From conception to development: investigating PROTACs features for improved cell permeability and successful protein degradation
C Cecchini, S Pannilunghi, S Tardy… - Frontiers in …, 2021 - frontiersin.org
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
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 …
[图书][B] Absorption and drug development: solubility, permeability, and charge state
A Avdeef - 2012 - books.google.com
Explains how to perform and analyze the results of the latest physicochemical methods With
this book as their guide, readers have access to all the current information needed to …
this book as their guide, readers have access to all the current information needed to …
Intramolecular hydrogen bonding in medicinal chemistry
The formation of intramolecular hydrogen bonds has a very pronounced effect on molecular
structure and properties. We study both aspects in detail with the aim of enabling a more …
structure and properties. We study both aspects in detail with the aim of enabling a more …
Pharmaceutical excipients—quality, regulatory and biopharmaceutical considerations
Practically all medications contain excipients, which are added for the purpose of production
enhancement, patient acceptability, improving stability, controlling release etc. Typically …
enhancement, patient acceptability, improving stability, controlling release etc. Typically …
Oral bioavailability: issues and solutions via nanoformulations
K Pathak, S Raghuvanshi - Clinical pharmacokinetics, 2015 - Springer
The delivery of drugs through the oral route is regarded as most optimal to achieve desired
therapeutic effects and patient compliance. However, poor pharmacokinetic profiles of oral …
therapeutic effects and patient compliance. However, poor pharmacokinetic profiles of oral …
Bacterial lipid membranes as promising targets to fight antimicrobial resistance, molecular foundations and illustration through the renewal of aminoglycoside …
MP Mingeot-Leclercq, JL Décout - MedChemComm, 2016 - pubs.rsc.org
Hereunder, we highlight bacterial membrane anionic lipids as attractive targets in the design
of antibacterial drugs which can be effective against both Gram-positive and Gram-negative …
of antibacterial drugs which can be effective against both Gram-positive and Gram-negative …
A novel design of artificial membrane for improving the PAMPA model
X Chen, A Murawski, K Patel, CL Crespi… - Pharmaceutical …, 2008 - Springer
Purpose Since the first demonstration of PAMPA, the artificial membrane has been
traditionally prepared by impregnating a porous filter with a solution of lipid mixture. While …
traditionally prepared by impregnating a porous filter with a solution of lipid mixture. While …
The rise of PAMPA
A Avdeef - Expert opinion on drug metabolism & toxicology, 2005 - Taylor & Francis
The parallel artificial membrane permeability assay (PAMPA), as a passive-permeability
screen, is a possible low-cost alternative to cellular models for the earliest ADME primary …
screen, is a possible low-cost alternative to cellular models for the earliest ADME primary …
PAMPA—critical factors for better predictions of absorption
ABSTRACT PAMPA, log P OCT, and Caco‐2 are useful tools in drug discovery for the
prediction of oral absorption, brain penetration and for the development of structure …
prediction of oral absorption, brain penetration and for the development of structure …