IUBio

Can proteinase inhibitors penetrate the cell membrane?

Fergus Doherty Fergus.Doherty at nottingham.ac.uk
Tue Nov 16 12:05:30 EST 1999


In article <383175A8.3865DDA3 at uni-tuebingen.de>, Byung-Hoon Kim
<byung-hoon.kim at uni-tuebingen.de> wrote:

> Hi, all
> 
> Can proteinase inhibitors (Aprotinin, Leupeptin and Pepstatin) penetrate
> the cell membrane?
> 
> 
> Byung-Hoon Kim

No, leupeptin can't, not sure about the others but I doubt it.  They are
taken up by endocytosis and act on lysosomal proteases AFAIK.  However,
there are some protease inhibitors which reputedly are membrane permeant. 
The one I know is E64-d, a dervative of the cysteine protease inhibitor E64
(which is membrane impermeant). E64-d will inhibit cytoplasmic calpain I
believe.

-- 
Fergus Doherty,
School of Biomedical Sciences,
Nottingham University,

Fergus.Doherty at nottingham.ac.uk
0115 970 9366 (74-41366 internal)




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