Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate (Q33598799)

28 July 2017

title

Discovery of a Selective S1P1 Receptor Agonist Efficacious at Low Oral Dose and Devoid of Effects on Heart Rate (English)

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28 July 2017

Simon J Dowell

8

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Duncan S Holmes

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object named as

Duncan S Holmes

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28 July 2017

Emmanuel H Demont

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Benjamin I Andrews

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Rino A Bit

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Colin A Campbell

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Jason W B Cooke

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Nigel Deeks

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Sapna Desai

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Pam Gaskin

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James R J Gray

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Andrea Haynes

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Umesh Kumar

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Mary A Morse

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Greg J Osborne

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Terry Panchal

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Bela Patel

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Alcide Perboni

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Simon Taylor

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Robert Watson

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Jason Witherington

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Robert Willis

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28 July 2017

publication date

24 March 2011

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ACS Medicinal Chemistry Letters

28 July 2017

published in

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28 July 2017

volume

2

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issue

6

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28 July 2017

page(s)

444-449

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Lead- and drug-like compounds: the rule-of-five revolution

28 July 2017

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Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS

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2-imino-thiazolidin-4-one derivatives as potent, orally active S1P1 receptor agonists.

21 June 2018

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Removal of sphingosine 1-phosphate receptor-3 (S1P(3)) agonism is essential, but inadequate to obtain immunomodulating 2-aminopropane-1,3-diol S1P(1) agonists with reduced effect on heart rate

21 June 2018

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21 June 2018

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Full pharmacological efficacy of a novel S1P1 agonist that does not require S1P-like headgroup interactions

21 June 2018

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21 June 2018

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21 June 2018

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21 June 2018

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21 June 2018

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Oral fingolimod (FTY720) for relapsing multiple sclerosis

21 June 2018

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A rational utilization of high-throughput screening affords selective, orally bioavailable 1-benzyl-3-carboxyazetidine sphingosine-1-phosphate-1 receptor agonists

21 June 2018

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Lymphocyte egress from thymus and peripheral lymphoid organs is dependent on S1P receptor 1

21 June 2018

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Phosphorylation of the immunomodulatory drug FTY720 by sphingosine kinases

21 June 2018

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A comparison of physiochemical property profiles of development and marketed oral drugs

21 June 2018

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21 June 2018

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Molecular properties that influence the oral bioavailability of drug candidates

21 June 2018

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21 June 2018

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21 June 2018

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SAR studies of 3-arylpropionic acids as potent and selective agonists of sphingosine-1-phosphate receptor-1 (S1P1) with enhanced pharmacokinetic properties.

30 October 2018

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Sphingosine 1-phosphate type 1 receptor agonism inhibits transendothelial migration of medullary T cells to lymphatic sinuses

30 October 2018

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Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer

30 October 2018

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KRP-203, a novel synthetic immunosuppressant, prolongs graft survival and attenuates chronic rejection in rat skin and heart allografts

30 October 2018

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Selecting against S1P3 enhances the acute cardiovascular tolerability of 3-(N-benzyl)aminopropylphosphonic acid S1P receptor agonists

30 October 2018

1 reference

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Immune cell regulation and cardiovascular effects of sphingosine 1-phosphate receptor agonists in rodents are mediated via distinct receptor subtypes.

30 October 2018

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

30 October 2018

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Chromatographic Hydrophobicity Index by Fast-Gradient RP-HPLC: A High-Throughput Alternative to log P/log D

30 October 2018

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PubMed

https://pubmed.ncbi.nlm.nih.gov/24900328

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1021/ML2000214

1 reference

28 July 2017

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28 July 2017

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