Dear Makoto,

The following publications might be helpful:

1-

Fluorescent Bisphosphonate and Carboxyphosphonate Probes: A Versatile Imaging Toolkit for Applications in Bone Biology and Biomedicine

Shuting Sun†‡, Katarzyna M. Błażewska†§, Anastasia P. Kadina†, Boris A. Kashemirov†, Xuchen Duan⊥, James T. Triffitt⊥, James E. Dunford⊥, R. Graham G. Russell⊥, Frank H. Ebetino‡, Anke J. Roelofs#, Fraser P. Coxon#, Mark W. Lundy‡, and Charles E. McKenna*†

† Department of Chemistry, University of Southern California, Los Angeles, California 90089, United States

‡ BioVinc LLC, 6162 Bristol Parkway, Culver City, California 90230, United States

§ Faculty of Chemistry, Lodz University of Technology, Zeromskiego 116, 90-924 Lodz, Poland

⊥ Botnar Research Centre, Nuffield Department of Orthopaedics, Rheumatology and Musculoskeletal Sciences, University of Oxford, Nuffield Orthopaedic Centre, Oxford, OX3 7LD, United Kingdom

# Musculoskeletal Research Programme, Institute of Medical Sciences, University of Aberdeen, Aberdeen, AB25 2ZD, United Kingdom

Bioconjugate Chem., Article ASAP

DOI: 10.1021/acs.bioconjchem.5b00369

Publication Date (Web): December 8, 2015

A bone imaging toolkit of 21 fluorescent probes with variable spectroscopic properties, bone mineral binding affinities, and antiprenylation activities has been created, including a novel linking strategy. The linking chemistry allows attachment of a diverse selection of dyes fluorescent in the visible to near-infrared range to any of the three clinically important heterocyclic bisphosphonate bone drugs (risedronate, zoledronate, and minodronate or their analogues). The resultant suite of conjugates offers multiple options to “mix and match” parent drug structure, fluorescence emission wavelength, relative bone affinity, and presence or absence of antiprenylation activity, for bone-related imaging applications.

http://pubs.acs.org/doi/abs/10.1021/acs.bioconjchem.5b00369?journalCode=bcches

2-Chem Biol. Author manuscript; available in PMC 2015 Mar 20.

Published in final edited form as:

Chem Biol. 2014 Mar 20; 21(3): 345–356.

Published online 2014 Feb 20. doi:  10.1016/j.chembiol.2014.01.004

PMCID: PMC4074398

NIHMSID: NIHMS569726

Structure-guided design of fluorescent S-adenosylmethionine analogs for a high-throughput screen to target SAM-I riboswitch RNAs

Scott F. Hickey1,3 and Ming C. Hammond1,2,3

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The publisher's final edited version of this article is available at Chem Biol

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Summary

Many classes of S-adenosylmethionine (SAM)-binding RNAs and proteins are of interest as potential drug targets in diverse therapeutic areas, from infectious diseases to cancer. In the former case, the SAM-I riboswitch is an attractive target because this structured RNA element is found only in bacterial mRNAs and regulates multiple genes in several human pathogens. Here we describe the synthesis of stable and fluorescent analogs of SAM in which the fluorophore is introduced through a functionalizable linker to the ribose. A Cy5-labeled SAM analog was shown to bind several SAM-I riboswitches via in-line probing and fluorescence polarization (FP) assays, including one from Staphylococcus aureus that controls the expression of SAM synthetase in this organism. A fluorescent ligand displacement assay was developed and validated for high-throughput screening of compounds to target the SAM-I riboswitch class.

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4074398/

3- Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor

Luke S. Schembri†, Leigh A. Stoddart§, Stephen J. Briddon§, Barrie Kellam⊥, Meritxell Canals‡, Bim Graham*†, and Peter J. Scammells*†

†Medicinal Chemistry and ‡Drug Discovery Biology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia

§ Cell Signaling Research Group, School of Life Sciences, Queen’s Medical Centre, University of Nottingham, Nottingham NG7 2UH, U.K.

⊥ School of Pharmacy, Centre for Biomolecular Sciences, University of Nottingham, Nottingham NG7 2RD, U.K.

J. Med. Chem., 2015, 58 (24), pp 9754–9767

DOI: 10.1021/acs.jmedchem.5b01664

Publication Date (Web): December 3, 2015

Copyright © 2015 American Chemical Society

Fluorescently labeled ligands are useful pharmacological research tools for studying receptor localization, trafficking, and signaling processes via fluorescence imaging. They are also employed in fluorescent binding assays. This study is centered on the design, synthesis, and pharmacological evaluation of fluorescent probes for the opioid receptors, for which relatively few non-peptidic fluorescent probes currently exist. The known μ-opioid receptor (MOR) partial agonist, buprenorphine, was structurally elaborated to include an amidoalkylamine linker moiety that was coupled with a range of fluorophores to afford new fluorescent probes. All compounds proved to be selective MOR antagonists. Confocal fluorescence microscopy studies revealed that the probe incorporating a sulfonated cyanine-5 fluorophore was the most appropriate for imaging studies. This ligand was subsequently employed in an automated fluorescence-based competition binding assay, allowing the pKi values of several well-known opioid ligands to be determined. Thus, this new probe will prove useful in future studies of MOR receptor pharmacology.

http://pubs.acs.org/doi/abs/10.1021/acs.jmedchem.5b01664?journalCode=jmcmar

In addition, attached please find a review article which I think will be helpful too.

Front Chem. 2014; 2: 48.

Published online 2014 Jul 15. doi:  10.3389/fchem.2014.00048

PMCID: PMC4097105

Revisiting 30 years of biofunctionalization and surface chemistry of inorganic nanoparticles for nanomedicine

João Conde,1,*† Jorge T. Dias,2,† Valeria Grazú,2,* Maria Moros,2 Pedro V. Baptista,3 and Jesus M. de la Fuente2,4,5

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Abstract

In the last 30 years we have assisted to a massive advance of nanomaterials in material science. Nanomaterials and structures, in addition to their small size, have properties that differ from those of larger bulk materials, making them ideal for a host of novel applications. The spread of nanotechnology in the last years has been due to the improvement of synthesis and characterization methods on the nanoscale, a field rich in new physical phenomena and synthetic opportunities. In fact, the development of functional nanoparticles has progressed exponentially over the past two decades. This work aims to extensively review 30 years of different strategies of surface modification and functionalization of noble metal (gold) nanoparticles, magnetic nanocrystals and semiconductor nanoparticles, such as quantum dots. The aim of this review is not only to provide in-depth insights into the different biofunctionalization and characterization methods, but also to give an overview of possibilities and limitations of the available nanoparticles.

Keywords: biofunctionalization, chemistry surface, gold nanoparticles, magnetic nanoparticles, quantum dots

Hoping this will be helpful,

Rafik

Dear Rafik, 

Thank you very much for kindly introducing articles.  I will look into them.  

Makoto

Have you tried photobleaching?

Dear Ravi, Thank you for your advise.  I have  tried with some available light sources but found it unsuccessful.  I think a powerful laser is needed for photobleaching (I could not find appropriate laser source yet...).