Entries by L.E.M Kistemaker

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 […]

Combination therapy of tiotropium and ciclesonide attenuates airway inflammation and remodeling in a guinea pig model of chronic asthma

Kistemaker LEM, Bos IST, Menzen MH, Maarsingh H, Meurs H & Gosens R. Resp Res 2016 Feb 4. Publication: http://www.ncbi.nlm.nih.gov/pubmed/26846267 Abstract Background: The long-acting anticholinergic tiotropium has recently been registered for the treatment of asthma, and its use is associated with a reduction in exacerbation frequency. Anti-inflammatory and anti-remodeling effects of tiotropium have been demonstrated in […]

Anti-inflammatory effects of targeted lung denervation in patients with COPD.

Kistemaker LEM, Slebos DJ, Meurs H, Kerstjens HAM & Gosens R. Eur Respir J. 2015 Sep 4. Publication: http://www.ncbi.nlm.nih.gov/pubmed/26341988 Abstract Background: Acetylcholine does not only induce bronchoconstriction, but is also identified as a regulator of airway inflammation in animal models of COPD. This has not been demonstrated in patients with COPD. Targeted lung denervation (TLD) is a […]