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Signaling of an allosteric, nanomolar potent, low molecular weight agonist for the follicle-stimulating hormone receptor.
Biochem Pharmacol. 2013 Apr 15;85(8):1162-70. doi: 10.1016/j.bcp.2013.02.001. Epub 2013 Feb 13.
Biochem Pharmacol. 2013.
PMID: 23415902
Identification of substituted 6-amino-4-phenyltetrahydroquinoline derivatives: potent antagonists for the follicle-stimulating hormone receptor.
van Straten NC, van Berkel TH, Demont DR, Karstens WJ, Merkx R, Oosterom J, Schulz J, van Someren RG, Timmers CM, van Zandvoort PM.
van Straten NC, et al. Among authors: karstens wj.
J Med Chem. 2005 Mar 24;48(6):1697-700. doi: 10.1021/jm049676l.
J Med Chem. 2005.
PMID: 15771412
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Discovery of N-(Indazol-3-yl)piperidine-4-carboxylic Acids as RORγt Allosteric Inhibitors for Autoimmune Diseases.
Zhang H, Lapointe BT, Anthony N, Azevedo R, Cals J, Correll CC, Daniels M, Deshmukh S, van Eenenaam H, Ferguson H, Hegde LG, Karstens WJ, Maclean J, Miller JR, Moy LY, Simov V, Nagpal S, Oubrie A, Palte RL, Parthasarathy G, Sciammetta N, van der Stelt M, Woodhouse JD, Trotter BW, Barr K.
Zhang H, et al. Among authors: karstens wj.
ACS Med Chem Lett. 2020 Jan 9;11(2):114-119. doi: 10.1021/acsmedchemlett.9b00431. eCollection 2020 Feb 13.
ACS Med Chem Lett. 2020.
PMID: 32071676
Free PMC article.
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Complete inhibition of rhTSH-, Graves' disease IgG-, and M22-induced cAMP production in differentiated orbital fibroblasts by a low-molecular-weight TSHR antagonist.
van Zeijl CJ, van Koppen CJ, Surovtseva OV, de Gooyer ME, Plate R, Conti P, Karstens WJ, Timmers M, Saeed P, Wiersinga WM, Miltenburg AM, Fliers E, Boelen A.
van Zeijl CJ, et al. Among authors: karstens wj.
J Clin Endocrinol Metab. 2012 May;97(5):E781-5. doi: 10.1210/jc.2011-2931. Epub 2012 Mar 14.
J Clin Endocrinol Metab. 2012.
PMID: 22419705
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Mechanism of action of a nanomolar potent, allosteric antagonist of the thyroid-stimulating hormone receptor.
van Koppen CJ, de Gooyer ME, Karstens WJ, Plate R, Conti PG, van Achterberg TA, van Amstel MG, Brands JH, Wat J, Berg RJ, Lane JR, Miltenburg AM, Timmers CM.
van Koppen CJ, et al. Among authors: karstens wj.
Br J Pharmacol. 2012 Apr;165(7):2314-24. doi: 10.1111/j.1476-5381.2011.01709.x.
Br J Pharmacol. 2012.
PMID: 22014107
Free PMC article.
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Multidimensional profiling of CSF1R screening hits and inhibitors: assessing cellular activity, target residence time, and selectivity in a higher throughput way.
Uitdehaag JC, Sünnen CM, van Doornmalen AM, de Rouw N, Oubrie A, Azevedo R, Ziebell M, Nickbarg E, Karstens WJ, Ruygrok S.
Uitdehaag JC, et al. Among authors: karstens wj.
J Biomol Screen. 2011 Oct;16(9):1007-17. doi: 10.1177/1087057111418113. Epub 2011 Aug 26.
J Biomol Screen. 2011.
PMID: 21873591
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