“In-Water” Three-Component One-Pot Reaction for the Facile Synthesis of Densely Functionalized 2,3-Dihydro-1H-pyrrol-2-ols and Mechanistic Insight

Saigal, N Sudheer, SC Sahoo, MM Khan… - ACS Sustainable …, 2024 - ACS Publications
An environmentally friendly multicomponent reaction strategy for the synthesis of functionally
rich all-carbon substituted 2, 3-dihydro-1 H-pyrrol-2-ols “in-water” at room temperature has …

Profiling Cellular Morphological Changes Induced by Dual‐Targeting PROTACs of Aurora Kinase and RNA‐Binding Protein YTHDF2

GL Goebel, N Giannino, P Lampe, X Qiu… - …, 2024 - Wiley Online Library
Proteolysis targeting chimeras (PROTACs) are new chemical modalities that degrade
proteins of interest, including established kinase targets and emerging RNA‐binding …

[HTML][HTML] Application of the Rumsfeld matrix to anticancer natural product target discovery

C Bailly - Pharmacological Research-Reports, 2024 - Elsevier
For a long time, natural products (NP) contribute to the treatment of human pathologies,
notably to cancer treatment with microbial and plant-derived products. The mechanism of …

NIMO: A Natural Product-Inspired Molecular Generative Model Based on Conditional Transformer

X Shen, T Zeng, N Chen, J Li, R Wu - Molecules, 2024 - mdpi.com
Natural products (NPs) have diverse biological activity and significant medicinal value. The
structural diversity of NPs is the mainstay of drug discovery. Expanding the chemical space …

Synthesis, Identification, and Chemoenzymatic Functionalisation of Inhibitors of Sterol Transport Proteins

FS Bro - 2024 - orbit.dtu.dk
Sterol transport proteins (STPs) mediate intracellular sterol transport, organelle contact sites,
and lipid metabolism. Their mis-regulation has been associated with lipid storage disorders …

Identification of a privileged scaffold for inhibition of sterol transport proteins through the synthesis and ring distortion of diverse, pseudo-natural products

FS Bro, L Depta, N Dekker, H Bryce-Rogers… - 2024 - chemrxiv.org
Sterol transport proteins mediate intracellular sterol transport, organelle contact sites, and
lipid metabolism. Despite their importance, the similarities in their sterol-binding domains …