PROTAC targeted protein degraders: the past is prologue

M Békés, DR Langley, CM Crews - Nature Reviews Drug Discovery, 2022 - nature.com
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 …

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 …

Rapid and direct control of target protein levels with VHL-recruiting dTAG molecules

B Nabet, FM Ferguson, BKA Seong, M Kuljanin… - Nature …, 2020 - nature.com
Chemical biology strategies for directly perturbing protein homeostasis including the
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 …

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 …

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 …

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 …

Selective and noncovalent targeting of RAS mutants for inhibition and degradation

KW Teng, ST Tsai, T Hattori, C Fedele, A Koide… - Nature …, 2021 - nature.com
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 …

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 …

Rapid and reversible knockdown of endogenously tagged endosomal proteins via an optimized HaloPROTAC degrader

H Tovell, A Testa, C Maniaci, H Zhou… - ACS chemical …, 2019 - ACS Publications
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 …