.

Summary: This study investigates the clinical potential of CXCR3 chemokine receptor in autoimmune diseases. By exploring the benzimidazolo-thiazole core scaffold, the potency of the antagonist is optimized and adverse reactions are mitigated. The CXCR3 antagonist ACT-672125 is shown to dose-dependently inhibit the recruitment of CXCR3 expressing T cells in inflamed lungs.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases

Emmanuel A. Meyer et al.

Summary: The chemokine receptor CXCR3 is involved in autoimmune diseases and its selective antagonist ACT-660602 has been discovered through chemical optimization. This antagonist has shown promising results in reducing tissue damage caused by inflammation in a mouse model.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Pharmacology & Pharmacy

CXCR7 Antagonism Reduces Acute Lung Injury Pathogenesis

Laetitia Pouzol et al.

Summary: The loss of control in immune cell trafficking to inflamed lung tissue leads to ALI/ARDS. The paper investigates the pathological role of the CXCR3/CXCR4/CXCR7 axis in a murine model of ALI. The study suggests the clinical potential of the CXCR7 antagonist, ACT-1004-1239, in reducing inflammation and improving lung function in ALI/ARDS.

FRONTIERS IN PHARMACOLOGY (2021)

Review Chemistry, Medicinal

hERG toxicity assessment: Useful guidelines for drug design

Amanda Garrido et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Chemistry, Multidisciplinary

Taming Ambident Triazole Anions: Regioselective Ion Pairing Catalyzes Direct N-Alkylation with Atypical Regioselectivity

Harvey J. A. Dale et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2019)

Article Chemistry, Medicinal

Decreasing the CYP2D6 contribution to metabolism of a CK1 epsilon inhibitor

Roy J. Vaz et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2018)

Review Medicine, General & Internal

The Role of CXCR3 and Its Chemokine Ligands in Skin Disease and Cancer

Paula T. Kuo et al.

FRONTIERS IN MEDICINE (2018)

Review Pharmacology & Pharmacy

Designing small molecule CXCR3 antagonists

James E. Pease

EXPERT OPINION ON DRUG DISCOVERY (2017)

Article Gastroenterology & Hepatology

Eldelumab [Anti-IP-10] Induction Therapy for Ulcerative Colitis: A Randomised, Placebo-Controlled, Phase 2b Study

William J. Sandborn et al.

JOURNAL OF CROHNS & COLITIS (2016)

Article Chemistry, Medicinal

Small Molecule CXCR3 Antagonists

Stephen P. Andrews et al.

JOURNAL OF MEDICINAL CHEMISTRY (2016)

Article Pharmacology & Pharmacy

Pharmacometric Analyses to Support Early Development Decisions for LY2878735: A Novel Serotonin Norepinephrine Reuptake Inhibitor

E. Raddad et al.

CPT-PHARMACOMETRICS & SYSTEMS PHARMACOLOGY (2013)

Review Oncology

CXCR3 in T cell function

Joanna R. Groom et al.

EXPERIMENTAL CELL RESEARCH (2011)

Review Cell Biology

CXCR3 ligands: redundant, collaborative and antagonistic functions

Joanna R. Groom et al.

IMMUNOLOGY AND CELL BIOLOGY (2011)

Article Pharmacology & Pharmacy

Desipramine, substrate for CYP2D6 activity: population pharmacokinetic model and design elements of drug-drug interaction trials

Ivelina Gueorguieva et al.

BRITISH JOURNAL OF CLINICAL PHARMACOLOGY (2010)

Review Pharmacology & Pharmacy

Polymorphism of Human Cytochrome P450 2D6 and Its Clinical Significance Part I

Shu-Feng Zhou

CLINICAL PHARMACOKINETICS (2009)

Article Chemistry, Organic

An investigation into the alkylation of 1,2,4-triazole

PG Bulger et al.

TETRAHEDRON LETTERS (2000)