Results 41 to 50 of about 2,002 (201)

Photoactivatable prodrugs of antimelanoma agent Vemurafenib [PDF]

, 2015
In this study, we report on novel photoactivatable caged prodrugs of vemurafenib. This kinase inhibitor was the first approved drug for the personalized treatment of BRAF-mutated melanoma and showed impressive results in clinical studies.
Bollag G., Bollag G., Boris Pinchuk, Byrnes K. R., Chapman P. B., Christian Peifer, Collins I., Curley K., Dar A. C., Dario Alessi, Dissanayake K., Ellis-Davies G. C. R., Flaherty K. T., Jang S., Johannessen C. M., Kaplan J. H., Klán P., Lee J. T., Levitzki A., Li H., Matsumura Y., Mayer G., Morckel A. R., Morison W. L., Paul Davies, Pelliccioli A. P., Poulikakos P. I., Rabiller M., Rebecca Horbert, Shi H., Shi H., Sosman J. A., Swaika A., Søndergaard J. N., Veldhuyzen W. F., Velema W. A., Villanueva J., Wang Q., Wood J. S., Yang H.   +39 more
core   +3 more sources

Precise photopharmacological eradication of metastatic tumor cells

Disease Models & Mechanisms
ABSTRACT Owing to their high efficacy, antimitotic chemotherapeutics are the mainstay for most cancer treatments. However, these drugs do not discriminate between tumor and healthy cells, thus show dose-limiting toxicity and severe adverse effects. To improve treatments, rendering chemotherapeutics tumor-cell specific is highly desirable.
Adam Varady, Sarah Grissenberger, Andrea Wenninger-Weinzierl, Hugo Poplimont, Caterina Sturtzel, Nicole Schmitner, Li Gao, Robin A. Kimmel, Martin Distel   +8 more
doaj   +3 more sources

Photopharmacological Control of Cyclic Antimicrobial Peptides

ChemBioChem, 2018
AbstractGramicidin S is a naturally occurring antimicrobial cyclic peptide. Herein, we present a series of cyclic peptides based on gramicidin S that contain an azobenzene photoswitch to reversibly control secondary structure and, hence, antimicrobial activity.
Yuan Qi Yeoh, Jingxian Yu, Steven W. Polyak, John R. Horsley, Andrew D. Abell   +4 more
openaire   +5 more sources

On the promise of photopharmacology using photoswitches: a medicinal chemist's perspective. [PDF]

, 2020
Photopharmacology is a growing area of endeavor that employs photoswitchable ligands to allow for light-dependent pharmacological activity. By coupling light to therapeutic action, improved spatial and temporal selectivity can be achieved and ...
Fuchter, MJ
core   +1 more source

Substituted nitrogen-bridged diazocines

Beilstein Journal of Organic Chemistry, 2021
Novel nitrogen-bridged diazocines (triazocines) were synthesized that carry a formyl or an acetyl group at the CH2NR-bridge and bromo- or iodo-substituents at the distant phenyl ring.
Pascal Lentes, Jeremy Rudtke, Thomas Griebenow, Rainer Herges   +3 more
doaj   +1 more source

Deuteration as a General Strategy to Enhance Azobenzene-Based Photopharmacology. [PDF]

Angew Chem Int Ed Engl
Roßmann K, Gonzalez-Hernandez AJ, Bhuyan R, Schattenberg C, Sun H, Börjesson K, Levitz J, Broichhagen J.   +7 more
europepmc   +2 more sources

Shedding light on metabotropic glutamate receptors using optogenetics and photopharmacology [PDF]

, 2018
International ...
Goudet, Cyril, Llebaria, Amadeu, Rovira, Xavier   +2 more
core   +3 more sources

Optochemical Control of Immune Checkpoint Blockade via Light‐Triggered PD‐L1 Dimerization

Advanced NanoBiomed Research, 2022
The blockade of PD‐1/PD‐L1, which serves to “release the brake” of tumor immunity, represents a promising approach for treating various malignancies. However, the systemic immune‐related side effects significantly undermine its therapeutic efficacy.
Yuwei Liu, Kaiqi Long, Weirong Kang, Tianyi Wang, Weiping Wang   +4 more
doaj   +1 more source

Recent Approaches to the Identification of Novel Microtubule-Targeting Agents

Frontiers in Molecular Biosciences, 2022
Microtubules are key components of the eukaryotic cytoskeleton with essential roles in cell division, intercellular transport, cell morphology, motility, and signal transduction.
Susanna Eli, Rossella Castagna, Marina Mapelli, Emilio Parisini   +3 more
doaj   +1 more source

In vivophotopharmacology enabled by multifunctional fibers [PDF]

ACS Chemical Neuroscience, 2020
ABSTRACTTo reversibly manipulate neural circuits with increased spatial and temporal control, photoswitchable ligands can add an optical switch to a target receptor or signaling cascade. This approach, termed photopharmacology, has been enabling to molecular neuroscience, however, its application to behavioral experiments has been impeded by a lack of ...
James A. Frank, Marc-Joseph Antonini, Po-Han Chiang, Andres Canales, David B. Konrad, Indie C. Garwood, Gabriela Rajic, Florian Koehler, Yoel Fink, Polina Anikeeva   +9 more
openaire   +2 more sources