Understanding cell penetration of cyclic peptides

PG Dougherty, A Sahni, D Pei - Chemical Reviews, 2019 - ACS Publications
Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …

Mathematical modeling of release kinetics from supramolecular drug delivery systems

C Mircioiu, V Voicu, V Anuta, A Tudose, C Celia… - Pharmaceutics, 2019 - mdpi.com
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 …

[PDF][PDF] Physicochemical and biopharmaceutical aspects influencing skin permeation and role of SLN and NLC for skin drug delivery

EB Souto, JF Fangueiro, AR Fernandes, A Cano… - Heliyon, 2022 - cell.com
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 …

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 …

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 …

Understanding and improving the membrane permeability of VH032-based PROTACs

VG Klein, CE Townsend, A Testa… - ACS medicinal …, 2020 - ACS Publications
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 …

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 …

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 …

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 …

Mathematical models of skin permeability: an overview

S Mitragotri, YG Anissimov, AL Bunge… - International journal of …, 2011 - Elsevier
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 …