Targeted protein degradation: advances, challenges, and prospects for computational methods
The therapeutic approach of targeted protein degradation (TPD) is gaining momentum due
to its potentially superior effects compared with protein inhibition. Recent advancements in …
to its potentially superior effects compared with protein inhibition. Recent advancements in …
Early evaluation of opportunities in oral delivery of PROTACs to overcome their molecular challenges
Abstract PROteolysis TArgeting Chimeras (PROTACs) offer new opportunities in modern
medicine by targeting proteins that are intractable to classic inhibitors. Heterobifunctional in …
medicine by targeting proteins that are intractable to classic inhibitors. Heterobifunctional in …
[HTML][HTML] Phase homogeneity in ternary amorphous solid dispersions and its impact on solubility, dissolution and supersaturation–Influence of processing and …
F Pöstges, J Lenhart, E Stoyanov, DJ Lunter… - International Journal of …, 2023 - Elsevier
As performance of ternary amorphous solid dispersions (ASDs) depends on the solid-state
characteristics and polymer mixing, a comprehensive understanding of synergistic …
characteristics and polymer mixing, a comprehensive understanding of synergistic …
Salinization Dramatically Enhance the Anti-Prostate Cancer Efficacies of AR/AR-V7 and Mnk1/2 Molecular Glue Degraders, Galeterone and VNPP433-3β Which …
RS Thankan, E Thomas, P Purushottamachar… - Bioorganic …, 2023 - Elsevier
Abstract Galeterone, 3β-(hydroxy)-17-(1H-benzimidazole-1-yl) androsta-5, 16-diene (Gal, 1)
and VNPP433-3β, 3β-(1H-imidazole-1-yl-17-(1H-benzimidazole-1-yl) androsta-5, 16-diene …
and VNPP433-3β, 3β-(1H-imidazole-1-yl-17-(1H-benzimidazole-1-yl) androsta-5, 16-diene …
Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs
Abstract Background Proteolysis-targeting chimeras (PROTACs) are being developed for
therapeutic use. However, they have poor pharmacokinetic profiles and their tissue …
therapeutic use. However, they have poor pharmacokinetic profiles and their tissue …
Cyclodextrin Based Host-Guest Inclusion Complex, an Approach to Enhancing the Physicochemical and Biopharmaceutical Application of Poorly Water-soluble Drugs
M Inam, MF Sareh Sadat, W Chen - Chemical Research in Chinese …, 2023 - Springer
H ost-guest inclusion complexes have been extensively studied for drug delivery
applications. The host molecule, typically cyclodextrin, creates a cavity, in which the guest …
applications. The host molecule, typically cyclodextrin, creates a cavity, in which the guest …
[HTML][HTML] ASDs of PROTACs: Spray-dried solid dispersions as enabling formulations
N Hofmann, M Harms, K Mäder - International Journal of Pharmaceutics, 2024 - Elsevier
Proteolysis targeting chimeras (PROTACs) are a promising class of pharmaceutical agents
with a unique mode of action. PROTACs enable the targeting of a broad variety of structures …
with a unique mode of action. PROTACs enable the targeting of a broad variety of structures …
[HTML][HTML] Use of Poly (vinyl alcohol) in Spray-Dried Dispersions: Enhancing Solubility and Stability of Proteolysis Targeting Chimeras
L Mareczek, LK Mueller, L Halstenberg, TM Geiger… - Pharmaceutics, 2024 - mdpi.com
PROTACs, proteolysis targeting chimeras, are bifunctional molecules inducing protein
degradation through a unique proximity-based mode of action. While offering several …
degradation through a unique proximity-based mode of action. While offering several …
[HTML][HTML] Concordance of vacuum compression molding with spray drying in screening of amorphous solid dispersions of itraconazole
Spray drying is a well-established method for screening spray dried dispersions (SDDs) but
is material consuming, and the amorphous solid dispersions (ASDs) formed have low bulk …
is material consuming, and the amorphous solid dispersions (ASDs) formed have low bulk …
Orally Bioavailable Proteolysis-Targeting Chimeras: An Innovative Approach in the Golden Era of Discovering Small-Molecule Cancer Drugs
Proteolysis-targeting chimeras (PROTACs) are an emerging therapeutic modality that show
promise to open a target space not accessible to conventional small molecules via a …
promise to open a target space not accessible to conventional small molecules via a …