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ESKM, a novel therapeutic agent for sensitive and resistant PH+ leukemias

The mechanism of resistance to JAK2 inhibitor in myeloproliferative neoplasms patients

Effects of PARP inhibitors in BRCA gene-mutated ovarian cancer

DASATINIB; An inhibitor of Receptor Tyrosine Kinase

GP130/JAK/STAT3 signaling pathway induces multiple myeloma

Copper dependent Cancer

Ras-Raf-MEK-ERK-other MAPKs pathway is becoming Wortmannin intriguing. Now, Donita C. Brady, Christopher M. Counter and et al (from Duke, Oxford and North Carolina) found that, with Copper, MEK1 phosphorylates ERK1/2 better.
And I am very happy to know another metal transporter: CTR1 (Cu transporter 1).
In college textbooks of my time, there was no copper. Na, K, Ca, Fe, Mg, Zn... played the roles.Cu is considered useless or even toxic. Nevertheless, AZD6244 no Cu-deficient diseases are published. (Wiki calls copper deficiency "very rare", and mostly occurs in "ruminant animals".)

Otherwisely, this report may mean: over-dosed copper may cause cancer (tumorigenesis) or cancer drug resistance (along with BRAF V600E mutation in this experiment).

Then, I am curious about the way scientists block copper-MEK binding or inhibit CTRs (we all postulate that there will be a series of Cu transporters.) EDTA/EGTA Cu mimics Computer-aided small molecule design And sometimes labor-intensive work will be most effective---namely, HTS, high throughput sceening (of CTR modulators). After all, a nice opportunity for pharmaceuticals.

 

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S2758 Wortmannin Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Wortmannin blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays. Wortmannin also inhibits PLK1 activity.

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