Gleevec inhibits c-fms

[Guest guest]

I just found this abstract while surfing Pubmed. It seems that

Gleevec not only inhibits bcr/abl, c-kit and PDGF (which we always

knew), but now they've found that it also inhibits an enzyme called

c-fms which plays a role in breast cancer, ovarian cancer and

rheumatoid arthritis. Very interesting.

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http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?

cmd=Retrieve & db=pubmed & dopt=Abstract & list_uids=15917650 & query_hl=14 & i

tool=pubmed_docsum

Inhibition of c-fms by imatinib: expanding the spectrum of treatment.

Dewar AL, Zannettino AC, TP, Lyons AB.

Division of Haematology, Hanson Institute, Institute of Medical and

Veterinary Science, Adelaide, South Australia.

andrea.dewar@...

Imatinib is a selective protein tyrosine kinase inhibitor currently

used in the treatment of chronic myeloid leukaemia (CML). It

specifically suppresses the growth of bcr-abl expressing CML

progenitor cells by blocking the ATP-binding site of the kinase

domain of bcr-abl. Imatinib also inhibits the c-abl, platelet

derived growth factor receptor (PDGFR), abl-related gene and stem

cell factor receptor, c-kit, protein tyrosine kinases. It is through

inhibition of c-kit that imatinib is also used clinically in the

treatment of gastrointestinal stromal tumours. We have recently

demonstrated that imatinib also specifically targets the macrophage

colony stimulating factor receptor, c-fms, at therapeutic

concentrations. Although this finding has important implications

with regard to potential side effects in patients currently

receiving imatinib therapy, these results suggest that imatinib may

also be useful in the treatment of diseases where c-fms is

implicated. This includes breast and ovarian cancer and inflammatory

conditions such as rheumatoid arthritis. We also speculate that

imatinib may be used in diseases where bone destruction occurs due

to excessive osteoclast activity, such as in the haematologic

malignancy, multiple myeloma.

PMID: 15917650 [PubMed - in process]