Statins can block inflammation

LFA703, a statin with high binding affinity for the LFA-1 site but low activity against HMG-CoA reductase has increased anti-inflammatory effects.

Tudor Toma(ttoma@mail.dntis.ro)
May 31, 2001

Finding anti-inflammatory drugs with higher specificity and fewer side effects than steroids is of considerable importance for clinicians in many fields of medicine. In May Nature Medicine Gabriele Weitz–Schmidt and colleagues from Novartis Pharma AG in Switzerland report that statin compounds commonly used for the treatment of hypercholesterolemia have anti-inflammatory properties which can be enhanced by optimisation of the statin molecule.

Weitz-Schmidt et al found that the anti-inflammatory properties of statins is a function of their ability to prevent the binding between β2 integrin leukocyte function antigen-1 (LFA-1) and ICAM-1 via a novel allostearic site within LFA-1. This effect stops the recruitment of leukocytes to sites of inflammation and is unrelated to the statins ability to inhibit 3-hydroxy-3-methylglutaryl coenzyme-A reductase (HMG-CoA) — the mechanism by which statins reduce cholesterol levels. They subsequently developed the molecule LFA703 with enhanced binding affinity for the LFA-1, but with reduced activity against HMG-CoA. LFA703...

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