A novel type of water-soluble prodrugs of cyclosporine A (CsA) is described, featuring a modular system of an enzyme-cleavable group, a solubilizing moiety and a chemodegradable spacer attached to the hydroxyl function of (4R)-4-[(E)-2-butenyl]-4-,N-dimeth ...
Cyclosporins are a family of hydrophobic cyclic undecapeptides produced by the fungus Tolypocladium niveum. The main metabolite cyclosporin A (CsA, see Scheme, R = R' = H) is the first line drug currently used to prevent rejection of organ transplants. Its ...
Cyclosporin is a cyclic undecapeptide useful as drug for organ transplantation due to its immunosuppressive properties. Ten years ago, an anti-viral activity was discovered, incompatible with immunosuppression. These two activities originate in the presenc ...
Mycobacterium tuberculosis, the etiological agent of the infectious disease tuberculosis, kills approximately 1.5 million people annually, while the spread of multidrug-resistant strains is of great global concern. Thus, continuous efforts to identify new ...
A unique, dual-function, photoactivatable anticancer prodrug, RuEuL, has been tailored that features a ruthenium(II) complex linked to a cyclen-europium chelate via a pi-conjugated bridge. Under irradiation at 488 nm, the dark-inactive prodrug undergoes ph ...
Complexes with general formula p,t-[Ru(CO)(PR3)(tren)]X-2 [R=Ph (1) or p-tol (2); tren=tris(2-aminoethyl)amine; X=Cl- or PF6-] were prepared from [RuCl2(CO)(dmf)(PR3)] by direct reaction with tren. The complexes were fully characterized by NMR (H-1, P-31{H ...
The mechanism of action of sulfasalazine, an anti-inflammatory drug used against inflammatory bowel diseases and rheumatoid arthritis is, despite its medical importance, still not well understood. Recently, it was shown that sulfasalazine and its metabolit ...
Received 5 January 2009 Accepted 22 March 2009 Available online 27 March 2009 Keywords: Mixed micelles Drug delivery Block copolymers Sirolimus Extracellular matrix We present the formation of collagen-binding mixed micelles and their potential suitability ...
The cyclosporins comprise a family of cyclic 11-peptides containing seven N-methylated, hydrophobic amino acids. Cyclosporine A (CsA) representing the major member of this family is widely used as immunosuppressive agent in organ transplantations. The biol ...
