Literature DB >> 25065587

Targeting thapsigargin towards tumors.

Nhu Thi Quynh Doan1, Eleonora Sandholdt Paulsen1, Pankaj Sehgal2, Jesper Vuust Møller2, Poul Nissen3, Samuel R Denmeade4, John T Isaacs4, Craig A Dionne5, Søren Brøgger Christensen6.   

Abstract

The skin irritating principle from Thapsia garganica was isolated, named thapsigargin and the structure elucidated. By inhibiting the sarco/endoplasmic reticulum Ca(2+) ATPase (SERCA) thapsigargin provokes apoptosis in almost all cells. By conjugating thapsigargin to peptides, which are only substrates for either prostate specific antigen (PSA) or prostate specific membrane antigen (PSMA) prodrugs were created, which selectively affect prostate cancer cells or neovascular tissue in tumors. One of the prodrug is currently tested in clinical phase II. The prodrug under clinical trial has been named mipsagargin.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Prodrug; Prostate specific antigen (PSA); Prostate specific membrane antigen (PSMA); Sarco/endoplasmic reticulum (SERCA); Targeting drugs; Thapsigargin

Mesh：

Substances：

Year:  2014        PMID： 25065587      PMCID： PMC4696022          DOI： 10.1016/j.steroids.2014.07.009

Source DB:  PubMed          Journal:  Steroids        ISSN： 0039-128X            Impact factor:   2.668


  29 in total

1.  Crystal structure of the calcium pump of sarcoplasmic reticulum at 2.6 A resolution.

Authors:  C Toyoshima; M Nakasako; H Nomura; H Ogawa
Journal:  Nature       Date:  2000-06-08       Impact factor: 49.962

2.  Tethered lipids from Thapsia garganica.

Authors:  Huizhen Liu; Carl Erik Olsen; S Brøgger Christensen
Journal:  J Nat Prod       Date:  2004-09       Impact factor: 4.050

3.  Total synthesis of two novel subpicomolar sarco/endoplasmatic reticulum Ca2+-ATPase inhibitors designed by an analysis of the binding site of thapsigargin.

Authors:  Helmer Søhoel; Tommy Liljefors; Steven V Ley; Steven F Oliver; Alessandra Antonello; Martin D Smith; Carl Erik Olsen; John T Isaacs; S Brøgger Christensen
Journal:  J Med Chem       Date:  2005-11-03       Impact factor: 7.446

4.  Thapsigargin, a histamine secretagogue, is a non-12-O-tetradecanoylphorbol-13-acetate (TPA) type tumor promoter in two-stage mouse skin carcinogenesis.

Authors:  H Hakii; H Fujiki; M Suganuma; M Nakayasu; T Tahira; T Sugimura; P J Scheuer; S B Christensen
Journal:  J Cancer Res Clin Oncol       Date:  1986       Impact factor: 4.553

Review 5.  Proteases as activators for cytotoxic prodrugs in antitumor therapy.

Authors:  Ulrich H Weidle; Georg Tiefenthaler; Guy Georges
Journal:  Cancer Genomics Proteomics       Date:  2014 Mar-Apr       Impact factor: 4.069

6.  Design, synthesis, and pharmacological evaluation of thapsigargin analogues for targeting apoptosis to prostatic cancer cells.

Authors:  C M Jakobsen; S R Denmeade; J T Isaacs; A Gady; C E Olsen; S B Christensen
Journal:  J Med Chem       Date:  2001-12-20       Impact factor: 7.446

7.  Thapsigargine and thapsigargicine, two new histamine liberators from Thapsia garganica L.

Authors:  U Rasmussen; S Brøogger Christensen; F Sandberg
Journal:  Acta Pharm Suec       Date:  1978

8.  Prostate-specific antigen-activated thapsigargin prodrug as targeted therapy for prostate cancer.

Authors:  Samuel R Denmeade; Carsten M Jakobsen; Samuel Janssen; Saeed R Khan; Elizabeth S Garrett; Hans Lilja; S Brogger Christensen; John T Isaacs
Journal:  J Natl Cancer Inst       Date:  2003-07-02       Impact factor: 13.506

9.  On the mechanism of histamine release induced by thapsigargin from Thapsia garganica L.

Authors:  S A Patkar; U Rasmussen; B Diamant
Journal:  Agents Actions       Date:  1979-04

10.  Differential effects of thapsigargin analogues on apoptosis of prostate cancer cells: complex regulation by intracellular calcium.

Authors:  Charlotte Dubois; Fabien Vanden Abeele; Pankaj Sehgal; Claus Olesen; Steffen Junker; Søren B Christensen; Natalia Prevarskaya; Jesper V Møller
Journal:  FEBS J       Date:  2013-09-02       Impact factor: 5.542
View more
  47 in total

1.  Structure/activity relationship of thapsigargin inhibition on the purified Golgi/secretory pathway Ca2+/Mn2+-transport ATPase (SPCA1a).

Authors:  Jialin Chen; Joren De Raeymaecker; Jannik Brøndsted Hovgaard; Susanne Smaardijk; Ilse Vandecaetsbeek; Frank Wuytack; Jesper Vuust Møller; Jan Eggermont; Marc De Maeyer; Søren Brøgger Christensen; Peter Vangheluwe
Journal:  J Biol Chem       Date:  2017-03-06       Impact factor: 5.157

Review 2.  Development of Anticancer Agents from Plant-Derived Sesquiterpene Lactones.

Authors:  Yulin Ren; Jianhua Yu; A Douglas Kinghorn
Journal:  Curr Med Chem       Date:  2016       Impact factor: 4.530

Review 3.  Ca2+ as a therapeutic target in cancer.

Authors:  Scott Gross; Pranava Mallu; Hinal Joshi; Bryant Schultz; Christina Go; Jonathan Soboloff
Journal:  Adv Cancer Res       Date:  2020-07-09       Impact factor: 6.242

Review 4.  SERCA control of cell death and survival.

Authors:  Elie R Chemaly; Luca Troncone; Djamel Lebeche
Journal:  Cell Calcium       Date:  2017-07-12       Impact factor: 6.817

5.  Direct detection of SERCA calcium transport and small-molecule inhibition in giant unilamellar vesicles.

Authors:  Tengfei Bian; Joseph M Autry; Denise Casemore; Ji Li; David D Thomas; Gaohong He; Chengguo Xing
Journal:  Biochem Biophys Res Commun       Date:  2016-11-01       Impact factor: 3.575

6.  The kinase PERK and the transcription factor ATF4 play distinct and essential roles in autophagy resulting from tunicamycin-induced ER stress.

Authors:  Morten Luhr; Maria Lyngaas Torgersen; Paula Szalai; Adnan Hashim; Andreas Brech; Judith Staerk; Nikolai Engedal
Journal:  J Biol Chem       Date:  2019-03-29       Impact factor: 5.157

7.  Blockade of Oncogenic NOTCH1 with the SERCA Inhibitor CAD204520 in T Cell Acute Lymphoblastic Leukemia.

Authors:  Matteo Marchesini; Andrea Gherli; Anna Montanaro; Laura Patrizi; Claudia Sorrentino; Luca Pagliaro; Chiara Rompietti; Samuel Kitara; Sabine Heit; Claus E Olesen; Jesper V Møller; Monia Savi; Leonardo Bocchi; Rocchina Vilella; Federica Rizzi; Marilena Baglione; Giorgia Rastelli; Caterina Loiacono; Roberta La Starza; Cristina Mecucci; Kimberly Stegmaier; Franco Aversa; Donatella Stilli; Anne-Marie Lund Winther; Paolo Sportoletti; Maike Bublitz; William Dalby-Brown; Giovanni Roti
Journal:  Cell Chem Biol       Date:  2020-05-07       Impact factor: 8.116

8.  Localization and in-Vivo Characterization of Thapsia garganica CYP76AE2 Indicates a Role in Thapsigargin Biosynthesis.

Authors:  Trine Bundgaard Andersen; Karen Agatha Martinez-Swatson; Silas Anselm Rasmussen; Berin Alain Boughton; Kirsten Jørgensen; Johan Andersen-Ranberg; Nils Nyberg; Søren Brøgger Christensen; Henrik Toft Simonsen
Journal:  Plant Physiol       Date:  2017-03-08       Impact factor: 8.340

9.  Protease-activated pore-forming peptides for the treatment and imaging of prostate cancer.

Authors:  Aaron M LeBeau; Samuel R Denmeade
Journal:  Mol Cancer Ther       Date:  2014-12-23       Impact factor: 6.261

Review 10.  Calcium-ATPases: Gene disorders and dysregulation in cancer.

Authors:  Donna Dang; Rajini Rao
Journal:  Biochim Biophys Acta       Date:  2015-11-30
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.