A Biodistribution Study of the Radiolabeled Kv1.3-Blocking Peptide DOTA-HsTX1[R14A] Demonstrates Brain Uptake in a Mouse Model of Neuroinflammation.

Mice Animals Neuroinflammatory Diseases Tissue Distribution Lipopolysaccharides Gallium Radioisotopes / metabolism Mice, Inbred C57BL Peptides / chemistry Brain / diagnostic imaging Inflammation / metabolism Positron-Emission Tomography
HsTX1[R14A] Kv1.3 channels microglia neuroinflammation positron emission tomography (PET)

Journal

Molecular pharmaceutics
ISSN: 1543-8392
Titre abrégé: Mol Pharm
Pays: United States
ID NLM: 101197791

Informations de publication

Date de publication:
02 01 2023
Historique:
pubmed: 5 11 2022
medline: 4 1 2023
entrez: 4 11 2022
Statut: ppublish

Résumé

The voltage-gated potassium channel Kv1.3 regulates the pro-inflammatory function of microglia and is highly expressed in the post-mortem brains of individuals with Alzheimer's and Parkinson's diseases. HsTX1[R14A] is a selective and potent peptide inhibitor of the Kv1.3 channel (IC

Identifiants

DOI: 10.1021/acs.molpharmaceut.2c00614 PMID: 36331024
pubmed: 36331024
doi: 10.1021/acs.molpharmaceut.2c00614
doi:

Substances chimiques

1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid 1HTE449DGZ
Lipopolysaccharides 0
Gallium Radioisotopes 0
Peptides 0

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

255-266

Auteurs

Sanjeevini Babu Reddiar (SB)

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.
ORCID: 0000-0003-0550-1683

Michael de Veer (M)

Monash Biomedical Imaging, Monash University, Melbourne, Victoria 3800, Australia.

Brett M Paterson (BM)

Monash Biomedical Imaging, Monash University, Melbourne, Victoria 3800, Australia.
School of Chemistry, Monash University, Clayton, Victoria 3800, Australia.

Tara Sepehrizadeh (T)

Monash Biomedical Imaging, Monash University, Melbourne, Victoria 3800, Australia.

Dorothy C C Wai (DCC)

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.
ORCID: 0000-0002-3871-9980

Agota Csoti (A)

Department of Biophysics and Cell Biology, Faculty of Medicine, University of Debrecen, Debrecen 4010, Hungary.

Gyorgy Panyi (G)

Department of Biophysics and Cell Biology, Faculty of Medicine, University of Debrecen, Debrecen 4010, Hungary.

Joseph A Nicolazzo (JA)

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.
ORCID: 0000-0002-0983-7152

Raymond S Norton (RS)

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Victoria 3052, Australia.
ARC Centre for Fragment-Based Design, Monash University, Parkville, Victoria 3052, Australia.
ORCID: 0000-0001-8893-0584

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Eucaryotes › Animaux › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › États, signes et symptômes pathologiques › Processus pathologiques › Inflammation › Maladies neuro-inflammatoires › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Pharmacocinétique › Distribution tissulaire › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Facteurs biologiques › Toxines biologiques › Toxines bactériennes › Endotoxines › Lipopolysaccharides › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Produits chimiques inorganiques › Métaux › Métaux lourds › Gallium › Isotopes du gallium › Radio-isotopes du gallium › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée C57BL › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Acides aminés, peptides et protéines › Peptides › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Système nerveux › Système nerveux central › Encéphale › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › États, signes et symptômes pathologiques › Processus pathologiques › Inflammation › A Biodistribution Study of the Radiolabeled...
questionsmedicales.fr › Diagnostic › Techniques et procédures diagnostiques › Techniques de diagnostic radioisotopique › Scintigraphie › Tomoscintigraphie › Tomographie par émission de positons › A Biodistribution Study of the Radiolabeled...