Drugs that Act as Inhibitors of NF-κB.

[pjoshea13]

No, I haven't joined the other side, but in a group this size a fair number would prefer a legitimate drug to a handful of polyphenols generally regarded as safe.

This paper [1] is from 2010.

"Constitutive activation of NF-κB signaling has been found in some types of tumors including breast, colon, prostate, skin and lymphoid, hence therapeutic blockade of NF-κB signaling in cancer cells provides an attractive strategy for the development of anticancer drugs."

The inhibition of NF-kB is the inhibition of scores of downstream proteins that are all induced for cell survival.

Recent posts have been concentrating on inflammation. Sub-clinical inflammation has an effect on survival - even in those who are supposedly healthy. Men with PCa have a poorer response to treatment when there is inflammation.

But NF-kB does a lot more than stimulate the production of COX/LOX enzymes, it really is a great target.

"To identify small molecule inhibitors of NF-κB signaling, we screened approximately 2,800 clinically approved drugs and bioactive compounds from the NIH Chemical Genomics Center Pharmaceutical Collection (NPC) in a NF-κB mediated β-lactamase reporter gene assay. Each compound was tested at fifteen different concentrations in a quantitative high throughput screening format. We identified nineteen drugs that inhibited NF-κB signaling, with potencies as low as 20 nM. Many of these drugs, including emetine, fluorosalan, sunitinib malate, bithionol, narasin, tribromsalan, and lestaurtinib, inhibited NF-κB signaling via inhibition of IκBα phosphorylation. Others, such as ectinascidin 743, chromomycin A3 and bortezomib utilized other mechanisms. Furthermore, many of these drugs induced caspase 3/7 activity and had an inhibitory effect on cervical cancer cell growth. Our results indicate that many currently approved pharmaceuticals have previously unappreciated effects on NF-κB signaling, which may contribute to anticancer therapeutic effects. Comprehensive profiling of approved drugs provides insight into their molecular mechanisms, thus providing a basis for drug repurposing."

It's a full text paper, with lots to interested those interested in a pharmaceutical solution.

-Patrick

[1] ncbi.nlm.nih.gov/pmc/articl...

[dbrooks_h]

Aleve for inflammation

[pjoshea13]

I wonder if any of the NSAIDs inhibit 5-LOX? -Patrick

[CalBear74]

For those who would like to know more about the significance of NF-Kappa b , Julius Goepp, MD has written this article for Life Extension's online health magazine:

lifeextension.com/Magazine/...

Many of you may be taking supplements that have been shown to inhibit NF-KB.

[PhilipSZacarias]

An excellent and useful paper. Thank you for posting. Cheers, Phil

[cesanon]

These are the Inhibitors of NF-κB that might possibly be able to be accessable for off label use:

Emetine is a drug used as both an anti-protozoal and to induce vomiting.

Sunitinib (marketed as Sutent by Pfizer, and previously known as SU11248) is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications

Bithionol is an anthelmintic used to treat Anoplocephala perfoliata (tapeworms) in horses[1] and Fasciola hepatica (liver flukes).

Narasin is a coccidiostat and antibacterial agent. It is a derivative of salinomycin with an additional methyl group

Trabectedin is an antitumor chemotherapy drug sold by Pharma Mar S.A. and Johnson and Johnson under the brand name Yondelis. It is approved for use in Europe, Russia, and South Korea for the treatment of advanced soft-tissue sarcoma.

Chromomycin A3 or Toyomycin is an anthraquinone antibiotic glycoside produced by the fermentation of a certain strain of Streptomyces griseus.

Bortezomib (BAN, INN and USAN; marketed as Velcade by Takeda Oncology; Chemobort by Cytogen and Bortecad by Cadila Healthcare) It is an anti-cancer drug and the first therapeutic proteasome inhibitor to be used in humans. It is approved in the U.S. and Europe for treating relapsed multiple myeloma and mantle cell lymphoma.