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An optimized derivative of an endogenous CXCR4 antagonist prevents atopic dermatitis and airway inflammation

Acta Pharmaceutica Sinica B 2021年第9期11卷 2694-2708页

作者： Mirja Harms Monica MWHabib Simona Nemska Antonella Nicolò andrea gilg Nico Preising Pandian Sokkar Sara Carmignani Martina Raasholm Gilbert Weidinger Gönül Kizilsavas Manfred Wagner Ludger Ständker Ashraf HAbadi Hassan Jumaa Frank Kirchhoff Nelly Frossard Elsa Sanchez-Garcia Jan Münch Institute of Molecular Virology Ulm University Medical CenterUlm 89081Germany Department of Pharmaceutical Chemistry Faculty of Pharmacy and BiotechnologyGerman University in CairoCairo 11835Egypt Laboratoire D'Innovation Thérapeutique UMR7200 CNRS/Universitéde Strasbourg and LabEx MEDALISFacultéde PharmacieIllkirch 67412France Institute of Immunology Ulm University Medical CenterUlm 89081Germany Core Facility Functional Peptidomics Ulm University Medical CenterUlm 89081Germany Center of Medical Biotechnology University of Duisburg-EssenDuisburg 47057Germany Max-Planck-Institute for Coal Research Düsseldorf 45470Germany Faculty of Allied Health Sciences Chettinad Hospital and Research InstituteChettinad Academy of Research and EducationKelambakkam 603103India Max-Planck-Institut für Molekulare Physiologie Dortmund 44227Germany Institute of Biochemistry and Molecular Biology Ulm UniversityUlm 89081Germany Max Planck Institute for Polymer Research Mainz 55128Germany

Aberrant CXCR4/CXCL12 signaling is involved in many pathophysiological processes such as cancer and inflammatory diseases.A natural fragment of serum albumin,named EPI-X4,has previously been identified as endogenous peptide antagonist and inverse agonist of CXCR4 and is a promising compound for the development of improved analogues for the therapy of CXCR4-associated *** generate optimized EPI-X4 derivatives we here performed molecular docking analysis to identify key interaction motifs of EPI-X4/*** rational drug design allowed to increase the anti-CXCR4 activity of *** EPI-X4 derivative JM#21 bound CXCR4 and suppressed CXCR4-tropic HIV-1 infection more efficiently than the clinically approved small molecule CXCR4 antagonist ***-X4 JM#21 did not exert toxic effects in zebrafish embryos and suppressed allergen-induced infiltration of eosinophils and other immune cells into the airways of animals in an asthma mouse ***,topical administration of the optimized EPI-X4 derivative efficiently prevented inflammation of the skin in a mouse model of atopic ***,rationally designed EPIX4 JM#21 is a novel potent antagonist of CXCR4 and the first CXCR4 inhibitor with therapeutic efficacy in atopic *** clinical development of this new class of CXCR4 antagonists for the therapy of atopic dermatitis,asthma and other CXCR4-associated diseases is highly warranted.

关键词： CXCR4 antagonist Asthma Allergy Inflammation Atopic dermatitis

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