NDLI: Infrared-emitting, peptidase-resistant fluorescent ligands of the bradykinin B2 receptor: application to cytofluorometry and imaging

Content Provider	Springer Nature : BioMed Central
Author	Gera, Lajos Charest-Morin, Xavier Jean, Melissa Bachelard, Hélène Marceau, François
Abstract	Background We have previously reported the design, pharmacological properties and imaging application of bradykinin (BK) B2 receptor (B2R) ligands conjugated with fluorophores such as fluorescein derivatives at their N-terminus. To take advantage of the high penetration of infrared light into living tissues and their low autofluorescence in this region of the spectrum, additional probes conjugated with cyanine dye 7 (Cy7) were synthesized and characterized. Results The antagonist B-9430 (D-Arg-[Hyp3,Igl5,D-Igl7,Oic8]-BK) and the agonist B-9972 (D-Arg-[Hyp3,Igl5,Oic7,Igl8]-BK) were N-terminally extended with the infrared fluorophore Cy7, producing the peptides B-10665 and B-10666, respectively. Pharmacological studies indicated that the agonist B-10666 lost much affinity for the B2R vs. the parent peptide, whereas the antagonist B-10665 better retained its potency vs. B-9430 (competition of [3H]BK binding to human B2R, contractility of the human isolated umbilical vein for which potency losses were more important in each case). Both probes stained HEK 293 cells that expressed the B2R-green fluorescent protein (GFP) construction in a specific manner (confocal microscopy) and with very extensive co-localization of the green and infrared fluorescence in either case. The agonist B-10666 at 100 nM promoted the endocytosis of B2R-GFP in live cells, but not the antagonist version at 10–25 nM. The Cy7-labeled peptides did not label cells expressing the β2-adrenoceptor-GFP construction. B-10665 at low nanomolar concentrations was an effective probe for the recombinant B2Rs in cytofluorometry and macroscopic imaging of cell wells (IVIS imaging system operated for infrared fluorescence detection). Conclusions Despite a propensity for non-specific binding when used at high concentrations and limited sensitivity, Cy7-conjugated peptidase-resistant B2R ligands support original imaging and cytofluorometric applications.
Related Links	https://bmcresnotes.biomedcentral.com/counter/pdf/10.1186/s13104-016-2258-1.pdf
Ending Page	10
Page Count	10
Starting Page	1
File Format	HTM / HTML
ISSN	17560500
DOI	10.1186/s13104-016-2258-1
Journal	BMC Research Notes
Issue Number	1
Volume Number	9
Language	English
Publisher	BioMed Central
Publisher Date	2016-09-26
Access Restriction	Open
Subject Keyword	Biomedicine Medicine Public Health Life Sciences Bradykinin B2 receptors Fluorescence Cyanine dye 7 Human umbilical vein Microscopy Cytofluorometry Medicine/Public Health
Content Type	Text
Resource Type	Article
Subject	Biochemistry, Genetics and Molecular Biology Medicine
Journal Impact Factor	1.6/2023

Sl.	Authority	Responsibilities	Communication Details
1	Ministry of Education (GoI), Department of Higher Education	Sanctioning Authority	https://www.education.gov.in/ict-initiatives
2	Indian Institute of Technology Kharagpur	Host Institute of the Project: The host institute of the project is responsible for providing infrastructure support and hosting the project	https://www.iitkgp.ac.in
3	National Digital Library of India Office, Indian Institute of Technology Kharagpur	The administrative and infrastructural headquarters of the project	Dr. B. Sutradhar bsutra@ndl.gov.in
4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
5	Website/Portal (Helpdesk)	Queries regarding NDLI and its services	support@ndl.gov.in
6	Contents and Copyright Issues	Queries related to content curation and copyright issues	content@ndl.gov.in
7	National Digital Library of India Club (NDLI Club)	Queries related to NDLI Club formation, support, user awareness program, seminar/symposium, collaboration, social media, promotion, and outreach	clubsupport@ndl.gov.in
8	Digital Preservation Centre (DPC)	Assistance with digitizing and archiving copyright-free printed books	dpc@ndl.gov.in
9	IDR Setup or Support	Queries related to establishment and support of Institutional Digital Repository (IDR) and IDR workshops	idr@ndl.gov.in

Cucurbit[7]uril Complexation of Near-Infrared Fluorescent Azobenzene-Cyanine Conjugates

Design of fluorescent bradykinin analogs: application to imaging of B2 receptor-mediated agonist endocytosis and trafficking and angiotensin-converting enzyme.

Synthesis of a novel water-soluble near-infrared cyanine dye.

Pharmacological effects of recombinant human tissue kallikrein on bradykinin B 2 receptors

In Vitro Pharmacological Profile of a New Small Molecule Bradykinin B2 Receptor Antagonist

A Robust Bioassay of the Human Bradykinin $B_{2}$ Receptor That Extends Molecular and Cellular Studies: The Isolated Umbilical Vein

Near infrared fluorescent imaging of brain tumor with IR780 dye incorporated phospholipid nanoparticles

Fluorescent ligands of the bradykinin B1 receptors: pharmacologic characterization and application to the study of agonist-induced receptor translocation and cell surface receptor expression.

Modeling analysis of interactions of bradykinin b1 and b2 receptors with their endogenous ligands.

Infrared-emitting, peptidase-resistant fluorescent ligands of the bradykinin B2 receptor: application to cytofluorometry and imaging

Similar Documents

Cucurbit[7]uril Complexation of Near-Infrared Fluorescent Azobenzene-Cyanine Conjugates

Design of fluorescent bradykinin analogs: application to imaging of B2 receptor-mediated agonist endocytosis and trafficking and angiotensin-converting enzyme.

Synthesis of a novel water-soluble near-infrared cyanine dye.

Pharmacological effects of recombinant human tissue kallikrein on bradykinin B 2 receptors

In Vitro Pharmacological Profile of a New Small Molecule Bradykinin B2 Receptor Antagonist

A Robust Bioassay of the Human Bradykinin $B_{2}$ Receptor That Extends Molecular and Cellular Studies: The Isolated Umbilical Vein

Near infrared fluorescent imaging of brain tumor with IR780 dye incorporated phospholipid nanoparticles

Fluorescent ligands of the bradykinin B1 receptors: pharmacologic characterization and application to the study of agonist-induced receptor translocation and cell surface receptor expression.

Modeling analysis of interactions of bradykinin b1 and b2 receptors with their endogenous ligands.

Infrared-emitting, peptidase-resistant fluorescent ligands of the bradykinin B2 receptor: application to cytofluorometry and imaging