[HTML][HTML] 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 …
Nrf2/Keap1/ARE signaling: Towards specific regulation
The Nrf2 transcription factor governs the expression of hundreds genes involved in cell
defense against oxidative stress, the hallmark of numerous diseases such as …
defense against oxidative stress, the hallmark of numerous diseases such as …
Target and tissue selectivity of PROTAC degraders
RG Guenette, SW Yang, J Min, B Pei… - Chemical Society …, 2022 - pubs.rsc.org
Targeted protein degradation (TPD) strategies have revolutionized how scientists tackle
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
challenging protein targets deemed undruggable with traditional small molecule inhibitors …
The dawn of a new era: targeting the “undruggables” with antibody-based therapeutics
The high selectivity and affinity of antibodies toward their antigens have made them a highly
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …
valuable tool in disease therapy, diagnosis, and basic research. A plethora of chemical and …
Chasing molecular glue degraders: screening approaches
A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
Expanding chemical probe space: quality criteria for covalent and degrader probes
IV Hartung, J Rudolph, MM Mader… - Journal of Medicinal …, 2023 - ACS Publications
Within druggable target space, new small-molecule modalities, particularly covalent
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …
inhibitors and targeted degraders, have expanded the repertoire of medicinal chemists …
Molecular glues: the adhesive connecting targeted protein degradation to the clinic
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
[HTML][HTML] Predicting the structural basis of targeted protein degradation by integrating molecular dynamics simulations with structural mass spectrometry
T Dixon, D MacPherson, B Mostofian… - Nature …, 2022 - nature.com
Targeted protein degradation (TPD) is a promising approach in drug discovery for degrading
proteins implicated in diseases. A key step in this process is the formation of a ternary …
proteins implicated in diseases. A key step in this process is the formation of a ternary …
[HTML][HTML] Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
Current efforts in the proteolysis targeting chimera (PROTAC) field mostly focus on choosing
an appropriate E3 ligase for the target protein, improving the binding affinities towards the …
an appropriate E3 ligase for the target protein, improving the binding affinities towards the …