Literature DB >> 25516790

Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.

Daniel J Buzard1, Sun Hee Kim1, Luis Lopez1, Andrew Kawasaki1, Xiuwen Zhu1, Jeanne Moody1, Lars Thoresen1, Imelda Calderon1, Brett Ullman1, Sangdon Han1, Juerg Lehmann1, Tawfik Gharbaoui1, Dipanjan Sengupta1, Lorene Calvano1, Antonio Garrido Montalban1, You-An Ma1, Carleton Sage1, Yinghong Gao1, Graeme Semple1, Jeff Edwards1, Jeremy Barden1, Michael Morgan1, Weichao Chen1, Khawja Usmani1, Chuan Chen1, Abu Sadeque1, Ronald J Christopher1, Jayant Thatte1, Lixia Fu1, Michelle Solomon1, David Mills1, Kevin Whelan1, Hussien Al-Shamma1, Joel Gatlin1, Minh Le1, Ibragim Gaidarov1, Todd Anthony1, David J Unett1, Anthony Blackburn1, Jaimie Rueter1, Scott Stirn1, Dominic P Behan1, Robert M Jones1.   

Abstract

APD334 was discovered as part of our internal effort to identify potent, centrally available, functional antagonists of the S1P1 receptor for use as next generation therapeutics for treating multiple sclerosis (MS) and other autoimmune diseases. APD334 is a potent functional antagonist of S1P1 and has a favorable PK/PD profile, producing robust lymphocyte lowering at relatively low plasma concentrations in several preclinical species. This new agent was efficacious in a mouse experimental autoimmune encephalomyelitis (EAE) model of MS and a rat collagen induced arthritis (CIA) model and was found to have appreciable central exposure.

Entities:  

Keywords:  APD334; FTY720; S1P1; Sphingosine-1-phosphate; fingolimod; gilenya

Year:  2014        PMID： 25516790      PMCID： PMC4265817          DOI： 10.1021/ml500389m

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


  21 in total

1.  Synthesis, stereochemical determination and biochemical characterization of the enantiomeric phosphate esters of the novel immunosuppressive agent FTY720.

Authors:  Jeffrey J Hale; Lin Yan; William E Neway; Richard Hajdu; James D Bergstrom; James A Milligan; Gan-Ju Shei; Gary L Chrebet; Rosemary A Thornton; Deborah Card; Mark Rosenbach; Suzanne Mandala
Journal:  Bioorg Med Chem       Date:  2004-09-15       Impact factor: 3.641

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.  A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya).

Authors:  Jerold Chun; Volker Brinkmann
Journal:  Discov Med       Date:  2011-09       Impact factor: 2.970

4.  Discovery of a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.

Authors:  Emmanuel H Demont; Sandra Arpino; Rino A Bit; Colin A Campbell; Nigel Deeks; Sapna Desai; Simon J Dowell; Pam Gaskin; James R J Gray; Lee A Harrison; Andrea Haynes; Tom D Heightman; Duncan S Holmes; Philip G Humphreys; Umesh Kumar; Mary A Morse; Greg J Osborne; Terry Panchal; Karen L Philpott; Simon Taylor; Robert Watson; Robert Willis; Jason Witherington
Journal:  J Med Chem       Date:  2011-09-09       Impact factor: 7.446

5.  Immunosuppressive and anti-angiogenic sphingosine 1-phosphate receptor-1 agonists induce ubiquitinylation and proteasomal degradation of the receptor.

Authors:  Myat Lin Oo; Shobha Thangada; Ming-Tao Wu; Catherine H Liu; Timothy L Macdonald; Kevin R Lynch; Chen-Yong Lin; Timothy Hla
Journal:  J Biol Chem       Date:  2007-01-21       Impact factor: 5.157

6.  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

Review 7.  Th17 cell, the new player of neuroinflammatory process in multiple sclerosis.

Authors:  F Jadidi-Niaragh; A Mirshafiey
Journal:  Scand J Immunol       Date:  2011-07       Impact factor: 3.487

8.  Sphingosine 1-phosphate (S1P) receptor agonists mediate pro-fibrotic responses in normal human lung fibroblasts via S1P2 and S1P3 receptors and Smad-independent signaling.

Authors:  Katrin Sobel; Katalin Menyhart; Nina Killer; Bérengère Renault; Yasmina Bauer; Rolf Studer; Beat Steiner; Martin H Bolli; Oliver Nayler; John Gatfield
Journal:  J Biol Chem       Date:  2013-04-15       Impact factor: 5.157

Review 9.  Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis.

Authors:  Jerold Chun; Hans-Peter Hartung
Journal:  Clin Neuropharmacol       Date:  2010 Mar-Apr       Impact factor: 1.592

10.  Sphingosine 1-phosphate receptor 5 mediates the immune quiescence of the human brain endothelial barrier.

Authors:  Ruben van Doorn; Melissa A Lopes Pinheiro; Gijs Kooij; Kim Lakeman; Bert van het Hof; Susanne M A van der Pol; Dirk Geerts; Jack van Horssen; Paul van der Valk; Elizabeth van der Kam; Eric Ronken; Arie Reijerkerk; Helga E de Vries
Journal:  J Neuroinflammation       Date:  2012-06-20       Impact factor: 8.322
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  9 in total

1.  Identification and Preclinical Pharmacology of BMS-986104: A Differentiated S1P1 Receptor Modulator in Clinical Trials.

Authors:  T G Murali Dhar; Hai-Yun Xiao; Jenny Xie; Lois D Lehman-McKeeman; Dauh-Rurng Wu; Marta Dabros; Xiaoxia Yang; Tracy L Taylor; Xia D Zhou; Elizabeth M Heimrich; Rochelle Thomas; Kim W McIntyre; Bethanne Warrack; Hong Shi; Paul C Levesque; Jia L Zhu; James Hennan; Praveen Balimane; Zheng Yang; Anthony M Marino; Georgia Cornelius; Celia J D'Arienzo; Arvind Mathur; Ding Ren Shen; Mary Ellen Cvijic; Luisa Salter-Cid; Joel C Barrish; Percy H Carter; Alaric J Dyckman
Journal:  ACS Med Chem Lett       Date:  2016-01-19       Impact factor: 4.345

Review 2.  Review article: the sphingosine 1 phosphate/sphingosine 1 phosphate receptor axis - a unique therapeutic target in inflammatory bowel disease.

Authors:  Jie Wang; Idan Goren; Bo Yang; Sinan Lin; Jiannan Li; Michael Elias; Claudio Fiocchi; Florian Rieder
Journal:  Aliment Pharmacol Ther       Date:  2021-12-21       Impact factor: 8.171

3.  Repurposing the Sphingosine-1-Phosphate Receptor Modulator Etrasimod as an Antibacterial Agent Against Gram-Positive Bacteria.

Authors:  Matej Zore; Shella Gilbert-Girard; Paola San-Martin-Galindo; Inés Reigada; Leena Hanski; Kirsi Savijoki; Adyary Fallarero; Jari Yli-Kauhaluoma; Jayendra Z Patel
Journal:  Front Microbiol       Date:  2022-06-06       Impact factor: 6.064

Review 4.  Sphingosine-1-Phosphate (S1P) and S1P Signaling Pathway: Therapeutic Targets in Autoimmunity and Inflammation.

Authors:  Hsing-Chuan Tsai; May H Han
Journal:  Drugs       Date:  2016-07       Impact factor: 9.546

Review 5.  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 6.  Frontiers in Drug Research and Development for Inflammatory Bowel Disease.

Authors:  Diego Currò; Daniela Pugliese; Alessandro Armuzzi
Journal:  Front Pharmacol       Date:  2017-06-23       Impact factor: 5.810

7.  Amiselimod (MT-1303), a novel sphingosine 1-phosphate receptor-1 functional antagonist, inhibits progress of chronic colitis induced by transfer of CD4+CD45RBhigh T cells.

Authors:  Kyoko Shimano; Yasuhiro Maeda; Hirotoshi Kataoka; Mikako Murase; Sachiko Mochizuki; Hiroyuki Utsumi; Koichi Oshita; Kunio Sugahara
Journal:  PLoS One       Date:  2019-12-05       Impact factor: 3.240

8.  A Functionally Defined In Vivo Astrocyte Population Identified by c-Fos Activation in a Mouse Model of Multiple Sclerosis Modulated by S1P Signaling: Immediate-Early Astrocytes (ieAstrocytes).

Authors:  Aran Groves; Yasuyuki Kihara; Deepa Jonnalagadda; Richard Rivera; Grace Kennedy; Mark Mayford; Jerold Chun
Journal:  eNeuro       Date:  2018-09-24

Review 9.  Emerging therapeutic options in inflammatory bowel disease.

Authors:  Jesus K Yamamoto-Furusho; Norma N Parra-Holguín
Journal:  World J Gastroenterol       Date:  2021-12-28       Impact factor: 5.742
  9 in total

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