PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
A guide to: generation and design of nanobodies
S Muyldermans - The FEBS journal, 2021 - Wiley Online Library
A nanobody (Nb) is a registered trademark of Ablynx, referring to the single antigen‐binding
domain of heavy chain‐only antibodies (HCAbs) that are circulating in Camelidae. Nbs are …
domain of heavy chain‐only antibodies (HCAbs) that are circulating in Camelidae. Nbs are …
Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules
Chemical biology strategies for directly perturbing protein homeostasis including the
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
degradation tag (dTAG) system provide temporal advantages over genetic approaches and …
Delivering on the promise of protein degraders
MN O'Brien Laramy, S Luthra, MF Brown… - Nature Reviews Drug …, 2023 - nature.com
Over the past 3 years, the first bivalent protein degraders intentionally designed for targeted
protein degradation (TPD) have advanced to clinical trials, with an initial focus on …
protein degradation (TPD) have advanced to clinical trials, with an initial focus on …
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 …
degradation in a highly selective and effective manner, has created tremendous excitement …
Nanobody technology: a versatile toolkit for microscopic imaging, protein–protein interaction analysis, and protein function exploration
E Beghein, J Gettemans - Frontiers in immunology, 2017 - frontiersin.org
Over the last two decades, nanobodies or single-domain antibodies have found their way in
research, diagnostics, and therapy. These antigen-binding fragments, derived from Camelid …
research, diagnostics, and therapy. These antigen-binding fragments, derived from Camelid …
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 …
and involve many different amino-acids. Therefore, molecules able to interfere with mutant …
Selective and noncovalent targeting of RAS mutants for inhibition and degradation
Activating mutants of RAS are commonly found in human cancers, but to date selective
targeting of RAS in the clinic has been limited to KRAS (G12C) through covalent inhibitors …
targeting of RAS in the clinic has been limited to KRAS (G12C) through covalent inhibitors …
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 …
exploration of biology and in their ultimate application to medicine. Besides ligands for …
Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader
Inducing post-translational protein knockdown is an important approach to probe biology
and validate drug targets. An efficient strategy to achieve this involves expression of a …
and validate drug targets. An efficient strategy to achieve this involves expression of a …