Results 11 to 20 of about 65,300 (300)
Dimensionless parameter predicts bacterial prodrug success
Understanding mechanisms of antibiotic failure is foundational to combating the growing threat of multidrug‐resistant bacteria. Prodrugs—which are converted into a pharmacologically active compound after administration—represent a growing class of ...
Brandon Alexander Holt +7 more
doaj +2 more sources
Breast cancer leads to high mortality of women in the world. Docetaxel (DTX) has been widely applied as one of the first-line chemotherapeutic drugs for breast cancer therapy.
Shenwu Zhang +11 more
doaj +2 more sources
Aryloxy Pivaloyloxymethyl Prodrugs as Nucleoside Monophosphate Prodrugs [PDF]
Intracellular phosphorylation of therapeutic nucleoside analogues into their active triphosphate metabolites is a prerequisite for their pharmacological activity. However, the initial phosphorylation of these unnatural nucleosides into their monophosphate derivatives can be a rate-limiting step in their activation. To address this, we herein report the
Ashwag S. Alanazi +2 more
openaire +2 more sources
Prodrugs and prodrug-activated systems in gene therapy [PDF]
The inclusion of genes that control cell fate (so-called suicide, or kill-switch, genes) into gene therapy vectors is based on a compelling rationale for the safe and selective elimination of aberrant transfected cells. Prodrug-activated systems were developed in the 1980s and 1990s and rely on the enzymatic conversion of non-active prodrugs to active ...
Semira Sheikh +2 more
openaire +2 more sources
The purpose of this work is to review the published strategies for the productionof prodrugs of amines. The review is divided in two main groups of approaches: those thatrely on enzymatic activation and those that take advantage of physiological chemicalconditions for release of the drugs.
John F. Gilmer +2 more
openaire +3 more sources
Parkinson`s disease (PD) is a progressive, neurodegenerative disorder whichinvolves the loss of dopaminergic neurons of the substantia nigra pars compacta. Currenttherapy is essentially symptomatic, and L-Dopa (LD), the direct precursor of dopamine(DA), is the treatment of choice in more advanced stages of the disease.
DI STEFANO, Antonio +2 more
openaire +4 more sources
A pH-responsive prodrug delivery system of 10-HCPT for controlled release and tumor targeting
Yang Liu,1–3 Dan Li,2 Xinhong Guo,2 Haiwei Xu,2 Zhi Li,2 Yanling Zhang,2 Chuanjun Song,4 Ruhan Fan,2 Xing Tang,1,* Zhenzhong Zhang2,* 1Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, 2Department of ...
Liu Y +9 more
doaj +1 more source
Morphine is not a prodrug [PDF]
Editor–A prodrug is defined as a medication that is administered in an inactive or less than fully active form and is then converted to its active form through a normal metabolic process (http://en. wikipedia.org/wiki/Prodrug). The title of a recent publication in the British Journal of Analgesia, ‘Morphine-6-glucuronide is responsible for the ...
A, Dahan, J, Lötsch
openaire +2 more sources
The main objective of this review is to describe the importance of dendrimer prodrugs in the design of new drugs, presenting numerous applications of these nanocomposites in the pharmaceutical field. Therefore, the use of dendrimer prodrugs as carrier for drug delivery, to improve pharmacokinetic properties of prototype, to promote drug sustained ...
Soraya da Silva Santos +2 more
openaire +3 more sources
Tetrazine-mediated bioorthogonal prodrug–prodrug activation
Prodrug–prodrug activation describes the simultaneous, traceless and bioorthogonal activation of two drugs.
Kevin Neumann +3 more
openaire +4 more sources

