Autotaxin – A Target for the Treatment of Drug-Resistant Ovarian Cancer?

King-Underwood, John; Allin, Steven M.; Redman, C. W. E.; Richardson, Alan

doi:10.5772/27377

Cited by 2 publications

(4 citation statements)

References 106 publications

(97 reference statements)

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“…Then, 5 years later, the growth factor LPA (lysophosphatidic acid) was identified as the major ovarian 'cancer-activating agent' present in ascites fluid [17]. Autotaxin is a secreted phospholipase D that is responsible for the production of LPA from lysophosphatidylcholine and is also observed in ascites fluid [18,19]. Autotaxin is overexpressed in many cancer types, particularly in metastatic disease [18,20].…”

Section: Autotaxinmentioning

confidence: 99%

“…Autotaxin is a secreted phospholipase D that is responsible for the production of LPA from lysophosphatidylcholine and is also observed in ascites fluid [18,19]. Autotaxin is overexpressed in many cancer types, particularly in metastatic disease [18,20]. LPA and autotaxin have been shown to increase cell migration and invasion, contribute to a supportive microenvironment, and inhibit apoptosis.…”

Section: Autotaxinmentioning

confidence: 99%

“…Several LPA analogues have been identified as potent inhibitors of autotaxin, but may also bind LPA receptors [18]. Several LPA analogues have been identified as potent inhibitors of autotaxin, but may also bind LPA receptors [18].…”

Section: Autotaxinmentioning

confidence: 99%

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New strategies for the treatment of ovarian cancer

Robinson

Fisher

Stamelos

et al. 2014

Biochemical Society Transactions

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Ovarian cancer usually responds well to chemotherapy, but once the disease becomes resistant to chemotherapy, the treatment options available are inadequate. A number of strategies are currently undergoing clinical evaluation, among which angiogenesis and PARP [poly(ADP-ribose) polymerase] inhibitors appear promising. Pre-clinical studies have identified several potential new therapeutic strategies, and we review the potential for use of BH3 (Bcl-2 homology) mimetics, autotaxin inhibitors and statins to treat ovarian cancer.

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Section: Autotaxinmentioning

confidence: 99%

Section: Autotaxinmentioning

confidence: 99%

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New strategies for the treatment of ovarian cancer

Robinson

Fisher

Stamelos

et al. 2014

Biochemical Society Transactions

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“…13 Autotaxin is overexpressed in ovarian cancers that are resistant to chemotherapy, 14 and it has also been shown to delay apoptosis induced by carboplatin in ovarian cancer cells. 15 Together with the well-established role of LPA in ovarian cancer cell migration and invasion, 16 this suggests that inhibition of autotaxin has therapeutic potential in the treatment of ovarian cancer.…”

mentioning

confidence: 95%

Dendrimer Conjugate of [4-(Tetradecanoylamino)benzyl]phosphonic Acid (S32826) as an Autotaxin Inhibitor

Fisher

Hilton-Bolt

Edwards

et al. 2013

ACS Med. Chem. Lett.

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Autotaxin is an extracellular phospholipase D that catalyzes the hydrolysis of lysophosphatidyl choline (LPC) to bioactive lipid lysophosphatidic acid (LPA). LPA has been implicated in many pathological processes relevant to cancer, including cell migration and invasion, proliferation, and survival. The most potent autotaxin inhibitor described to date is the LPA analogue S32826 (IC 50 5.6 nM). S32826 and many other autotaxin inhibitors are notably lipophilic, creating a need to improve their physical properties. Polymers are becoming an increasingly useful tool in the delivery of drugs and have the potential to improve the properties of small molecules. Herein we report the synthesis of a S32826 dendrimer conjugate and its biological evaluation. The conjugate was found to inhibit autotaxin activity using two different substrates and to decrease the migration of an ovarian cancer cell line modified to overexpress autotaxin. Furthermore, the conjugate potentiated activation of caspase 3/7 induced by carboplatin.

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Autotaxin – A Target for the Treatment of Drug-Resistant Ovarian Cancer?

Cited by 2 publications

References 106 publications

New strategies for the treatment of ovarian cancer

New strategies for the treatment of ovarian cancer

Dendrimer Conjugate of [4-(Tetradecanoylamino)benzyl]phosphonic Acid (S32826) as an Autotaxin Inhibitor

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