Carbon dots: a review with focus on sustainability

J Ren, H Opoku, S Tang, L Edman… - Advanced Science, 2024 - Wiley Online Library
Carbon dots (CDs) are an emerging class of nanomaterials with attractive optical properties,
which promise to enable a variety of applications. An important and timely question is …

New insights into DNA helicases as druggable targets for cancer therapy

A Datta, RM Brosh Jr - Frontiers in molecular biosciences, 2018 - frontiersin.org
Small molecules that deter the functions of DNA damage response machinery are
postulated to be useful for enhancing the DNA damaging effects of chemotherapy or ionizing …

Development of a novel B-cell lymphoma 6 (BCL6) PROTAC to provide insight into small molecule targeting of BCL6

W McCoull, T Cheung, E Anderson, P Barton… - ACS Chemical …, 2018 - ACS Publications
B-cell lymphoma 6 (BCL6) inhibition is a promising mechanism for treating hematological
cancers but high quality chemical probes are necessary to evaluate its therapeutic potential …

Noncovalent CDK12/13 dual inhibitors-based PROTACs degrade CDK12-Cyclin K complex and induce synthetic lethality with PARP inhibitor

T Niu, K Li, L Jiang, Z Zhou, J Hong, X Chen… - European journal of …, 2022 - Elsevier
Abstract Cyclin-dependent kinase 12 (CDK12) plays a crucial role in DNA-damage
response gene transcription and has recently been validated as a promising target in cancer …

Inhibition of β-catenin/B cell lymphoma 9 protein− protein interaction using α-helix–mimicking sulfono-γ-AApeptide inhibitors

P Sang, M Zhang, Y Shi, C Li… - Proceedings of the …, 2019 - National Acad Sciences
The rational design of α-helix–mimicking peptidomimetics provides a streamlined approach
to discover potent inhibitors for protein− protein interactions (PPIs). However, designing cell …

A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase

NJ Martinez, RR Asawa, MG Cyr, A Zakharov… - Scientific reports, 2018 - nature.com
Assessment of the interactions between a drug and its protein target in a physiologically
relevant cellular environment constitutes a major challenge in the pre-clinical drug discovery …

Design, optimization, and study of small molecules that target tau pre-mRNA and affect splicing

JL Chen, P Zhang, M Abe, H Aikawa… - Journal of the …, 2020 - ACS Publications
Approximately 95% of human genes are alternatively spliced, and aberrant splicing events
can cause disease. One pre-mRNA that is alternatively spliced and linked to …

New hemisynthetic derivatives of sphaeropsidin phytotoxins triggering severe endoplasmic reticulum swelling in cancer cells

A Ingels, R Scott, AR Hooper… - Scientific Reports, 2024 - nature.com
Sphaeropsidins are iso-pimarane diterpenes produced by phytopathogenic fungi that
display promising anticancer activities. Sphaeropsidin A, in particular, has been shown to …

[HTML][HTML] Overcoming Challenges in Small-Molecule Drug Bioavailability: A Review of Key Factors and Approaches

K Wu, SH Kwon, X Zhou, C Fuller, X Wang… - International Journal of …, 2024 - mdpi.com
The bioavailability of small-molecule drugs remains a critical challenge in pharmaceutical
development, significantly impacting therapeutic efficacy and commercial viability. This …

[HTML][HTML] Structure and inhibition of SARS-CoV-1 and SARS-CoV-2 main proteases by oral antiviral compound AG7404

M Fàbrega-Ferrer, A Herrera-Morandé, S Muriel-Goñi… - Antiviral Research, 2022 - Elsevier
Severe acute respiratory syndrome coronaviruses 1 and 2 (SARS-CoV-1 and SARS-CoV-2)
pose a threat to global public health. The 3C-like main protease (M pro), which presents …