Radiosynthesis and in vivo evaluation of a new positron emission tomography radiotracer targeting bromodomain and extra-terminal domain (BET) family proteins.

Brain / diagnostic imaging Isotope Labeling Kinetics Methylation Nuclear Proteins / chemistry Positron-Emission Tomography / methods Protein Domains Radioactive Tracers Radiochemistry
Bromodomain Epigenetic Imaging PET Radiotracer

Journal

Nuclear medicine and biology
ISSN: 1872-9614
Titre abrégé: Nucl Med Biol
Pays: United States
ID NLM: 9304420

Informations de publication

Date de publication:
Historique:
received: 22 01 2020
revised: 02 04 2020
accepted: 07 04 2020
pubmed: 23 4 2020
medline: 14 7 2021
entrez: 23 4 2020
Statut: ppublish

Résumé

Bromodomain and extra-terminal domain (BET) family proteins play a vital role in the epigenetic regulation process by interacting with acetylated lysine (Ac-K) residues in histones. BET inhibitors have become promising candidates to treat various diseases through the inhibition of the interaction between BET bromodomains and Ac-K of histone tails. With a molecular imaging probe, noninvasive imaging such as positron emission tomography (PET) can visualize the distribution and roles of BET family proteins in vivo and enlighten our understanding of BET protein function in both healthy and diseased tissue. We radiolabeled the potent BET inhibitor INCB054329 by N-methylation to make [ In our in vitro evaluation, PB003 showed a high BET binding affinity for BRDs (K The imaging results in rodents in vivo demonstrate that [

Identifiants

DOI: 10.1016/j.nucmedbio.2020.04.003 PMID: 32320910
pubmed: 32320910
pii: S0969-8051(20)30017-2
doi: 10.1016/j.nucmedbio.2020.04.003
pii:
doi:

Substances chimiques

Nuclear Proteins 0
Radioactive Tracers 0

Types de publication

Journal Article Research Support, N.I.H., Extramural Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

96-101

Subventions

Organisme : NIH HHS
ID : S10 OD023517
Pays : United States
Organisme : NINDS NIH HHS
ID : R01 NS108115
Pays : United States

Informations de copyright

Copyright © 2020 Elsevier Inc. All rights reserved.

Auteurs

Ping Bai (P)

Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, PR China; Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA; University of Chinese Academy of Sciences, Beijing 100049, PR China.

Xiaoxia Lu (X)

Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu 610041, PR China.

Yu Lan (Y)

Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA.

Zude Chen (Z)

Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA.

Debasis Patnaik (D)

Chemical Neurobiology Laboratory, Center for Genomic Medicine, Department of Neurology, Massachusetts General Hospital, Harvard Medical School, Boston, MA 02114, USA.

Stephanie Fiedler (S)

Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA.

Robin Striar (R)

Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA.

Stephen J Haggarty (SJ)

Chemical Neurobiology Laboratory, Center for Genomic Medicine, Department of Neurology, Massachusetts General Hospital, Harvard Medical School, Boston, MA 02114, USA.

Changning Wang (C)

Athinoula A. Martinos Center for Biomedical Imaging, Department of Radiology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA 02129, USA. Electronic address: cwang15@mgh.harvard.edu.

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Classifications MeSH

questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Techniques d'investigation › Marquage isotopique › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Cinétique › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Métabolisme › Alkylation › Méthylation › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines nucléaires › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Diagnostic › Techniques et procédures diagnostiques › Techniques de diagnostic radioisotopique › Scintigraphie › Tomoscintigraphie › Tomographie par émission de positons › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Conformation moléculaire › Conformation des protéines › Structure tertiaire des protéines › Domaines protéiques › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Actions chimiques et utilisations › Utilisations spécialisées de produits chimiques › Produits chimiques de laboratoire › Indicateurs et réactifs › Traceurs radioactifs › Radiosynthesis and in vivo evaluation of a new...
questionsmedicales.fr › Disciplines des sciences naturelles › Chimie › Chimie physique › Radiochimie › Radiosynthesis and in vivo evaluation of a new...