Prey for the proteasome: targeted protein degradation—a medicinal chemist's perspective

LM Luh, U Scheib, K Juenemann… - Angewandte Chemie …, 2020 - Wiley Online Library
Targeted protein degradation (TPD), the ability to control a proteins fate by triggering its
degradation in a highly selective and effective manner, has created tremendous excitement …

Exploring cellular biochemistry with nanobodies

RW Cheloha, TJ Harmand, C Wijne… - Journal of Biological …, 2020 - ASBMB
Reagents that bind tightly and specifically to biomolecules of interest remain essential in the
exploration of biology and in their ultimate application to medicine. Besides ligands for …

A potent KRAS macromolecule degrader specifically targeting tumours with mutant KRAS

N Bery, A Miller, T Rabbitts - Nature Communications, 2020 - nature.com
Tumour-associated KRAS mutations are the most prevalent in the three RAS-family isoforms
and involve many different amino-acids. Therefore, molecules able to interfere with mutant …

Opportunities and challenges of protein-based targeted protein degradation

F Shen, LMK Dassama - Chemical Science, 2023 - pubs.rsc.org
In the 20 years since the first report of a proteolysis targeting chimeric (PROTAC) molecule,
targeted protein degradation (TPD) technologies have attempted to revolutionize the fields …

Nanobodies as molecular imaging probes

S Barakat, M Berksöz, P Zahedimaram, S Piepoli… - Free Radical Biology …, 2022 - Elsevier
Camelidae derived single-domain antibodies (sdAbs), commonly known as nanobodies
(Nbs), are the smallest antibody fragments with full antigen-binding capacity. Owing to their …

[HTML][HTML] A current overview of RhoA, RhoB, and RhoC functions in vascular biology and pathology

R Eckenstaler, M Hauke, RA Benndorf - Biochemical Pharmacology, 2022 - Elsevier
The Rho subfamily members of Rho GTPases, RhoA, RhoB, and RhoC, are key regulators
of signal transduction in a variety of cellular processes, including regulation of actomyosin …

Targeted protein degradation tools: overview and future perspectives

Y Prozzillo, G Fattorini, MV Santopietro, L Suglia… - Biology, 2020 - mdpi.com
Simple Summary Gene inactivation is a powerful strategy to study the function of specific
proteins in the context of cellular physiology that can be applied for only non-essential …

Productive HIV-1 infection of tissue macrophages by fusion with infected CD4+ T cells

R Mascarau, M Woottum, L Fromont, R Gence… - Journal of Cell …, 2023 - rupress.org
Macrophages are essential for HIV-1 pathogenesis and represent major viral reservoirs.
Therefore, it is critical to understand macrophage infection, especially in tissue …

Progress in the therapeutic inhibition of Cdc42 signalling

NP Murphy, HR Mott, D Owen - Biochemical Society …, 2021 - portlandpress.com
Cdc42 is a member of the Rho family of small GTPases and a key regulator of the actin
cytoskeleton, controlling cell motility, polarity and cell cycle progression. It signals …

A cell-permeant nanobody-based degrader that induces fetal hemoglobin

F Shen, G Zheng, M Setegne, K Tenglin… - ACS Central …, 2022 - ACS Publications
Proximity-based strategies to degrade proteins have enormous therapeutic potential in
medicine, but the technologies are limited to proteins for which small molecule ligands exist …