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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 …
[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
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 …
pharmaceutical compounds for treatment of a wide range of diseases. Their prevalence in …
Sequence-based drug design as a concept in computational drug design
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 …
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
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 …
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
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 …
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
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 …
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
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 …
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 …
permeability of compounds in in vitro conditions. Due to the significant increase in …
How big is too big for cell permeability?
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 …
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 …
such as fibrosis, cancer, metabolic, inflammatory, and heart disease. We recently found a …