Literature DB >> 25923815

Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II.

Jan Tykvart1,2, Jiří Schimer1,2, Andrej Jančařík1, Jitka Bařinková1, Václav Navrátil1,2, Jana Starková1, Karolína Šrámková1, Jan Konvalinka1,2, Pavel Majer1, Pavel Šácha1,2.   

Abstract

We present here a structure-aided design of inhibitors targeting the active site as well as exosites of glutamate carboxypeptidase II (GCPII), a prostate cancer marker, preparing potent and selective inhibitors that are more than 1000-fold more active toward GCPII than its closest human homologue, glutamate carboxypeptidase III (GCPIII). Additionally, we demonstrate that the prepared inhibitor conjugate can be used for sensitive and selective imaging of GCPII in mammalian cells.

Entities:  

Mesh：

Substances：

Year:  2015        PMID： 25923815     DOI： 10.1021/acs.jmedchem.5b00278

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  8 in total

1.  2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics.

Authors:  Ryo Nakajima; Zora Nováková; Werner Tueckmantel; Lucia Motlová; Cyril Bařinka; Alan P Kozikowski
Journal:  ACS Med Chem Lett       Date:  2018-10-24       Impact factor: 4.345

Review 2.  Prostate-specific membrane antigen as a target for cancer imaging and therapy.

Authors:  A P Kiess; S R Banerjee; R C Mease; S P Rowe; A Rao; C A Foss; Y Chen; X Yang; S Y Cho; S Nimmagadda; M G Pomper
Journal:  Q J Nucl Med Mol Imaging       Date:  2015-07-24       Impact factor: 2.346

3.  Synthesis and pre-clinical evaluation of a new class of high-affinity 18F-labeled PSMA ligands for detection of prostate cancer by PET imaging.

Authors:  James Kelly; Alejandro Amor-Coarasa; Anastasia Nikolopoulou; Dohyun Kim; Clarence Williams; Shashikanth Ponnala; John W Babich
Journal:  Eur J Nucl Med Mol Imaging       Date:  2016-11-15       Impact factor: 9.236

4.  Modular Medical Imaging Agents Based on Azide-Alkyne Huisgen Cycloadditions: Synthesis and Pre-Clinical Evaluation of 18 F-Labeled PSMA-Tracers for Prostate Cancer Imaging.

Authors:  Verena I Böhmer; Wiktor Szymanski; Keimpe-Oeds van den Berg; Chantal Mulder; Piermichele Kobauri; Hugo Helbert; Dion van der Born; Friederike Reeβing; Anja Huizing; Marten Klopstra; Douwe F Samplonius; Ines F Antunes; Jürgen W A Sijbesma; Gert Luurtsema; Wijnand Helfrich; Ton J Visser; Ben L Feringa; Philip H Elsinga
Journal:  Chemistry       Date:  2020-07-21       Impact factor: 5.236

5.  Rational design of a sensitivity-enhanced tracer for discovering efficient APC-Asef inhibitors.

Authors:  Jie Zhong; Yuegui Guo; Shaoyong Lu; Kun Song; Ying Wang; Li Feng; Zhen Zheng; Qiufen Zhang; Jiacheng Wei; Peng Sang; Yan Shi; Jianfeng Cai; Guoqiang Chen; Chen-Ying Liu; Xiuyan Yang; Jian Zhang
Journal:  Nat Commun       Date:  2022-08-24       Impact factor: 17.694

6.  A Novel Prostate-Specific Membrane-Antigen (PSMA) Targeted Micelle-Encapsulating Wogonin Inhibits Prostate Cancer Cell Proliferation via Inducing Intrinsic Apoptotic Pathway.

Authors:  Hailong Zhang; Xiaogang Liu; Fengbo Wu; Feifei Qin; Ping Feng; Ting Xu; Xiang Li; Li Yang
Journal:  Int J Mol Sci       Date:  2016-05-17       Impact factor: 5.923

Review 7.  Metalloproteases Affecting Blood Coagulation, Fibrinolysis and Platelet Aggregation from Snake Venoms: Definition and Nomenclature of Interaction Sites.

Authors:  R Manjunatha Kini; Cho Yeow Koh
Journal:  Toxins (Basel)       Date:  2016-09-29       Impact factor: 4.546

8.  Mouse glutamate carboxypeptidase II (GCPII) has a similar enzyme activity and inhibition profile but a different tissue distribution to human GCPII.

Authors:  Tomáš Knedlík; Barbora Vorlová; Václav Navrátil; Jan Tykvart; František Sedlák; Šimon Vaculín; Miloslav Franěk; Pavel Šácha; Jan Konvalinka
Journal:  FEBS Open Bio       Date:  2017-08-29       Impact factor: 2.693
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.