Results 31 to 40 of about 33,100 (295)

The Feasibility of Enzyme Targeted Activation for Amino Acid/Dipeptide Monoester Prodrugs of Floxuridine; Cathepsin D as a Potential Targeted Enzyme

Molecules, 2012
The improvement of therapeutic efficacy for cancer agents has been a big challenge which includes the increase of tumor selectivity and the reduction of adverse effects at non-tumor sites.
Gordon L. Amidon, Yasuhiro Tsume
doaj   +1 more source

Orthogonal Light- and Enzyme-Triggered and-Gate Prodrugs for Senolytic Therapy. [PDF]

Adv Sci (Weinh)
An orthogonal AND‐gate prodrug platform combines 390 nm near‐UV photocleavage with SA‐β‐gal activation to control payload release in senescent cells. Its modular architecture enables 4‐MU fluorescence, doxorubicin‐mediated cytotoxicity, and ARV‐771‐driven BRD4 degradation, supporting stimulus‐controlled senolytic design in cellular and organoid models.
Chang M, Zhang K, Wang J, Bi F, Dai Z, Yang M, Liu M, Peng H, Zhang F, Guo Y, Dai J, Liu Q, Wang W.   +12 more
europepmc   +2 more sources

Design of BET Inhibitor Prodrugs with Superior Efficacy and Devoid of Systemic Toxicities [PDF]

, 2020
Prodrugs engineered for preferential activation in diseased versus normal tissues offer immense potential to improve the therapeutic index of preclinical and clinical-stage active pharmaceutical ingredients that either cannot be developed otherwise or ...
Peter, Blume-Jensen, Sattanathan, Paramasivan, Samantha W., Brady, Peyton, Shieh, Farrukh, Vohidov, Olga, Burenkova, Hung V.-T., Nguyen, Jenny, Liu, Paul W., Kopesky, Jennifer, K. Saucier-Sawyer, Michael J., Jessel, Julie, Kim, Sung Jin, Huh, Joelle, Baddour, Donald E., Chickering, Elisa, de Stanchina, Lawrence A., Reiter, Bhavatarini, Vangamudi, David J., Turnquist, Kyriakos D., Economides, Michail V., Shipitsin, Jeremiah, Johnson, James C., Ackley, Nolan M., Gallagher, Matthew R., Golder, Allison M., Neenan, Deborah J. C., Ehrlich, Jannik N., Andersen, William K., Dahlberg, Gaurab, KC   +29 more
core   +3 more sources

Potential Development of Tumor-Targeted Oral Anti-Cancer Prodrugs: Amino Acid and Dipeptide Monoester Prodrugs of Gemcitabine

Molecules, 2017
One of the main obstacles for cancer therapies is to deliver medicines effectively to target sites. Since stroma cells are developed around tumors, chemotherapeutic agents have to go through stroma cells in order to reach tumors.
Yasuhiro Tsume, Adam J. Drelich, David E. Smith, Gordon L. Amidon   +3 more
doaj   +1 more source

Synthesis and Antiviral Activity of a Series of 2′-C-Methyl-4′-thionucleoside Monophosphate Prodrugs

Molecules, 2020
The NS5B RNA-dependent RNA polymerase of the hepatitis C virus (HCV) is a validated target for nucleoside antiviral drug therapy. We endeavored to synthesize and test a series of 4′-thionucleosides with a monophosphate prodrug moiety for their antiviral ...
Zackery W. Dentmon, Thomas M. Kaiser, Dennis C. Liotta   +2 more
doaj   +1 more source

Dansyl linked solid phase resins as an educational tool to teach the concepts of high throughput screening and prodrugs.

British Journal of Pharmacy, 2023
High throughput screening (HTS) and combinatorial chemistry, have been part of the process of drug design for nearly two decades. However, methods to teach their practical aspects to undergraduate students are scarce in the literature.
Jordi Morral, Ali Ibrahim, Fatima Traore, Klaus Pors   +3 more
doaj   +1 more source

Tetrazine-mediated bioorthogonal prodrug–prodrug activation

Chemical Science, 2018
Prodrug–prodrug activation describes the simultaneous, traceless and bioorthogonal activation of two drugs.
Kevin Neumann, Alessia Gambardella, Annamaria Lilienkampf, Mark Bradley   +3 more
openaire   +4 more sources

Glucocorticoids-based prodrug design: Current strategies and research progress

Asian Journal of Pharmaceutical Sciences
Attributing to their broad pharmacological effects encompassing anti-inflammation, antitoxin, and immunosuppression, glucocorticoids (GCs) are extensively utilized in the clinic for the treatment of diverse diseases such as lupus erythematosus, nephritis,
Hongbing Liu, Muse Ji, Peifu Xiao, Jingxin Gou, Tian Yin, Haibing He, Xing Tang, Yu Zhang   +7 more
doaj   +1 more source

Cytochrome P450-activated prodrugs [PDF]

, 2013
A prodrug is a compound that has negligible, or lower, activity against a specified pharmacological target than one of its major metabolites. Prodrugs can be used to improve drug delivery or pharmacokinetics, to decrease toxicity, or to target the drug ...
de Montellano, Paul R Ortiz, Paul R Ortiz de Montellano   +1 more
core   +1 more source

UiO‐66 metal–organic frameworks in biomedicine: From structural tunability to bioimaging, photodiagnostics, and photodynamic cancer therapy

FEBS Open Bio, EarlyView.
UiO‐66(Zr) metal–organic frameworks are chemically stable, biocompatible, and highly tunable nanomaterials. Their modular structure enables controlled drug delivery, multimodal bioimaging, and light‐activated photodynamic therapy, supporting integrated diagnostic and therapeutic (theranostic) applications in cancer and biomedical research.
Veronika Huntošová, Grigorii Rakhalskii, Miroslav Almáši   +2 more
wiley   +1 more source