Anyone used 3bp (3-bromopyruvate)?

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RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Fri May 19, 2017 09:25 PM

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RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Fri May 19, 2017 11:04 PM

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Calithera's share price has increased by 5 times since the start of this ------- year.

http://www.calithera.com/wp-content/uploads/2017/03/03.2017-

Not difficult to understand why when you consider that it has programs in triple negative breast, colorectal, RCC, just announced a deal to start up in lung and melanoma for CB-839. Metabolics attack such a fundamental component of cancer that potentially nearly any type might be within reach. 

Will be very interested in seeing what CB-839 and a pure anti-glycolytic might be able to achieve. Also love to see what happens with a strong inhibition of glycolysis alone.

RE: Anyone used 3bp (3-bromopyruvate)?

by dumbcritic on Sat May 20, 2017 04:52 PM

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On May 19, 2017 11:04 PM Jcancom wrote:

Calithera's share price has increased by 5 times since the start of this ------- year.

http://www.calithera.com/wp-content/uploads/2017/03/03.2017- Keystone-poster-Emberley-2017.pdf"" target="_blank" rel="nofollow">http://www.calithera.com/wp-content/uploads/2017/03/03.2017- target="_blank" rel="nofollow">http://www.calithera.com/wp-content/uploads/2017/03/03.2017-

Not difficult to understand why when you consider that it has programs in triple negative breast, colorectal, RCC, just announced a deal to start up in lung and melanoma for CB-839. Metabolics attack such a fundamental component of cancer that potentially nearly any type might be within reach. 

Will be very interested in seeing what CB-839 and a pure anti-glycolytic might be able to achieve. Also love to see what happens with a strong inhibition of glycolysis alone.

I hope they didn't drop their HKII inhibitor pipeline. If they haven't it would give them a wholly-owned combination regimen across multiple indications.

The novel prodrug of DON (JHU-083) had a synergistic effect with pd1 inhibitors just like CB-839. So this needs to be taken into a clinical trial.

Other amino acids need to be targeted as well https://www.nature.com/articles/ncomms15267 http://www.nature.com/nature/journal/v544/n7650/full/nature2

RE: Anyone used 3bp (3-bromopyruvate)?

by dumbcritic on Sat May 20, 2017 05:07 PM

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On May 19, 2017 9:25 PM Jcancom wrote:

Yet, more metabolic medicine.

http://ir.celgene.com/releasedetail.cfm?releaseid=1015105 "" target="_blank" rel="nofollow">http://ir.celgene.com/releasedetail.cfm?releaseid=1015105 " target="_blank" rel="nofollow">http://ir.celgene.com/releasedetail.cfm?releaseid=1015105

Agios are working with them on a IDH1m (Ivosidenib) and Pan-IDHm inhibitor (AG-881). Their 'next wave' programs (two and three) will be targeting other key enzymes in cancer metabolic pathways too.

RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sat May 20, 2017 08:33 PM

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Hey, you're right I thought I saw an HK-2 drug somewhere; now it has vanished. THAT would be a very very interesting combo to see what metabolics could do. On their presentations, CD-839 by itself does not look as though it is doing very much much, then they add in an mTOR and that pretty much stopped tumor growth for what seems forever. I would though like to see what happens as you said if they went right in their and targeted HK-2.

Stopping the HK-2 program was probably a corporate strategy move. With CB-839, looks like you will have all the friends that you could need.

This is all very exciting! Pharma has basically taken the insights gained from 3-BP and moved it all done to a nMolar drug that can be moved through rigorous trials. Wonder if any of them will be honest and fess up that this was Warburg all the way. You just have to look back to the complete absence of Warburg references before 2000 to know that this is true.

 

 

RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sun May 21, 2017 12:52 AM

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Don't understand. They go to the trouble and make a really good nM drug that looks very impressive and then a toxic drug is reformulated and it is even better and less toxic than CB-839. Why don't formulate CB-839 into NPs to make safer and more effective?

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5018752/pdf/pna

RE: Anyone used 3bp (3-bromopyruvate)?

by Jcancom on Sun May 21, 2017 02:44 AM

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I have a fondness for PMID:25579853. The idea is quite extreme, though it might possibly work. When I was reading it just now this popped out "Such evidence may explain why introduction of healthy mitochondria into cancer cell cytoplasm halts carcinogenesis".

Didn't a poster on our thread recently note that a phase 1 clinical trial has been published in which mitochondria are transfered to cells for therapeutic effect? 

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