To fingolimod and beyond: The rich pipeline of drug candidates that target S1P signaling.


:Sphingosine 1-phosphate (S1P) is an extracellular lipid signaling molecule that acts as a selective, high-affinity ligand for a family of five G protein-coupled receptors. This signaling system was first identified twenty years ago, and has since been shown to regulate a diverse range of physiological processes and disease states, such as cardiovascular development, immune function, hypoxic responses, and cancer. The therapeutic potential of targeting this system took center stage when it was demonstrated that the immune modulator, fingolimod (FTY720/Gilenya), exerts it lymphopenic effect by acting on S1P receptors, primarily on S1P receptor 1 (S1P1). In 2010, fingolimod became the first oral medication approved for the treatment of multiple sclerosis (MS). Since then, second-generation S1P receptor modulators have been under development in an effort to provide improved safety and efficacy profiles for MS, and to broaden their use to other autoimmune indications. Beyond the development of S1P1-modulators, there has been considerable effort in targeting other components of the S1P signaling pathway for the treatment of other diseases, such as cardiovascular disease, sepsis, and cancer. This manuscript provides an overview of the clinical and preclinical development of drugs targeting S1P signaling.


Pharmacol Res


Pharmacological research


Chew WS,Wang W,Herr DR




Has Abstract


2016-11-01 00:00:00




Pt A










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    journal_title:Pharmacological research

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    journal_title:Pharmacological research

    pub_type: 杂志文章


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    journal_title:Pharmacological research

    pub_type: 临床试验,杂志文章


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    pub_type: 杂志文章


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    journal_title:Pharmacological research

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    journal_title:Pharmacological research

    pub_type: 杂志文章,meta分析


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    journal_title:Pharmacological research

    pub_type: 杂志文章


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    pub_type: 杂志文章


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    journal_title:Pharmacological research

    pub_type: 杂志文章


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    pub_type: 杂志文章


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    journal_title:Pharmacological research

    pub_type: 杂志文章


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    journal_title:Pharmacological research

    pub_type: 杂志文章


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    更新日期:2010-04-01 00:00:00

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    journal_title:Pharmacological research

    pub_type: 杂志文章


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    更新日期:2002-01-01 00:00:00

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    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Salam OM,Nada SA,Arbid MS

    更新日期:2002-04-01 00:00:00

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    journal_title:Pharmacological research

    pub_type: 杂志文章


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    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Perugini C,Bagnati M,Cau C,Bordone R,Zoppis E,Paffoni P,Re R,Albano E,Bellomo G

    更新日期:2000-01-01 00:00:00

  • Endocannabinoids and cardiac contractile function: pathophysiological implications.

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    journal_title:Pharmacological research

    pub_type: 杂志文章,评审


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    更新日期:2009-08-01 00:00:00

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    journal_title:Pharmacological research

    pub_type: 杂志文章


    authors: Chen Y,Brooks MJ,Gieser L,Swaroop A,Palczewski K

    更新日期:2017-01-01 00:00:00

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    journal_title:Pharmacological research

    pub_type: 杂志文章


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  • Activity-based protein profiling of the human failing ischemic heart reveals alterations in hydrolase activities involving the endocannabinoid system.

    abstract:AIM:Acute myocardial infarction and subsequent post-infarction heart failure are among the leading causes of mortality worldwide. The endocannabinoid system has emerged as an important modulator of cardiovascular disease, however the role of endocannabinoid metabolic enzymes in heart failure is still elusive. Herein, w...

    journal_title:Pharmacological research

    pub_type: 杂志文章


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    更新日期:2020-01-01 00:00:00