Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents

Bioorganic & Medicinal Chemistry Letters
Hilary P BeckWang Shen

Abstract

The LPA(2) protein is overexpressed in many tumor cells. We report the optimization of a series of LPA(2) antagonists using calcium mobilization assay (aequorin assay) that led to the discovery of the first reported inhibitors selective for LPA(2). Key compounds were evaluated in vitro for inhibition of LPA(2) mediated Erk activation and proliferation of HCT-116 cells. These compounds could be used to evaluate the benefits of LPA(2) inhibition both in vitro and in vivo.

References

May 31, 2002·Pharmacological Reviews·Jerold ChunGabor Tigyi
Dec 28, 2002·Proceedings of the National Academy of Sciences of the United States of America·Thomas M McIntyreGlenn D Prestwich
Jun 21, 2003·The Journal of Organic Chemistry·Yong XuGlenn D Prestwich
Jul 5, 2003·Organic Letters·Danilo Zim, Stephen L Buchwald
Dec 13, 2003·The Journal of Biological Chemistry·Xianjun FangGordon B Mills
Jun 29, 2004·Laboratory Investigation; a Journal of Technical Methods and Pathology·Dai ShidaHirokazu Nagawa
Nov 13, 2004·Breast Cancer Research : BCR·Joji KitayamaHirokazu Nagawa
Apr 20, 2005·Proceedings of the National Academy of Sciences of the United States of America·Ming YangSongzhu An
Dec 15, 2005·Journal of Surgical Oncology·Hiroharu YamashitaHirokazu Nagawa
Jul 29, 2006·The Journal of Organic Chemistry·Honglu ZhangGlenn D Prestwich

❮ Previous
Next ❯

Citations

May 23, 2009·Nature Reviews. Cancer·Robert C BastGordon B Mills
Nov 2, 2013·Future Medicinal Chemistry·David C Budd, Yimin Qian
Aug 26, 2010·British Journal of Pharmacology·Gabor Tigyi
Apr 7, 2012·Journal of Oncology·Valentina Grossi, Cristiano Simone
Feb 24, 2015·Progress in Lipid Research·Sabin Llona-MinguezThomas Helleday
Mar 20, 2014·Journal of Lipid Research·Yun C YungJerold Chun
Jan 17, 2015·Biomolecules & Therapeutics·Nicole C Stoddard, Jerold Chun
May 14, 2020·Cancers·Sue Chin LeeGábor J Tigyi
Jan 27, 2016·Chembiochem : a European Journal of Chemical Biology·Elisabeth Von HaeftenMarc Nazare
Jun 15, 2021·European Journal of Medicinal Chemistry·Bhagyalalitha MeduriBijo Mathew
Jul 25, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Alexander V AksenovMichael Rubin
Aug 28, 2021·Cells·Pravita BalijepalliKathryn E Meier

❮ Previous
Next ❯

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.