Literature DB >> 24360556

Structure-activity relationship studies and biological characterization of human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors.

Damien Y Duveau1, Adam Yasgar1, Yuhong Wang1, Xin Hu1, Jennifer Kouznetsova1, Kyle R Brimacombe1, Ajit Jadhav1, Anton Simeonov1, Craig J Thomas1, David J Maloney2.   

Abstract

The structure-activity relationship (SAR) study of two chemotypes identified as inhibitors of the human NAD(+)-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD, 15-PGDH) was conducted. Top compounds from both series displayed potent inhibition (IC50 <50 nM), demonstrate excellent selectivity towards HPGD and potently induce PGE2 production in A549 lung cancer and LNCaP prostate cancer cells. Published by Elsevier Ltd.

Entities:  

Keywords:  15-PGDH; HPGD; Inhibitor; PGE(2); Prostaglandin

Mesh：

Substances：

Year:  2013        PMID： 24360556      PMCID： PMC3970110          DOI： 10.1016/j.bmcl.2013.11.081

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  16 in total

1.  15-Hydroxyprostaglandin dehydrogenase associates with poor prognosis in breast cancer, induces epithelial-mesenchymal transition, and promotes cell migration in cultured breast cancer cells.

Authors:  Laura Lehtinen; Paula Vainio; Harriet Wikman; Johannes Reemts; Mika Hilvo; Rana Issa; Sirkku Pollari; Burkhard Brandt; Matej Oresic; Klaus Pantel; Olli Kallioniemi; Kristiina Iljin
Journal:  J Pathol       Date:  2012-01-17       Impact factor: 7.996

2.  Inhibition of NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (15-PGDH) by cyclooxygenase inhibitors and chemopreventive agents.

Authors:  H Cho; H-H Tai
Journal:  Prostaglandins Leukot Essent Fatty Acids       Date:  2002-12       Impact factor: 4.006

Review 3.  Prostaglandins and cancer.

Authors:  D Wang; R N Dubois
Journal:  Gut       Date:  2005-08-23       Impact factor: 23.059

4.  4,7-Dimethoxy-1,10-phenanthroline: an excellent ligand for the Cu-catalyzed N-arylation of imidazoles.

Authors:  Ryan A Altman; Stephen L Buchwald
Journal:  Org Lett       Date:  2006-06-22       Impact factor: 6.005

5.  15-deoxy-delta 12,14-prostaglandin J2 inhibits multiple steps in the NF-kappa B signaling pathway.

Authors:  D S Straus; G Pascual; M Li; J S Welch; M Ricote; C H Hsiang; L L Sengchanthalangsy; G Ghosh; C K Glass
Journal:  Proc Natl Acad Sci U S A       Date:  2000-04-25       Impact factor: 11.205

Review 6.  NAD+-linked 15-hydroxyprostaglandin dehydrogenase: structure and biological functions.

Authors:  H-H Tai; H Cho; M Tong; Y Ding
Journal:  Curr Pharm Des       Date:  2006       Impact factor: 3.116

7.  High-affinity inhibitors of human NAD-dependent 15-hydroxyprostaglandin dehydrogenase: mechanisms of inhibition and structure-activity relationships.

Authors:  Frank H Niesen; Lena Schultz; Ajit Jadhav; Chitra Bhatia; Kunde Guo; David J Maloney; Ewa S Pilka; Minghua Wang; Udo Oppermann; Tom D Heightman; Anton Simeonov
Journal:  PLoS One       Date:  2010-11-02       Impact factor: 3.240

8.  Accumulation of 15-deoxy-delta(12,14)-prostaglandin J2 adduct formation with Keap1 over time: effects on potency for intracellular antioxidant defence induction.

Authors:  Joo Yeun Oh; Niroshini Giles; Aimee Landar; Victor Darley-Usmar
Journal:  Biochem J       Date:  2008-04-15       Impact factor: 3.857

9.  Essential role for hematopoietic prostaglandin D2 synthase in the control of delayed type hypersensitivity.

Authors:  Seema G Trivedi; Justine Newson; Ravindra Rajakariar; Thomas S Jacques; Robert Hannon; Yoshihide Kanaoka; Naomi Eguchi; Paul Colville-Nash; Derek W Gilroy
Journal:  Proc Natl Acad Sci U S A       Date:  2006-03-17       Impact factor: 11.205

10.  Copper-catalyzed N-arylation of imidazoles and benzimidazoles.

Authors:  Ryan A Altman; Erica D Koval; Stephen L Buchwald
Journal:  J Org Chem       Date:  2007-07-11       Impact factor: 4.354
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  5 in total

1.  Discovery of NCT-501, a Potent and Selective Theophylline-Based Inhibitor of Aldehyde Dehydrogenase 1A1 (ALDH1A1).

Authors:  Shyh-Ming Yang; Adam Yasgar; Bettina Miller; Madhu Lal-Nag; Kyle Brimacombe; Xin Hu; Hongmao Sun; Amy Wang; Xin Xu; Kimloan Nguyen; Udo Oppermann; Marc Ferrer; Vasilis Vasiliou; Anton Simeonov; Ajit Jadhav; David J Maloney
Journal:  J Med Chem       Date:  2015-07-24       Impact factor: 7.446

2.  Inhibitors of 15-Prostaglandin Dehydrogenase To Potentiate Tissue Repair.

Authors:  Monika I Antczak; Yongyou Zhang; Changguang Wang; Jennifer Doran; Jacinth Naidoo; Sukesh Voruganti; Noelle S Williams; Sanford D Markowitz; Joseph M Ready
Journal:  J Med Chem       Date:  2017-04-25       Impact factor: 7.446

Review 3.  Avoiding Fluorescence Assay Interference-The Case for Diaphorase.

Authors:  Matthew D Hall; Anton Simeonov; Mindy I Davis
Journal:  Assay Drug Dev Technol       Date:  2016-04       Impact factor: 1.738

4.  A Single Nucleotide Polymorphism in HPGD Gene Is Associated with Prostate Cancer Risk.

Authors:  Xiaofei Qi; Yu Wang; Jianquan Hou; Yuhua Huang
Journal:  J Cancer       Date:  2017-10-24       Impact factor: 4.207

5.  Discovery of Orally Bioavailable, Quinoline-Based Aldehyde Dehydrogenase 1A1 (ALDH1A1) Inhibitors with Potent Cellular Activity.

Authors:  Shyh-Ming Yang; Natalia J Martinez; Adam Yasgar; Carina Danchik; Catrine Johansson; Yuhong Wang; Bolormaa Baljinnyam; Amy Q Wang; Xin Xu; Pranav Shah; Dorian Cheff; Xinran S Wang; Jacob Roth; Madhu Lal-Nag; James E Dunford; Udo Oppermann; Vasilis Vasiliou; Anton Simeonov; Ajit Jadhav; David J Maloney
Journal:  J Med Chem       Date:  2018-05-31       Impact factor: 7.446
  5 in total

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