Entries by L.E.M Kistemaker

The novel TRPA1 antagonist BI01305834 inhibits ovalbumin-induced bronchoconstriction in guinea pigs

van den Berg MPM, Nijboer-Brinksma S, Bos IST, van den Berge M, Lamb D, van Faassen M, Kema IP, Gosens R, Kistemaker LEM. Respir Res. 2021 Feb 8;22(1):48. Publication: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7871391/. Abstract Background: Asthma is a chronic respiratory disease in which the nervous system plays a central role. Sensory nerve activation, amongst others via Transient Receptor […]

Rho-Kinase 1/2 Inhibition Prevents Transforming Growth Factor-β-Induced Effects on Pulmonary Remodeling and Repair

Wu X, Verschut V, Woest ME, Ng-Blichfeldt JP, Matias A, Villetti G, Accetta A, Facchinetti F, Gosens R, Kistemaker LEM. Front. Pharmacol., 20 January 2021. Publication: https://www.frontiersin.org/articles/10.3389/fphar.2020.609509/full Abstract Transforming growth factor (TGF)-β-induced myofibroblast transformation and alterations in mesenchymal-epithelial interactions contribute to chronic lung diseases such as chronic obstructive pulmonary disease (COPD), asthma and pulmonary fibrosis. […]

Differential effects of pirfenidone and nintedanib on mouse alveolar epithelial organoids

Manon Woest, Vicky Verschut, Reinoud Gosens, Loes Kistemaker ERS International Congress 2020 Abstract Rationale: Idiopathic pulmonary fibrosis is characterised by dysfunctional epithelial-mesenchymal communication and insufficient epithelial repair. Nintedanib and pirfenidone are the only approved pharmacological interventions for IPF that are known to affect the course of the disease. The mechanisms involved are not completely understood. […]

Pharmacological Screening Identifies SHK242 and SHK277 as Novel Arginase Inhibitors With Efficacy Against Allergen-Induced Airway Narrowing In Vitro and In Vivo

van den Berg MPM, Kurhade SH, Maarsingh H, Erceg S, Hulsbeek IR, Boekema PH, Kistemaker LEM, van Faassen M, Kema IP, Elsinga PH, Dömling A, Meurs H, Gosens R. J Pharmacol Exp Ther. 2020 Jul;374(1):62-73. Publication: https://pubmed.ncbi.nlm.nih.gov/32269169/ Abstract Arginase is a potential target for asthma treatment. However, there are currently no arginase inhibitors available for clinical […]

Cholinergic Neuroplasticity in Asthma Driven by TrkB Signaling

Dragunas G, Woest ME, Nijboer S, Bos ST, van Asselt J, de Groot AP, Vohlídalová E, Vermeulen CJ, Ditz B, Vonk JM, Koppelman GH, van den Berge M, Ten Hacken NHT, Timens W, Munhoz CD, Prakash YS, Gosens R, Kistemaker LEM. FASEB J. 2020 Jun;34(6):7703-7717. Publication: https://pubmed.ncbi.nlm.nih.gov/32277855/ Abstract Parasympathetic neurons in the airways control bronchomotor […]

Mesenchymal WNT-5A/5B Signaling Represses Lung Alveolar Epithelial Progenitors

Wu X, van Dijk EM, Ng-Blichfeldt JP, Bos IST, Ciminieri C, Königshoff M, Kistemaker LEM, Gosens R. Cells. 2019 Sep 25;8(10):1147. Publication: https://pubmed.ncbi.nlm.nih.gov/31557955 Abstract Chronic obstructive pulmonary disease (COPD) represents a worldwide concern with high morbidity and mortality, and is believed to be associated with accelerated ageing of the lung. Alveolar abnormalities leading to emphysema are […]

Second M3 Muscarinic Receptor Binding Site Contributes to Bronchoprotection by Tiotropium

Kistemaker LEM, Elzinga CRS, Tautermann CS, Pieper MP, Seeliger D, Alikhil S, Schmidt M, Meurs H, Gosens R. Br J Pharmacol. 2019 Aug;176(16):2864-2876. Publication: https://pubmed.ncbi.nlm.nih.gov/31077341 Abstract Background and purpose: The bronchodilator tiotropium binds not only to its main binding site on the M3 muscarinic receptor but also to an allosteric site. Here, we have investigated the functional relevance […]

The PDE4 inhibitor CHF-6001 and LAMAs inhibit bronchoconstriction-induced remodeling in lung slices

Kistemaker LEM, Oenema TA, Baarsma HA, Bos IST, Schmidt M, Facchinetti F, Civelli M, Villetti G, Gosens R. Am J Physiol Lung Cell Mol Physiol. 2017 Sep 1;313(3):L507-L515. Publication: http://www.ncbi.nlm.nih.gov/pubmed/28596292 Abstract Combination therapy of PDE4 inhibitors and anticholinergics induces bronchoprotection in COPD. Mechanical forces that arise during bronchoconstriction may contribute to airway remodeling. Therefore, we investigated […]

HDAC-3 selective inhibitor RGFP966 demonstrates anti-inflammatory properties by attenuating NF-κB p65 transcriptional activity

Leus NG, van der Wouden PE, van den Bosch T, Hooghiemstra WT, Ourailidou ME, Kistemaker LEM, Bischoff R, Gosens R, Haisma HJ & Dekker FJ. Biochem Pharmacol. 2016 May 15;108:58-74. Publication: http://www.ncbi.nlm.nih.gov/pubmed/26993378 Abstract The increasing number of patients suffering from chronic obstructive pulmonary disease (COPD) represents a major and increasing health problem. Therefore, novel therapeutic approaches […]