The time-lapsed [sup.1]H x NMR spectra in [D.sub.2]O (Figure S8) suggest lability of the chloro and also possibly imidazole ligands over time, demonstrating favorable characteristics for desired in vivo prodrug
First, Bcl-2 overexpression would only transiently occur during the short (<1 week) window in which NSC survival is critical for maximum prodrug
conversion and tumor tropism.
The rate constants ([K.sub.obs]) and the corresponding half-lives ([t.sub.1/2]) for the prodrug
were calculated (Tables 7 and 8).
Of the tested prodrugs
, the sulfenamide with a cyclohexyl tail (prodrug
1) appeared to be the most active inhibitor for both AChE and BuChE ([IC.sub.50] = 890 and 28 nmol/mL, resp.) thus demonstrating a dual-binding property that favours the inhibition of BuChE.
(OTCQB: NSPX), a clinical-stage biotechnology company that has a patented technology platform utilizing thapsigargin for its prodrug
delivery system, mipsagargin.
Recently, macromolecular prodrug
design (MPDD) and applications based on etherified renewable polysaccharides especially cellulose, e.g., hydroxypropylcellulose (HPC) , hydroxypropylmethylcellulose (HPMC) [5, 9], hydroxyethylcellulose , etc., have emerged as thrust area of research.
Many therapeutic drugs have undesirable properties that may become pharmacological, pharmaceutical, or pharmacokinetic barriers in clinical drug application; one of the most promising strategies for precise and efficient drug delivery and enhancement of a drug therapeutic effect is the prodrug
design approach which is becoming more elaborate in the development of efficient and selective drug delivery systems .
French researchers have introduced a new approach in Angewandte Chemie: the enzyme B-galactosidase releases the active drug from an inactive precursor, known as a prodrug
, which only can be taken up by tumor cells.
The enzyme will then activate the prodrug
, killing only the cancer cells.
Inc., a Eugene drug development company using technology licensed from the University of Oregon, won the $200,000 investment prize Thursday in the fourth annual Willamette Angel Conference.
Fostoin is a water-soluble prodrug
of phenytoin injection, a drug that has long been used both in Japan and overseas as a treatment for status epilepticus and other such conditions.
In a new approach, the group from the University's Departments of Chemistry and Biochemistry and Biological Sciences and the Friemann Life Sciences Centre, used a prodrug
strategy to address this issue.