Literature DB >> 24503274

Synthesis, [¹⁸F] radiolabeling, and evaluation of poly (ADP-ribose) polymerase-1 (PARP-1) inhibitors for in vivo imaging of PARP-1 using positron emission tomography.

Dong Zhou1, Wenhua Chu1, Jinbin Xu1, Lynne A Jones1, Xin Peng1, Shihong Li1, Delphine L Chen1, Robert H Mach2.   

Abstract

Imaging of poly (ADP-ribose) polymerase-1 (PARP-1) expression in vivo is a potentially powerful tool for developing PARP-1 inhibitors for drug discovery and patient care. We have synthesized several derivatives of benzimidazole carboxamide as PARP-1 inhibitors, which can be (18)F-labeled easily for positron emission tomographic (PET) imaging. Of the compounds synthesized, 12 had the highest inhibition potency for PARP-1 (IC50=6.3 nM). [(18)F]12 was synthesized under conventional conditions in high specific activity with 40-50% decay-corrected yield. MicroPET studies using [(18)F]12 in MDA-MB-436 tumor-bearing mice demonstrated accumulation of [(18)F]12 in the tumor that was blocked by olaparib, suggesting that the uptake of [(18)F]12 in the tumor is specific to PARP-1 expression.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Imaging; PARP-1; PET; Radiolabeling

Mesh：

Substances：

Year:  2014        PMID： 24503274      PMCID： PMC4020173          DOI： 10.1016/j.bmc.2014.01.019

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN： 0968-0896            Impact factor:   3.641


  30 in total

1.  The potential for poly (ADP-ribose) polymerase inhibitors in cancer therapy.

Authors:  M Javle; N J Curtin
Journal:  Ther Adv Med Oncol       Date:  2011-11       Impact factor: 8.168

2.  Highly efficient click labeling using 2-[¹⁸F]fluoroethyl azide and synthesis of an ¹⁸FN-hydroxysuccinimide ester as conjugation agent.

Authors:  Dong Zhou; Wenhua Chu; Carmen S Dence; Robert H Mach; Michael J Welch
Journal:  Nucl Med Biol       Date:  2012-07-04       Impact factor: 2.408

3.  The second zinc-finger domain of poly(ADP-ribose) polymerase determines specificity for single-stranded breaks in DNA.

Authors:  G Gradwohl; J M Ménissier de Murcia; M Molinete; F Simonin; M Koken; J H Hoeijmakers; G de Murcia
Journal:  Proc Natl Acad Sci U S A       Date:  1990-04       Impact factor: 11.205

Review 4.  Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.

Authors:  Dana V Ferraris
Journal:  J Med Chem       Date:  2010-06-24       Impact factor: 7.446

5.  Functions of poly(ADP-ribose) polymerase in controlling telomere length and chromosomal stability.

Authors:  F d'Adda di Fagagna; M P Hande; W M Tong; P M Lansdorp; Z Q Wang; S P Jackson
Journal:  Nat Genet       Date:  1999-09       Impact factor: 38.330

Review 6.  The diverse biological roles of mammalian PARPS, a small but powerful family of poly-ADP-ribose polymerases.

Authors:  Paul O Hassa; Michael O Hottiger
Journal:  Front Biosci       Date:  2008-01-01

7.  An enzymatic assay for poly(ADP-ribose) polymerase-1 (PARP-1) via the chemical quantitation of NAD(+): application to the high-throughput screening of small molecules as potential inhibitors.

Authors:  Karson S Putt; Paul J Hergenrother
Journal:  Anal Biochem       Date:  2004-03-01       Impact factor: 3.365

8.  Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.

Authors:  Donald J Skalitzky; Joseph T Marakovits; Karen A Maegley; Anne Ekker; Xiao-Hong Yu; Zdenek Hostomsky; Stephen E Webber; Brian W Eastman; Robert Almassy; Jianke Li; Nicola J Curtin; David R Newell; A Hilary Calvert; Roger J Griffin; Bernard T Golding
Journal:  J Med Chem       Date:  2003-01-16       Impact factor: 7.446

9.  The poly(ADP-ribose) polymerase inhibitor niraparib (MK4827) in BRCA mutation carriers and patients with sporadic cancer: a phase 1 dose-escalation trial.

Authors:  Shahneen K Sandhu; William R Schelman; George Wilding; Victor Moreno; Richard D Baird; Susana Miranda; Lucy Hylands; Ruth Riisnaes; Martin Forster; Aurelius Omlin; Nathan Kreischer; Khin Thway; Heidrun Gevensleben; Linda Sun; John Loughney; Manash Chatterjee; Carlo Toniatti; Christopher L Carpenter; Robert Iannone; Stan B Kaye; Johann S de Bono; Robert M Wenham
Journal:  Lancet Oncol       Date:  2013-06-28       Impact factor: 41.316

10.  Inhibitor-induced structural change of the active site of human poly(ADP-ribose) polymerase.

Authors:  Takayoshi Kinoshita; Isao Nakanishi; Masaichi Warizaya; Akinori Iwashita; Yoshiyuki Kido; Kouji Hattori; Takashi Fujii
Journal:  FEBS Lett       Date:  2004-01-02       Impact factor: 4.124
View more
  26 in total

1.  Preliminary evaluation of a novel 18F-labeled PARP-1 ligand for PET imaging of PARP-1 expression in prostate cancer.

Authors:  Dong Zhou; Jinbin Xu; Cedric Mpoy; Wenhua Chu; Sung Hoon Kim; Huifangjie Li; Buck E Rogers; John A Katzenellenbogen
Journal:  Nucl Med Biol       Date:  2018-08-24       Impact factor: 2.408

2.  A patient-derived-xenograft platform to study BRCA-deficient ovarian cancers.

Authors:  Erin George; Hyoung Kim; Clemens Krepler; Brandon Wenz; Mehran Makvandi; Janos L Tanyi; Eric Brown; Rugang Zhang; Patricia Brafford; Stephanie Jean; Robert H Mach; Yiling Lu; Gordon B Mills; Meenhard Herlyn; Mark Morgan; Xiaochen Zhang; Robert Soslow; Ronny Drapkin; Neil Johnson; Ying Zheng; George Cotsarelis; Katherine L Nathanson; Fiona Simpkins
Journal:  JCI Insight       Date:  2017-01-12

3.  Dual-Modality Optical/PET Imaging of PARP1 in Glioblastoma.

Authors:  Giuseppe Carlucci; Brandon Carney; Christian Brand; Susanne Kossatz; Christopher P Irwin; Sean D Carlin; Edmund J Keliher; Wolfgang Weber; Thomas Reiner
Journal:  Mol Imaging Biol       Date:  2015-12       Impact factor: 3.488

4.  PET of Poly (ADP-Ribose) Polymerase Activity in Cancer: Preclinical Assessment and First In-Human Studies.

Authors:  Loren S Michel; Samantha Dyroff; Frank J Brooks; Katherine J Spayd; Sora Lim; Jacquelyn T Engle; Sharon Phillips; Benjamin Tan; Andrea Wang-Gillam; Christopher Bognar; Wenhua Chu; Dong Zhou; Robert H Mach; Richard Laforest; Delphine L Chen
Journal:  Radiology       Date:  2016-11-14       Impact factor: 11.105

Review 5.  Molecular Imaging of PARP.

Authors:  Brandon Carney; Susanne Kossatz; Thomas Reiner
Journal:  J Nucl Med       Date:  2017-05-04       Impact factor: 10.057

6.  A PET imaging agent for evaluating PARP-1 expression in ovarian cancer.

Authors:  Mehran Makvandi; Austin Pantel; Lauren Schwartz; Erin Schubert; Kuiying Xu; Chia-Ju Hsieh; Catherine Hou; Hyoung Kim; Chi-Chang Weng; Harrison Winters; Robert Doot; Michael D Farwell; Daniel A Pryma; Roger A Greenberg; David A Mankoff; Fiona Simpkins; Robert H Mach; Lilie L Lin
Journal:  J Clin Invest       Date:  2018-04-16       Impact factor: 14.808

7.  The evolving landscape of predictive biomarkers of response to PARP inhibitors.

Authors:  Anish Thomas; Junko Murai; Yves Pommier
Journal:  J Clin Invest       Date:  2018-04-16       Impact factor: 14.808

8.  Non-invasive PET Imaging of PARP1 Expression in Glioblastoma Models.

Authors:  Brandon Carney; Giuseppe Carlucci; Beatriz Salinas; Valentina Di Gialleonardo; Susanne Kossatz; Axel Vansteene; Valerie A Longo; Alexander Bolaender; Gabriela Chiosis; Kayvan R Keshari; Wolfgang A Weber; Thomas Reiner
Journal:  Mol Imaging Biol       Date:  2016-06       Impact factor: 3.488

9.  [(18)F]FluorThanatrace uptake as a marker of PARP1 expression and activity in breast cancer.

Authors:  Christine E Edmonds; Mehran Makvandi; Brian P Lieberman; Kuiying Xu; Chenbo Zeng; Shihong Li; Catherine Hou; Hsiaoju Lee; Roger A Greenberg; David A Mankoff; Robert H Mach
Journal:  Am J Nucl Med Mol Imaging       Date:  2016-01-28

10.  A one-pot radiosynthesis of [18 F]PARPi.

Authors:  Thomas C Wilson; Nagavarakishore Pillarsetty; Thomas Reiner
Journal:  J Labelled Comp Radiopharm       Date:  2020-06-16       Impact factor: 1.921
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.