Fluorogenic Trp(redBODIPY) cyclopeptide targeting keratin 1 for imaging of aggressive carcinomas

Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and preparation of the first Trp-based red fluorogenic amino acid, which is synthetically accessible in a few steps and displays excellent photophysical p...

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Vydáno v:Chemical science (Cambridge) Ročník 11; číslo 5; s. 1368 - 1374
Hlavní autoři: Subiros-Funosas, Ramon, Ho, Vivian Cheuk Lam, Barth, Nicole D, Mendive-Tapia, Lorena, Pappalardo, Morena, Barril, Xavier, Ma, Ruoyu, Zhang, Cheng-Bin, Qian, Bin-Zhi, Sintes, Miquel, Ghashghaei, Ouldouz, Lavilla, Rodolfo, Vendrell, Marc
Médium: Journal Article
Jazyk:angličtina
Vydáno: CAMBRIDGE Royal Soc Chemistry 2020
Royal Society of Chemistry
The Royal Society of Chemistry
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ISSN:2041-6520, 2041-6539
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Abstract Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and preparation of the first Trp-based red fluorogenic amino acid, which is synthetically accessible in a few steps and displays excellent photophysical properties, and its application in a minimally-disruptive labelling strategy to prepare a new fluorogenic cyclopeptide for imaging of KRT1+ cells in whole intact tumour tissues. Trp(redBODIPY) is the first red-emitting Trp-based amino acid for the preparation of fluorogenic peptides with retention of target binding affinity.
AbstractList Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and preparation of the first Trp-based red fluorogenic amino acid, which is synthetically accessible in a few steps and displays excellent photophysical properties, and its application in a minimally-disruptive labelling strategy to prepare a new fluorogenic cyclopeptide for imaging of KRT1+ cells in whole intact tumour tissues.
Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and preparation of the first Trp-based red fluorogenic amino acid, which is synthetically accessible in a few steps and displays excellent photophysical properties, and its application in a minimally-disruptive labelling strategy to prepare a new fluorogenic cyclopeptide for imaging of KRT1+ cells in whole intact tumour tissues. Trp(redBODIPY) is the first red-emitting Trp-based amino acid for the preparation of fluorogenic peptides with retention of target binding affinity.
Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and preparation of the first Trp-based red fluorogenic amino acid, which is synthetically accessible in a few steps and displays excellent photophysical properties, and its application in a minimally-disruptive labelling strategy to prepare a new fluorogenic cyclopeptide for imaging of KRT1+ cells in whole intact tumour tissues. Trp(redBODIPY) is the first red-emitting Trp-based amino acid for the preparation of fluorogenic peptides with retention of target binding affinity.
Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and preparation of the first Trp-based red fluorogenic amino acid, which is synthetically accessible in a few steps and displays excellent photophysical properties, and its application in a minimally-disruptive labelling strategy to prepare a new fluorogenic cyclopeptide for imaging of KRT1+ cells in whole intact tumour tissues.Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and preparation of the first Trp-based red fluorogenic amino acid, which is synthetically accessible in a few steps and displays excellent photophysical properties, and its application in a minimally-disruptive labelling strategy to prepare a new fluorogenic cyclopeptide for imaging of KRT1+ cells in whole intact tumour tissues.
Author Qian, Bin-Zhi
Barril, Xavier
Barth, Nicole D
Ma, Ruoyu
Lavilla, Rodolfo
Subiros-Funosas, Ramon
Zhang, Cheng-Bin
Sintes, Miquel
Ghashghaei, Ouldouz
Ho, Vivian Cheuk Lam
Mendive-Tapia, Lorena
Pappalardo, Morena
Vendrell, Marc
AuthorAffiliation Facultat de Farmàcia
University of Barcelona and Institut de Biomedicina de la Universitat de Barcelona (IBUB)
University of Edinburgh
Centre for Inflammation Research
Laboratory of Physical Chemistry
Universitat de Barcelona and Institut de Biomedicina de la Universitat de Barcelona (IBUB)
Faculty of Pharmacy
Laboratory of Medicinal Chemistry
MRC Centre for Reproductive Health
AuthorAffiliation_xml – name: MRC Centre for Reproductive Health
– name: Laboratory of Medicinal Chemistry
– name: University of Edinburgh
– name: Centre for Inflammation Research
– name: Faculty of Pharmacy
– name: Facultat de Farmàcia
– name: Laboratory of Physical Chemistry
– name: Universitat de Barcelona and Institut de Biomedicina de la Universitat de Barcelona (IBUB)
– name: University of Barcelona and Institut de Biomedicina de la Universitat de Barcelona (IBUB)
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/34123261$$D View this record in MEDLINE/PubMed
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Issue 5
Keywords BREAST-CANCER
TRYPTOPHAN
AMINO-ACID
FLUORESCENT-PROBE
PEPTIDE
RAY CRYSTAL-STRUCTURE
Language English
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Snippet Keratin 1 (KRT1) is overexpressed in squamous carcinomas and associated with aggressive pathologies in breast cancer. Herein we report the design and...
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SubjectTerms Chemistry
Chemistry, Multidisciplinary
Keratin
Organic chemistry
Physical Sciences
Science & Technology
Title Fluorogenic Trp(redBODIPY) cyclopeptide targeting keratin 1 for imaging of aggressive carcinomas
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