Rapid cell growth and division, such as is seen in the
growth of aggressive tumours requires increased uptake of several
essential vitamins. Studies have shown that many cancer cell lines
over-express proteins involved in the uptake of folate, vitamin B12
Vitamin B12 targeting to cancer
Many rapidly dividing cells, such as cancers of the breast,
prostate, some leukaemias, and some kidney cell lines, actively accumulate
vitamin B12. Vitamin B12 exists within the cell as
two co-enzymes, methylcobalamin, which is involved in one carbon
synthesis, essential for DNA synthesis, and adenosylcobalamin, which is
involved in mitochondrial energy production within these highly
metabolically active cells. Tumours showing enhanced uptake of vitamin B12
are known to synthesize both vitamin B12 binding proteins, and
the binding protein receptors. Vitamin B12 has been found to be
suitable for imaging these cancers in humans and also as a targeting agent
for enhanced specificity of cytotoxins and polymer-bound cytotoxins.
Biotin targeting to cancer cells
Biotin is an essential vitamin, which is involved in cell
growth, fatty acid metabolism and energy production within the cell.
Recently, it has also been shown that biotin is required for biotinylation
Receptors involved in the uptake of biotin have been found to be
over-expressed on cancers of the breast, ovary, kidney, liver,
prostate, and some lung cell lines. Biotin has been found to be suitable
for imaging these cancers in humans and also as a targeting agent for
enhanced specificity of cytotoxins and polymer-bound cytotoxins. Recent
evidence suggests that uptake of biotin by these cells requires the
synthesis of both a biotin binding protein (most likely biotinidase, which
is then secreted), and a biotin binding protein receptor (which is
expressed on the cell surface).
Biotin-targeted fluorescent polymers have been shown to greatly enhance
the detection of small cancer masses and metastases.
staining of Small
Intestine and tumour
Biotin targeted Rhodamine-HPMA (red) successfully
identifies micro-metastases located adjacent to normal small intestinal
Vitamin-targeted delivery systems have been shown to
enhance cancer imaging and to increase the effectiveness and selectivity
of several cytotoxins
Mentor can provide expertise in the design, synthesis and scale-up of
targeted imaging agents and therapeutics for cancer therapy.
Mentor can provide expertise in the identification of potential
serum markers for cancer detection.