A recent paper i seen on JACS worth reading to know about some concepts in Chemistry-Biology interface. When i was working on a Nuerodegenarative diseases in Banglore for a Drug Discovery frim, we faced a potential problem exactly which is discussed in this current papper.
We had sucessfully screened a potent molecule for that diseases, but the problem of Blood Brain Barrier(BBB). It was indeed a large molecule with molecular weight > 400, it showed active resistance to pass the BBB. So finally 4 years work went into the rubbish bin.
Around 98% of the small molecules and 100% of the large molecules fail to became a drug because of their in ability to pass through BBB. The prescence of the HIV in the CNS and Cerebral fluid is the prime cause for no theraphy yet for AIDS, as the potent drugs fail to pass the BBB.
So bascically in this paper they have synthezised some BBB-Shuttles, which acts as cargo for the potent molecules to penetrate in the the brain.
The passive diffusion has been studied through (i) Parallel Artificial Membrane permeability Assay (PAMPA) and (ii) Immobalized Artificial Membrane Chromatography (IAMC).
A nice paper to read on. See the paper from more detailed information.
JACS, 2007, 129, 11802-11813.
Ahamed.
1 comment:
Good post.
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