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 …

[HTML][HTML] Successful oral delivery of poorly water-soluble drugs both depends on the intraluminal behavior of drugs and of appropriate advanced drug delivery systems

BJ Boyd, CAS Bergström, Z Vinarov, M Kuentz… - European Journal of …, 2019‏ - Elsevier
Poorly water-soluble drugs continue to be a problematic, yet important class of
pharmaceutical compounds for treatment of a wide range of diseases. Their prevalence in …

Sequence-based drug design as a concept in computational drug design

L Chen, Z Fan, J Chang, R Yang, H Hou, H Guo… - Nature …, 2023‏ - nature.com
Drug development based on target proteins has been a successful approach in recent
decades. However, the conventional structure-based drug design (SBDD) pipeline is a …

Bioavailability and bioaccessibility of food bioactive compounds; overview and assessment by in vitro methods

C Dima, E Assadpour, S Dima… - … Reviews in Food …, 2020‏ - Wiley Online Library
Oral bioavailability is the key to the bioefficiency of food bioactive ingredients; it evaluates
the relationship between foods and their health benefits. The analysis of the main factors …

[HTML][HTML] Oral absorption of peptides and nanoparticles across the human intestine: Opportunities, limitations and studies in human tissues

P Lundquist, P Artursson - Advanced drug delivery reviews, 2016‏ - Elsevier
In this contribution, we review the molecular and physiological barriers to oral delivery of
peptides and nanoparticles. We discuss the opportunities and predictivity of various in vitro …

Oral druggable space beyond the rule of 5: insights from drugs and clinical candidates

BC Doak, B Over, F Giordanetto, J Kihlberg - Chemistry & biology, 2014‏ - cell.com
The rule of 5 (Ro5) is a set of in silico guidelines applied to drug discovery to prioritize
compounds with an increased likelihood of high oral absorption. It has been influential in …

Toward the proactive design of sustainable chemicals: Ionic liquids as a prime example

S Beil, M Markiewicz, CS Pereira, P Stepnowski… - Chemical …, 2021‏ - ACS Publications
The tailorable and often unique properties of ionic liquids (ILs) drive their implementation
into a broad variety of seminal technologies. The modular design of ILs allows in this context …

[HTML][HTML] Caco-2 cell line standardization with pharmaceutical requirements and in vitro model suitability for permeability assays

M Kus, I Ibragimow, H Piotrowska-Kempisty - Pharmaceutics, 2023‏ - mdpi.com
The Caco-2 cell line derived from human colon carcinoma is commonly used to assess the
permeability of compounds in in vitro conditions. Due to the significant increase in …

How big is too big for cell permeability?

P Matsson, J Kihlberg - Journal of medicinal chemistry, 2017‏ - ACS Publications
Understanding how to design cell permeable ligands for intracellular targets that have
difficult binding sites, such as protein–protein interactions, would open vast opportunities for …

Discovery and optimization of the first highly effective and orally available galectin-3 inhibitors for treatment of fibrotic disease

FR Zetterberg, A MacKinnon, T Brimert… - Journal of Medicinal …, 2022‏ - ACS Publications
Galectin-3 is a carbohydrate-binding protein central to regulating mechanisms of diseases
such as fibrosis, cancer, metabolic, inflammatory, and heart disease. We recently found a …