Synthesis and Preclinical Evaluation of Radio-Iodinated GRPR/PSMA Bispecific Heterodimers for the Theranostics Application in Prostate Cancer.

GRPR PSMA bispecific heterodimers prostate cancer radio-iodine theranostics

Journal

Pharmaceutics
ISSN: 1999-4923
Titre abrégé: Pharmaceutics
Pays: Switzerland
ID NLM: 101534003

Informations de publication

Date de publication:
23 Jul 2019
Historique:
received: 15 06 2019
revised: 16 07 2019
accepted: 20 07 2019
entrez: 26 7 2019
pubmed: 26 7 2019
medline: 26 7 2019
Statut: epublish

Résumé

Gastrin-releasing peptide receptor (GRPR) and prostate-specific membrane antigen (PSMA) are overexpressed in most prostate cancers. GRPR expression is higher in early stages while PSMA expression increases with progression. The possibility of targeting both markers with a single theranostics radiotracer could improve patient management. Three GRPR/PSMA-targeting bispecific heterodimers (urea derivative PSMA-617 and bombesin-based antagonist RM26 linked via X-triazolyl-Tyr-PEG2, X = PEG2 (BO530), (CH

Identifiants

pubmed: 31340483
pii: pharmaceutics11070358
doi: 10.3390/pharmaceutics11070358
pmc: PMC6680768
pii:
doi:

Types de publication

Journal Article

Langues

eng

Subventions

Organisme : Cancerfonden
ID : 2017/425
Organisme : Cancerfonden
ID : CAN2015/350
Organisme : Vetenskapsrådet
ID : 2015-02509
Organisme : Cancerfonden
ID : CAN 2018/436
Organisme : Vetenskapsrådet
ID : 2015-02353

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Auteurs

Ayman Abouzayed (A)

Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden.

Cheng-Bin Yim (CB)

Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden.

Bogdan Mitran (B)

Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden.

Sara S Rinne (SS)

Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden.

Vladimir Tolmachev (V)

Department of Immunology, Genetics and Pathology, Uppsala University, 75183 Uppsala, Sweden.

Mats Larhed (M)

Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden.
Science for Life Laboratory, Uppsala University, 75183 Uppsala, Sweden.

Ulrika Rosenström (U)

Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden.

Anna Orlova (A)

Department of Medicinal Chemistry, Uppsala University, 75183 Uppsala, Sweden. anna.orlova@ilk.uu.se.
Science for Life Laboratory, Uppsala University, 75183 Uppsala, Sweden. anna.orlova@ilk.uu.se.

Classifications MeSH