Results 11 to 20 of about 71,065 (294)
Supramolecular Degraders: An Emerging Paradigm in Targeted Protein Degradation. [PDF]
Adv Sci (Weinh)Dynamic supramolecular assembly reshapes targeted protein degradation by coordinating modular degrader construction, delivery, functional integration, and intracellular assembly or activation across proteasomal, endosomal–lysosomal, and autophagy–lysosomal pathways.
Liu K +8 more
europepmc +2 more sources
Use of a direct, positive selection strategy to generate improved prodrug-activating enzymes for cancer gene therapy [PDF]
, 2011 E. coli NfsB nitroreductase (NTR) is currently being studied in combination with the prodrug CB1954, as a gene directed enzyme prodrug therapy. NTR reduces CB1954 at either the 2- or 4-nitro groups to produce highly cytotoxic hydroxylamine derivatives ...
Baker, Shelley Louise
core +7 more sources
Aryloxy Pivaloyloxymethyl Prodrugs as Nucleoside Monophosphate Prodrugs [PDF]
Journal of Medicinal Chemistry, 2021 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
Morphine is not a prodrug [PDF]
British Journal of Anaesthesia, 2015 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
Desymmetrization of Pibrentasvir for Efficient Prodrug Synthesis [PDF]
, 2021 A novel and practical desymmetrization tactic is described to access a new class of pibrentasvir prodrugs. The homotopic benzimidazoles of pibrentasvir (PIB) are differentiated via a one-pot di-Boc/mono-de-Boc selective N-Boc protection and formaldehyde ...
Jan E., Waters +8 more
core +2 more sources
Molecules, 2016 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
Carrier-Free Stimulus-Responsive Theranostic Nanoprodrug Enabling GSH-Consumption-Promoted Chemo-Photodynamic Cancer Therapy. [PDF]
Adv Sci (Weinh)Leveraging the critical role of glutathione (GSH) in mediating drug resistance and scavenging reactive oxygen species (ROS) in cancer cells, a carrier‐free GSH‐consuming theranostic nanoprodrug, consisting of a BODIPY photosensitizer and the chemotherapeutic drug paclitaxel linked through a GSH‐consuming drug linker, is developed to deeply explore the ...
Huang H, Sui B.
europepmc +2 more sources
Ultrasound-Recharged Sub-Nanometer Palladium Catalysts for on-Demand and Self-Terminating Bioorthogonal Prodrug Activation in Cancer Therapy. [PDF]
Adv Sci (Weinh)Safe and precise bioorthogonal therapy of tumors was achieved by an ultrasound‐responsive heterostructured nanoreactor with on‐demand catalytic activity. Under piezoelectric catalysis, the system undergoes reversible Pd2+/Pd0 redox cycling, concurrently enabling spatiotemporally controlled prodrug activation and self‐terminating catalytic dose ...
Xia D +9 more
europepmc +2 more sources
A CNS-Targeting Prodrug Strategy for Nuclear Receptor Modulators [PDF]
, 2020 Neurodegenerative diseases lack a breadth of treatment options due, in part, to the known difficulties associated with a drug’s passage across the blood-brain barrier.
Skylar, Ferrara, Thomas, Scanlan
core +1 more source
A pH-responsive prodrug delivery system of 10-HCPT for controlled release and tumor targeting
International Journal of Nanomedicine, 2017 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