Synthesis, Structure−Activity Relationships, and Biological Evaluation of Fatty Alcohol Phosphates as Lysophosphatidic Acid Receptor Ligands, Activators of PPARγ, and Inhibitors of Autotaxin†

Gangadhar G. Durgam; Tamas Virag; Michelle D. Walker; Ryoko Tsukahara; Satoshi Yasuda; Karoly Liliom; Laurens A. van Meeteren; Wouter H. Moolenaar; Nicole Wilke; Wolfgang Siess; Gabor Tigyi; Duane D. Miller

doi:10.1021/jm049609r

Synthesis, Structure−Activity Relationships, and Biological Evaluation of Fatty Alcohol Phosphates as Lysophosphatidic Acid Receptor Ligands, Activators of PPARγ, and Inhibitors of Autotaxin†

Journal of Medicinal Chemistry ◽

10.1021/jm049609r ◽

2005 ◽

Vol 48 (15) ◽

pp. 4919-4930 ◽

Cited By ~ 74

Author(s):

Gangadhar G. Durgam ◽

Tamas Virag ◽

Michelle D. Walker ◽

Ryoko Tsukahara ◽

Satoshi Yasuda ◽

...

Keyword(s):

Fatty Alcohol ◽

Lysophosphatidic Acid ◽

Biological Evaluation ◽

Receptor Ligands ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor ◽

Structure Activity Relationships ◽

Structure Activity

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Initial structure–activity relationships of lysophosphatidic acid receptor antagonists: discovery of a high-affinity LPA1/LPA3 receptor antagonist

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2004.03.076 ◽

2004 ◽

Vol 14 (11) ◽

pp. 2735-2740 ◽

Cited By ~ 42

Author(s):

Brian H. Heasley ◽

Renata Jarosz ◽

Kevin R. Lynch ◽

Timothy L. Macdonald

Keyword(s):

Receptor Antagonist ◽

Lysophosphatidic Acid ◽

Initial Structure ◽

Receptor Antagonists ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor ◽

Structure Activity Relationships ◽

High Affinity ◽

Structure Activity

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Studies on structure—Activity relationships of retinoic acid receptor ligands by means of molecular modeling

Vitamins & Hormones ◽

10.1016/s0083-6729(00)59007-4 ◽

2000 ◽

pp. 159-215 ◽

Cited By ~ 4

Author(s):

F. Bachmair ◽

R. Hoffmann ◽

G. Daxenbichler ◽

Th. Langew

Keyword(s):

Retinoic Acid ◽

Molecular Modeling ◽

Retinoic Acid Receptor ◽

Receptor Ligands ◽

Acid Receptor ◽

Structure Activity Relationships ◽

Structure Activity

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Bicyclic core estrogens as full antagonists: synthesis, biological evaluation and structure–activity relationships of estrogen receptor ligands based on bridged oxabicyclic core arylsulfonamides

Organic & Biomolecular Chemistry ◽

10.1039/c2ob26531a ◽

2012 ◽

Vol 10 (43) ◽

pp. 8692 ◽

Cited By ~ 21

Author(s):

Manghong Zhu ◽

Chen Zhang ◽

Jerome C. Nwachukwu ◽

Sathish Srinivasan ◽

Valerie Cavett ◽

...

Keyword(s):

Estrogen Receptor ◽

Biological Evaluation ◽

Receptor Ligands ◽

Structure Activity Relationships ◽

Structure Activity ◽

Estrogen Receptor Ligands

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Synthesis and pharmacological evaluation of second-generation phosphatidic acid derivatives as lysophosphatidic acid receptor ligands

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2005.10.031 ◽

2006 ◽

Vol 16 (3) ◽

pp. 633-640 ◽

Cited By ~ 40

Author(s):

Gangadhar G. Durgam ◽

Ryoko Tsukahara ◽

Natalia Makarova ◽

Michelle D. Walker ◽

Yuko Fujiwara ◽

...

Keyword(s):

Phosphatidic Acid ◽

Lysophosphatidic Acid ◽

Second Generation ◽

Receptor Ligands ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor ◽

Pharmacological Evaluation

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The Effect of ASP6432, a Novel Type 1 Lysophosphatidic Acid Receptor Antagonist, on Urethral Function and Prostate Cell Proliferation

10.26226/morressier.59b63e3fd462b8029238929e ◽

2017 ◽

Author(s):

Kazuyuki Sakamoto

Keyword(s):

Cell Proliferation ◽

Receptor Antagonist ◽

Lysophosphatidic Acid ◽

Prostate Cell ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor ◽

Urethral Function

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Faculty Opinions recommendation of The lysophosphatidic acid receptor LPA1 links pulmonary fibrosis to lung injury by mediating fibroblast recruitment and vascular leak.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.1103139.559129 ◽

2008 ◽

Author(s):

Michael Pillinger

Keyword(s):

Pulmonary Fibrosis ◽

Lung Injury ◽

Lysophosphatidic Acid ◽

Vascular Leak ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor

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Interaction of the SARS-COV2 Envelope Protein (E) with Lysophosphatidic Acid Receptor 1 (LPAR1) and Additional Human Proteins Involved in Inflammation, Immunity, ADP Ribosylation and Vesicular Transport

SSRN Electronic Journal ◽

10.2139/ssrn.3701791 ◽

2020 ◽

Author(s):

Girish Nallur

Keyword(s):

Lysophosphatidic Acid ◽

Envelope Protein ◽

Vesicular Transport ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor ◽

Adp Ribosylation ◽

Human Proteins

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A blocking peptide stabilizes lysophosphatidic acid receptor 1 and promotes lysophosphatidic acid‐induced cellular responses

Journal of Cellular Biochemistry ◽

10.1002/jcb.29919 ◽

2021 ◽

Author(s):

Sarah J Taleb ◽

Jianxin Wei ◽

Rachel K Mialki ◽

Su Dong ◽

Yanhui Li ◽

...

Keyword(s):

Lysophosphatidic Acid ◽

Cellular Responses ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor

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Synthesis and Biological Evaluation of 14-Alkoxymorphinans. 18.1N-Substituted 14-Phenylpropyloxymorphinan-6-ones with Unanticipated Agonist Properties: Extending the Scope of Common Structure−Activity Relationships

Journal of Medicinal Chemistry ◽

10.1021/jm021118o ◽

2003 ◽

Vol 46 (9) ◽

pp. 1758-1763 ◽

Cited By ~ 23

Author(s):

Elisabeth Greiner ◽

Mariana Spetea ◽

Roland Krassnig ◽

Falko Schüllner ◽

Mario Aceto ◽

...

Keyword(s):

Biological Evaluation ◽

Structure Activity Relationships ◽

Common Structure ◽

Structure Activity ◽

Synthesis And Biological Evaluation

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A lysophosphatidic acid receptor lacking the PDZ-binding domain is constitutively active and stimulates cell proliferation

Biochimica et Biophysica Acta (BBA) - Molecular Cell Research ◽

10.1016/j.bbamcr.2007.11.013 ◽

2008 ◽

Vol 1783 (5) ◽

pp. 748-759 ◽

Cited By ~ 51

Author(s):

Shinya Shano ◽

Kazuki Hatanaka ◽

Shinsuke Ninose ◽

Ryutaro Moriyama ◽

Toshifumi Tsujiuchi ◽

...

Keyword(s):

Cell Proliferation ◽

Lysophosphatidic Acid ◽

Binding Domain ◽

Acid Receptor ◽

Lysophosphatidic Acid Receptor ◽

Constitutively Active

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