Understanding cell penetration of cyclic peptides
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …
Mathematical modeling of release kinetics from supramolecular drug delivery systems
Embedding of active substances in supramolecular systems has as the main goal to ensure
the controlled release of the active ingredients. Whatever the final architecture or entrapment …
the controlled release of the active ingredients. Whatever the final architecture or entrapment …
[PDF][PDF] Physicochemical and biopharmaceutical aspects influencing skin permeation and role of SLN and NLC for skin drug delivery
The skin is a complex and multifunctional organ, in which the static versus dynamic balance
is responsible for its constant adaptation to variations in the external environment that is …
is responsible for its constant adaptation to variations in the external environment that is …
Coexistence of passive and carrier-mediated processes in drug transport
K Sugano, M Kansy, P Artursson, A Avdeef… - Nature reviews Drug …, 2010 - nature.com
The permeability of biological membranes is one of the most important determinants of the
pharmacokinetic processes of a drug. Although it is often accepted that many drug …
pharmacokinetic processes of a drug. Although it is often accepted that many drug …
Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes
M Kansy, F Senner, K Gubernator - Journal of medicinal chemistry, 1998 - ACS Publications
Although biological activity is a key issue in developing a potent drug, other factors such as
solubility, absorption, partitioning, or biodegredation are equally important. Unfortunately …
solubility, absorption, partitioning, or biodegredation are equally important. Unfortunately …
Understanding and improving the membrane permeability of VH032-based PROTACs
Proteolysis targeting chimeras (PROTACs) are catalytic heterobifunctional molecules that
can selectively degrade a protein of interest by recruiting a ubiquitin E3 ligase to the target …
can selectively degrade a protein of interest by recruiting a ubiquitin E3 ligase to the target …
Impact of dynamically exposed polarity on permeability and solubility of chameleonic drugs beyond the rule of 5
M Rossi Sebastiano, BC Doak… - Journal of medicinal …, 2018 - ACS Publications
Conformational flexibility has been proposed to significantly affect drug properties outside
rule-of-5 (Ro5) chemical space. Here, we investigated the influence of dynamically exposed …
rule-of-5 (Ro5) chemical space. Here, we investigated the influence of dynamically exposed …
pH determines the energetic efficiency of the cyanobacterial CO2 concentrating mechanism
NM Mangan, A Flamholz, RD Hood… - Proceedings of the …, 2016 - National Acad Sciences
Many carbon-fixing bacteria rely on a CO2 concentrating mechanism (CCM) to elevate the
CO2 concentration around the carboxylating enzyme ribulose bisphosphate carboxylase …
CO2 concentration around the carboxylating enzyme ribulose bisphosphate carboxylase …
Estimation of blood-brain barrier crossing of drugs using molecular size and shape, and H-bonding descriptors
H van de Waterbeemd, G Camenisch… - Journal of drug …, 1998 - Taylor & Francis
The influence of physicochemical properties, including lipophilicity, H-bonding capacity and
molecular size and shape descriptors on brain uptake has been investigated using a …
molecular size and shape descriptors on brain uptake has been investigated using a …
Mathematical models of skin permeability: an overview
Mathematical models of skin permeability play an important role in various fields including
prediction of transdermal drug delivery and assessment of dermal exposure to industrial …
prediction of transdermal drug delivery and assessment of dermal exposure to industrial …