Literature DB >> 24125884

Modulators of the Sphingosine 1-phosphate receptor 1.

Mariangela Urbano1, Miguel Guerrero, Hugh Rosen, Edward Roberts.   

Abstract

The Sphingosine 1-phosphate receptor (S1P-R) signaling system has proven to be of biological and medical importance in autoimmune settings. S1P1-R is a validated drug target for multiple sclerosis (MS) for which FTY720 (Fingolimod), a S1P1,3-5-R pan-agonist, was recently approved as the first orally active drug for the treatment of relapsing-remitting MS. Transient bradycardia and long half-life are the FTY720 critical pitfalls. This review provides the latest advances on next-generation S1P1-R modulators from 2012 up to date, with an overview of the chemical structures, structure-activity relationships, and relevant biological and clinical properties.
Copyright © 2013 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Autoimmune diseases; FTY720; S1P(1)-R agonists; S1P(1)-R antagonists

Mesh：

Substances：

Year:  2013        PMID： 24125884      PMCID： PMC3926431          DOI： 10.1016/j.bmcl.2013.09.058

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


  43 in total

Review 1.  Structural and functional characteristics of S1P receptors.

Authors:  Teresa Sanchez; Timothy Hla
Journal:  J Cell Biochem       Date:  2004-08-01       Impact factor: 4.429

2.  Fused tricyclic indoles as S1P₁ agonists with robust efficacy in animal models of autoimmune disease.

Authors:  Daniel J Buzard; Sangdon Han; Luis Lopez; Andrew Kawasaki; Jeanne Moody; Lars Thoresen; Brett Ullman; Juerg Lehmann; Imelda Calderon; Xiuwen Zhu; Tawfik Gharbaoui; Dipanjan Sengupta; Ashwin Krishnan; Yinghong Gao; Jeff Edwards; Jeremy Barden; Michael Morgan; Khawja Usmani; Chuan Chen; Abu Sadeque; Jayant Thatte; Michelle Solomon; Lixia Fu; Kevin Whelan; Ling Liu; Hussien Al-Shamma; Joel Gatlin; Minh Le; Charles Xing; Sheryll Espinola; Robert M Jones
Journal:  Bioorg Med Chem Lett       Date:  2012-05-07       Impact factor: 2.823

Review 3.  Fingolimod (FTY720): discovery and development of an oral drug to treat multiple sclerosis.

Authors:  Volker Brinkmann; Andreas Billich; Thomas Baumruker; Peter Heining; Robert Schmouder; Gordon Francis; Shreeram Aradhye; Pascale Burtin
Journal:  Nat Rev Drug Discov       Date:  2010-10-29       Impact factor: 84.694

4.  Discovery of a novel class of zwitterionic, potent, selective and orally active S1P₁ direct agonists.

Authors:  Nuria Aguilar; Marta Mir; Pedro M Grima; Manel López; Victor Segarra; Laia Esteban; Imma Moreno; Nuria Godessart; Gema Tarrasón; Teresa Domenech; Dolors Vilella; Clara Armengol; Mònica Córdoba; Mar Sabaté; Daniel Casals; Maria Domínguez
Journal:  Bioorg Med Chem Lett       Date:  2012-10-11       Impact factor: 2.823

5.  Discovery of thiadiazole amides as potent, S1P₃-sparing agonists of sphingosine-1-phosphate 1 (S1P₁) receptor.

Authors:  Heng Xu; Haibo Zhang; Linbo Luan; Yan Xu; Chengyong Li; Yonghui Wang; Fangbin Han; Ting Yang; Feng Ren; Jia-Ning Xiang; John D Elliott; Yonggang Zhao; Taylor B Guo; Hongtao Lu; Wei Zhang; David Hirst; Matthew Lindon; Xichen Lin
Journal:  Bioorg Med Chem Lett       Date:  2012-02-15       Impact factor: 2.823

Review 6.  International Union of Pharmacology. XXXIV. Lysophospholipid receptor nomenclature.

Authors:  Jerold Chun; Edward J Goetzl; Timothy Hla; Yasuyuki Igarashi; Kevin R Lynch; Wouter Moolenaar; Susan Pyne; Gabor Tigyi
Journal:  Pharmacol Rev       Date:  2002-06       Impact factor: 25.468

7.  Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.

Authors:  Shifeng Pan; Nathanael S Gray; Wenqi Gao; Yuan Mi; Yi Fan; Xing Wang; Tove Tuntland; Jianwei Che; Sophie Lefebvre; Yu Chen; Alan Chu; Klaus Hinterding; Anne Gardin; Peter End; Peter Heining; Christian Bruns; Nigel G Cooke; Barbara Nuesslein-Hildesheim
Journal:  ACS Med Chem Lett       Date:  2013-01-04       Impact factor: 4.345

8.  Synthesis and SAR of 1,3-thiazolyl thiophene and pyridine derivatives as potent, orally active and S1P₃-sparing S1P₁ agonists.

Authors:  Masayoshi Asano; Tsuyoshi Nakamura; Yukiko Sekiguchi; Yumiko Mizuno; Takahiro Yamaguchi; Kazuhiko Tamaki; Takaichi Shimozato; Hiromi Doi-Komuro; Takashi Kagari; Wataru Tomisato; Ryotaku Inoue; Hiroshi Yuita; Keiko Oguchi-Oshima; Reina Kaneko; Futoshi Nara; Yumi Kawase; Noriko Masubuchi; Shintaro Nakayama; Tetsufumi Koga; Eiko Namba; Hatsumi Nasu; Takahide Nishi
Journal:  Bioorg Med Chem Lett       Date:  2012-03-23       Impact factor: 2.823

9.  Pharmacokinetic/pharmacodynamic relationships of FTY720 in kidney transplant recipients.

Authors:  S I Park; C R Felipe; P G Machado; R Garcia; A Skerjanec; R Schmouder; H Tedesco-Silva; J O Medina-Pestana
Journal:  Braz J Med Biol Res       Date:  2005-05-25       Impact factor: 2.590

10.  Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate.

Authors:  M Germana Sanna; Jiayu Liao; Euijung Jo; Christopher Alfonso; Min-Young Ahn; Melissa S Peterson; Bill Webb; Sophie Lefebvre; Jerold Chun; Nathanael Gray; Hugh Rosen
Journal:  J Biol Chem       Date:  2004-01-19       Impact factor: 5.157
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  14 in total

1.  A practical process for the preparation of [(32)P]S1P and binding assay for S1P receptor ligands.

Authors:  Adam J Rosenberg; Hui Liu; Zhude Tu
Journal:  Appl Radiat Isot       Date:  2015-04-17       Impact factor: 1.513

Review 2.  Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.

Authors:  Stuart L Schreiber; Joanne D Kotz; Min Li; Jeffrey Aubé; Christopher P Austin; John C Reed; Hugh Rosen; E Lucile White; Larry A Sklar; Craig W Lindsley; Benjamin R Alexander; Joshua A Bittker; Paul A Clemons; Andrea de Souza; Michael A Foley; Michelle Palmer; Alykhan F Shamji; Mathias J Wawer; Owen McManus; Meng Wu; Beiyan Zou; Haibo Yu; Jennifer E Golden; Frank J Schoenen; Anton Simeonov; Ajit Jadhav; Michael R Jackson; Anthony B Pinkerton; Thomas D Y Chung; Patrick R Griffin; Benjamin F Cravatt; Peter S Hodder; William R Roush; Edward Roberts; Dong-Hoon Chung; Colleen B Jonsson; James W Noah; William E Severson; Subramaniam Ananthan; Bruce Edwards; Tudor I Oprea; P Jeffrey Conn; Corey R Hopkins; Michael R Wood; Shaun R Stauffer; Kyle A Emmitte
Journal:  Cell       Date:  2015-06-04       Impact factor: 41.582

Review 3.  Sphingosine 1-Phosphate Receptor Modulators for the Treatment of Multiple Sclerosis.

Authors:  Burhan Z Chaudhry; Jeffrey A Cohen; Devon S Conway
Journal:  Neurotherapeutics       Date:  2017-10       Impact factor: 7.620

4.  A Global Map of Lipid-Binding Proteins and Their Ligandability in Cells.

Authors:  Micah J Niphakis; Kenneth M Lum; Armand B Cognetta; Bruno E Correia; Taka-Aki Ichu; Jose Olucha; Steven J Brown; Soumajit Kundu; Fabiana Piscitelli; Hugh Rosen; Benjamin F Cravatt
Journal:  Cell       Date:  2015-06-18       Impact factor: 41.582

Review 5.  An Overview of the Efficacy and Safety of Ozanimod for the Treatment of Relapsing Multiple Sclerosis.

Authors:  Marzia Fronza; Lorena Lorefice; Jessica Frau; Eleonora Cocco
Journal:  Drug Des Devel Ther       Date:  2021-05-11       Impact factor: 4.162

Review 6.  Targeting Sphingosine-1-Phosphate Signaling in Immune-Mediated Diseases: Beyond Multiple Sclerosis.

Authors:  Tamara Pérez-Jeldres; Manuel Alvarez-Lobos; Jesús Rivera-Nieves
Journal:  Drugs       Date:  2021-05-13       Impact factor: 11.431

Review 7.  Sphingosine 1-phosphate Receptor Modulator Therapy for Multiple Sclerosis: Differential Downstream Receptor Signalling and Clinical Profile Effects.

Authors:  Jerold Chun; Gavin Giovannoni; Samuel F Hunter
Journal:  Drugs       Date:  2021-02       Impact factor: 9.546

8.  Discovery and characterization of novel small-molecule CXCR4 receptor agonists and antagonists.

Authors:  Rama K Mishra; Andrew K Shum; Leonidas C Platanias; Richard J Miller; Gary E Schiltz
Journal:  Sci Rep       Date:  2016-07-26       Impact factor: 4.379

Review 9.  Benefit-Risk Profile of Sphingosine-1-Phosphate Receptor Modulators in Relapsing and Secondary Progressive Multiple Sclerosis.

Authors:  Giancarlo Comi; Hans-Peter Hartung; Rajesh Bakshi; Ian M Williams; Heinz Wiendl
Journal:  Drugs       Date:  2017-10       Impact factor: 9.546

10.  Regulation of Immune Cell Migration by Sphingosine-1-Phosphate.

Authors:  A Kumar; J D Saba
Journal:  Cell Mol Biol (OMICS)       Date:  2015-12-31
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