Fundamental aspects of DMPK optimization of targeted protein degraders

C Cantrill, P Chaturvedi, C Rynn, JP Schaffland… - Drug discovery today, 2020 - Elsevier
Highlights•Degraders are an emerging modality which fall into the 'beyond rule of
5'space.•Poor permeability and solubility are critical features limiting oral absorption.• …

Cyanobacteria and eukaryotic microalgae as emerging sources of antibacterial peptides

V Rojas, L Rivas, C Cárdenas, F Guzmán - Molecules, 2020 - mdpi.com
Cyanobacteria and microalgae are oxygen-producing photosynthetic unicellular organisms
encompassing a great diversity of species, which are able to grow under all types of extreme …

Amorphous solid dispersions (asds): The influence of material properties, manufacturing processes and analytical technologies in drug product development

R Iyer, V Petrovska Jovanovska, K Berginc, M Jaklič… - Pharmaceutics, 2021 - mdpi.com
Poorly water-soluble drugs pose a significant challenge to developability due to poor oral
absorption leading to poor bioavailability. Several approaches exist that improve the oral …

Discovery solubility measurement and assessment of small molecules with drug development in mind

JA Barrett, W Yang, SM Skolnik, LM Belliveau… - Drug discovery today, 2022 - Elsevier
Highlights•Seamless solubility understanding requires discovery-development
collaboration.•Gold standard methods in drug development map solubility of drug …

Application of machine learning in translational medicine: current status and future opportunities

N Terranova, K Venkatakrishnan, LJ Benincosa - The AAPS Journal, 2021 - Springer
The exponential increase in our ability to harness multi-dimensional biological and clinical
data from experimental to real-world settings has transformed pharmaceutical research and …

Therapeutic advances in oncology

J Liu, P Pandya, S Afshar - International journal of molecular sciences, 2021 - mdpi.com
Around 77 new oncology drugs were approved by the FDA in the past five years; however,
most cancers remain untreated. Small molecules and antibodies are dominant therapeutic …

Plasma protein-mediated uptake and contradictions to the free drug hypothesis: a critical review

JA Schulz, DM Stresser, JC Kalvass - Drug metabolism reviews, 2023 - Taylor & Francis
According to the free drug hypothesis (FDH), only free, unbound drug is available to interact
with biological targets. This hypothesis is the fundamental principle that continues to explain …

Smart design of patient-centric long-acting products: from preclinical to marketed pipeline trends and opportunities

C Bassand, A Villois, L Gianola, G Laue… - Expert opinion on …, 2022 - Taylor & Francis
Introduction We see a development in the field of long-acting products to serve patients with
chronic diseases by providing benefits in adherence, efficacy, and safety of the treatment …

Macrocyclic DNA-encoded chemical libraries: a historical perspective

L Plais, J Scheuermann - RSC Chemical Biology, 2022 - pubs.rsc.org
While macrocyclic peptides are extensively researched for therapeutically relevant protein
targets, DNA-encoded chemical libraries (DELs) are developed at a quick pace to discover …

Network pharmacology and molecular docking study on the active ingredients of qidengmingmu capsule for the treatment of diabetic retinopathy

M Zhang, J Yang, X Zhao, Y Zhao, S Zhu - Scientific Reports, 2021 - nature.com
Diabetic retinopathy (DR) is a leading cause of irreversible blindness globally.
Qidengmingmu Capsule (QC) is a Chinese patent medicine used to treat DR, but the …