دورية أكاديمية
أعرض في EDS

Fluorescent small-molecule agonists as follicle-stimulating hormone receptor imaging tools.

التفاصيل البيبلوغرافية
العنوان: Fluorescent small-molecule agonists as follicle-stimulating hormone receptor imaging tools.
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.)
References: J Cell Biol. 1993 Dec;123(5):1107-17. (PMID: 8245121)
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1717-20. (PMID: 15026057)
IEEE Trans Image Process. 1995;4(3):370-8. (PMID: 18289986)
Proc Natl Acad Sci U S A. 1998 Nov 10;95(23):13612-7. (PMID: 9811848)
Cancer Res. 2009 Aug 15;69(16):6506-14. (PMID: 19638590)
Trends Biochem Sci. 2004 Mar;29(3):119-26. (PMID: 15003269)
J Exp Clin Cancer Res. 2015 Feb 05;34:12. (PMID: 25652007)
Pharmacol Ther. 2003 Nov;100(2):101-18. (PMID: 14609715)
Biochem J. 2004 Jan 1;377(Pt 1):159-69. (PMID: 14505488)
Nat Methods. 2007 Feb;4(2):153-9. (PMID: 17220893)
Bioorg Med Chem Lett. 2004 Apr 5;14(7):1713-6. (PMID: 15026056)
Virology. 2005 Jul 20;338(1):53-60. (PMID: 15936793)
Sci Rep. 2013;3:1365. (PMID: 23455567)
Chembiochem. 2008 Jul 21;9(11):1735-8. (PMID: 18600815)
J Med Chem. 2005 Mar 24;48(6):1697-700. (PMID: 15771412)
Cell. 1984 Aug;38(1):101-8. (PMID: 6432338)
Mol Cell Endocrinol. 1983 Nov;33(1):37-52. (PMID: 6315509)
Bioorg Med Chem. 2006 Aug 15;14(16):5729-41. (PMID: 16675221)
Mol Cell Endocrinol. 1984 Jan;34(1):39-49. (PMID: 6321274)
Endocr Rev. 1997 Dec;18(6):739-73. (PMID: 9408742)
N Engl J Med. 2010 Oct 21;363(17):1621-30. (PMID: 20961245)
J Comb Chem. 2004 Mar-Apr;6(2):196-206. (PMID: 15002967)
Front Endocrinol (Lausanne). 2018 Nov 02;9:653. (PMID: 30450081)
J Biotechnol Biomater. 2015 Sep;5(3):. (PMID: 26779384)
Science. 2017 May 26;356(6340):. (PMID: 28495876)
BMC Cancer. 2013 May 20;13:246. (PMID: 23688201)
ChemMedChem. 2009 Dec;4(12):2098-102. (PMID: 19902448)
Curr Opin Chem Biol. 2005 Oct;9(5):517-25. (PMID: 16125436)
J Neurosci. 2004 Apr 21;24(16):4070-81. (PMID: 15102922)
Annu Rev Biochem. 1981;50:465-95. (PMID: 6267989)
Bioconjug Chem. 1993 Mar-Apr;4(2):105-11. (PMID: 7873641)
J Biol Chem. 2002 Jun 14;277(24):21939-46. (PMID: 11934883)
Br J Cancer. 2003 Jan 13;88(1):146-52. (PMID: 12556974)
Br J Pharmacol. 2014 Mar;171(5):1073-84. (PMID: 23734587)
Mol Endocrinol. 2001 Jan;15(1):184-200. (PMID: 11145749)
Endocr Rev. 2000 Oct;21(5):551-83. (PMID: 11041448)
Physiol Rev. 2002 Apr;82(2):473-502. (PMID: 11917095)
Br J Pharmacol. 2010 Feb;159(4):772-86. (PMID: 20105183)
Biochem Pharmacol. 2013 Apr 15;85(8):1162-70. (PMID: 23415902)
Bioorg Med Chem. 2005 Nov 1;13(21):5986-95. (PMID: 16099664)
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
الوصف
تدمد:2633-0679
DOI:10.1039/d0cb00068j