Safety and efficacy constitute the major criteria governing regulatory approval of any new
drug. The best method to maximize safety and efficacy is to deliver a proven therapeutic …

The past few years has witnessed a booming market of protein and peptide drugs, owing to
their superior efficiency and biocompatibility. Parenteral route is the most commonly …

Controlled activation is a critical component in prodrug development. Here we report a
concentration-sensitive platform approach for bioorthogonal prodrug activation by taking …

Prodrug design is a widely known molecular modification strategy that aims to optimize the
physicochemical and pharmacological properties of drugs to improve their solubility and …

Abstract The bisphosphonates ((HO) 2 P (O) CR 1 R 2 P (O)(OH) 2, BPs) were first shown to
inhibit bone resorption in the 1960s, but it was not until 30 years later that a detailed …

Phosphine oxides and related phosphorus-containing functional groups such as
phosphonates and phosphinates are established structural motifs that are still …

The phosphonic acid functional group, which is characterized by a phosphorus atom
bonded to three oxygen atoms (two hydroxy groups and one P= O double bond) and one …

Extensive research into prodrug modification of active pharmaceutical ingredients and
nanoparticle drug delivery systems has led to unprecedented levels of control over the …

Following the first report on the nucleoside phosphoramidate (ProTide) prodrug approach in
1990 by Chris McGuigan, the extensive investigation of ProTide technology has begun in …

Extracellular adenosine (ADO), present in high concentrations in the tumor
microenvironment (TME), suppresses immune function via inhibition of T cell and NK cell …