دورية أكاديمية
Fluorescent small-molecule agonists as follicle-stimulating hormone receptor imaging tools.
العنوان: | Fluorescent small-molecule agonists as follicle-stimulating hormone receptor imaging tools. |
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المؤلفون: | Hoogendoorn S; Leiden Institute of Chemistry, Leiden University Einsteinweg 55 2300 RA Leiden The Netherlands Sascha.hoogendoorn@unige.ch h.s.overkleeft@lic.leidenuniv.nl., van Puijvelde GHM; Leiden Academic Centre for Drug Research, Leiden University Einsteinweg 55 2300 RA Leiden The Netherlands., van der Marel GA; Leiden Institute of Chemistry, Leiden University Einsteinweg 55 2300 RA Leiden The Netherlands Sascha.hoogendoorn@unige.ch h.s.overkleeft@lic.leidenuniv.nl., van Koppen CJ; ElexoPharm GmbH Im Stadtwald Building A1.2 66123 Saarbrücken Germany., Timmers CM; Byondis B.V. Microweg 22 6545 CM Nijmegen The Netherlands., Overkleeft HS; Leiden Institute of Chemistry, Leiden University Einsteinweg 55 2300 RA Leiden The Netherlands Sascha.hoogendoorn@unige.ch h.s.overkleeft@lic.leidenuniv.nl. |
المصدر: | RSC chemical biology [RSC Chem Biol] 2020 Aug 03; Vol. 1 (4), pp. 263-272. Date of Electronic Publication: 2020 Aug 03 (Print Publication: 2020). |
نوع المنشور: | Journal Article |
اللغة: | English |
بيانات الدورية: | Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101768727 Publication Model: eCollection Cited Medium: Internet ISSN: 2633-0679 (Electronic) Linking ISSN: 26330679 NLM ISO Abbreviation: RSC Chem Biol Subsets: PubMed not MEDLINE |
أسماء مطبوعة: | Original Publication: Cambridge : Royal Society of Chemistry, [2020]- |
مستخلص: | Fluorescent cell surface receptor agonists allow visualization of processes that are set in motion by receptor activation. This study describes the synthesis of two fluorescent, low molecular weight ligands for the follicle-stimulating hormone receptor (FSHR), based on a dihydropyridine (DHP) agonist. We show that both BODIPY- and Cy5-conjugated DHP ( m -DHP-BDP and m -DHP-Cy5) are potent FSHR agonists, able to activate receptor signalling with nanomolar potencies and to effect receptor internalisation at higher concentrations. FSHR-dependent uptake of m -DHP-Cy5 is in stark contrast to the cellular uptake of m -DHP-BDP which was efficiently internalised also in the absence of FSHR. Our results comprise a first-in-class fluorescent low molecular weight ligand for in situ FSHR imaging and pertain the potential means for targeted delivery of drugs into the endolysosomal pathway of FSHR-expressing cells. Competing Interests: CJvK and CMT were employees of MSD (Organon). (This journal is © The Royal Society of Chemistry.) |
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تواريخ الأحداث: | Date Created: 20210830 Latest Revision: 20210831 |
رمز التحديث: | 20240628 |
مُعرف محوري في PubMed: | PMC8341919 |
DOI: | 10.1039/d0cb00068j |
PMID: | 34458765 |
قاعدة البيانات: | MEDLINE |
تدمد: | 2633-0679 |
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DOI: | 10.1039/d0cb00068j |