Literature DB >> 31749907

Optimization of PDE3A Modulators for SLFN12-Dependent Cancer Cell Killing.

Timothy A Lewis1, Luc de Waal1,2, Xiaoyun Wu1,2, Willmen Youngsaye1, Antje Wengner3, Charlotte Kopitz3, Martin Lange3, Stefan Gradl3, Manuel Ellermann3, Philip Lienau3, Stuart L Schreiber1, Heidi Greulich1,2, Matthew Meyerson1,2.   

Abstract

6-(4-(Diethylamino)-3-nitrophenyl)-5-methyl-4,5-dihydropyridazin-3(2H)-one, or DNMDP, potently and selectively inhibits phosphodiesterases 3A and 3B (PDE3A and PDE3B) and kills cancer cells by inducing PDE3A/B interactions with SFLN12. The structure-activity relationship (SAR) of DNMDP analogs was evaluated using a phenotypic viability assay, resulting in several compounds with suitable pharmacokinetic properties for in vivo analysis. One of these compounds, BRD9500, was active in an SK-MEL-3 xenograft model of cancer.
Copyright © 2019 American Chemical Society.

Entities:  

Year:  2019        PMID： 31749907      PMCID： PMC6862344          DOI： 10.1021/acsmedchemlett.9b00360

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  12 in total

1.  Cardiotonic agents. 8. Selective inhibitors of adenosine 3',5'-cyclic phosphate phosphodiesterase III. Elaboration of a five-point model for positive inotropic activity.

Authors:  W H Moos; C C Humblet; I Sircar; C Rithner; R E Weishaar; J A Bristol; A T McPhail
Journal:  J Med Chem       Date:  1987-11       Impact factor: 7.446

2.  Estrogen-Related Hormones Induce Apoptosis by Stabilizing Schlafen-12 Protein Turnover.

Authors:  Dianrong Li; Jie Chen; Youwei Ai; Xiaoqiong Gu; Li Li; Di Che; Zhaodi Jiang; Lin Li; She Chen; Huangwei Huang; Jiawen Wang; Tao Cai; Yang Cao; Xiangbin Qi; Xiaodong Wang
Journal:  Mol Cell       Date:  2019-08-13       Impact factor: 17.970

3.  Copper-catalyzed direct amination of ortho-functionalized haloarenes with sodium azide as the amino source.

Authors:  Haibo Zhao; Hua Fu; Renzhong Qiao
Journal:  J Org Chem       Date:  2010-05-21       Impact factor: 4.354

4.  HL 725, an extremely potent inhibitor of platelet phosphodiesterase and induced platelet aggregation in vitro.

Authors:  D Ruppert; K U Weithmann
Journal:  Life Sci       Date:  1982-11-08       Impact factor: 5.037

Review 5.  Oxazolidinone structure-activity relationships leading to linezolid.

Authors:  Michael R Barbachyn; Charles W Ford
Journal:  Angew Chem Int Ed Engl       Date:  2003-05-09       Impact factor: 15.336

6.  The effects of levosimendan and OR-1896 on isolated hearts, myocyte-sized preparations and phosphodiesterase enzymes of the guinea pig.

Authors:  Szabolcs Szilágyi; Piero Pollesello; Jouko Levijoki; Petri Kaheinen; Heimo Haikala; István Edes; Zoltán Papp
Journal:  Eur J Pharmacol       Date:  2004-02-13       Impact factor: 4.432

7.  Targeting tumor cells based on Phosphodiesterase 3A expression.

Authors:  Madiha Nazir; Wojciech Senkowski; Frida Nyberg; Kristin Blom; Per-Henrik Edqvist; Malin Jarvius; Claes Andersson; Mats G Gustafsson; Peter Nygren; Rolf Larsson; Mårten Fryknäs
Journal:  Exp Cell Res       Date:  2017-10-26       Impact factor: 3.905

8.  Phosphodiesterase 3A: a new player in development of interstitial cells of Cajal and a prospective target in gastrointestinal stromal tumors (GIST).

Authors:  Pierre Vandenberghe; Perrine Hagué; Steven C Hockman; Vincent C Manganiello; Pieter Demetter; Christophe Erneux; Jean-Marie Vanderwinden
Journal:  Oncotarget       Date:  2017-06-20

9.  Expression and regulation of Schlafen (SLFN) family members in primary human monocytes, monocyte-derived dendritic cells and T cells.

Authors:  Alexander Puck; Regina Aigner; Madhura Modak; Petra Cejka; Dieter Blaas; Johannes Stöckl
Journal:  Results Immunol       Date:  2015-10-22

10.  Identification of cancer-cytotoxic modulators of PDE3A by predictive chemogenomics.

Authors:  Luc de Waal; Timothy A Lewis; Matthew G Rees; Aviad Tsherniak; Xiaoyun Wu; Peter S Choi; Lara Gechijian; Christina Hartigan; Patrick W Faloon; Mark J Hickey; Nicola Tolliday; Steven A Carr; Paul A Clemons; Benito Munoz; Bridget K Wagner; Alykhan F Shamji; Angela N Koehler; Monica Schenone; Alex B Burgin; Stuart L Schreiber; Heidi Greulich; Matthew Meyerson
Journal:  Nat Chem Biol       Date:  2015-12-14       Impact factor: 15.040
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  6 in total

Review 1.  Naturally derived indole alkaloids targeting regulated cell death (RCD) for cancer therapy: from molecular mechanisms to potential therapeutic targets.

Authors:  Rui Qin; Feng-Ming You; Qian Zhao; Xin Xie; Cheng Peng; Gu Zhan; Bo Han
Journal:  J Hematol Oncol       Date:  2022-09-14       Impact factor: 23.168

2.  Classification models and SAR analysis on CysLT1 receptor antagonists using machine learning algorithms.

Authors:  Hongzhao Wang; Zijian Qin; Aixia Yan
Journal:  Mol Divers       Date:  2021-02-03       Impact factor: 3.364

Review 3.  Structural, molecular, and functional insights into Schlafen proteins.

Authors:  Ukhyun Jo; Yves Pommier
Journal:  Exp Mol Med       Date:  2022-06-29       Impact factor: 12.153

4.  14-weeks combined exercise epigenetically modulated 118 genes of menopausal women with prediabetes.

Authors:  Natália Yumi Noronha; Guilherme da Silva Rodrigues; Isabella Harumi Yonehara Noma; Camila Fernanda Cunha Brandao; Karine Pereira Rodrigues; Alexandre Colello Bruno; Chanachai Sae-Lee; Lígia Moriguchi Watanabe; Marcela Augusta de Souza Pinhel; Isabelle Mello Schineider; Mariana Luciano de Almeida; Fernando Barbosa Júnior; Déborah Araújo Morais; Wellington Tavares de Sousa Júnior; Torsten Plösch; Carlos Roberto Bueno Junior; Carla Barbosa Nonino
Journal:  Front Endocrinol (Lausanne)       Date:  2022-08-15       Impact factor: 6.055

5.  Identifying Susceptibility Loci for Cutaneous Squamous Cell Carcinoma Using a Fast Sequence Kernel Association Test.

Authors:  Manyan Huang; Chen Lyu; Xin Li; Abrar A Qureshi; Jiali Han; Ming Li
Journal:  Front Genet       Date:  2021-05-10       Impact factor: 4.599

6.  Structure of PDE3A-SLFN12 complex reveals requirements for activation of SLFN12 RNase.

Authors:  Colin W Garvie; Xiaoyun Wu; Malvina Papanastasiou; Sooncheol Lee; James Fuller; Gavin R Schnitzler; Steven W Horner; Andrew Baker; Terry Zhang; James P Mullahoo; Lindsay Westlake; Stephanie H Hoyt; Marcus Toetzl; Matthew J Ranaghan; Luc de Waal; Joseph McGaunn; Bethany Kaplan; Federica Piccioni; Xiaoping Yang; Martin Lange; Adrian Tersteegen; Donald Raymond; Timothy A Lewis; Steven A Carr; Andrew D Cherniack; Christopher T Lemke; Matthew Meyerson; Heidi Greulich
Journal:  Nat Commun       Date:  2021-07-16       Impact factor: 14.919
  6 in total

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