Advancing targeted protein degradation for cancer therapy

B Dale, M Cheng, KS Park, HÜ Kaniskan… - Nature Reviews …, 2021 - nature.com
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …

[HTML][HTML] Proteolysis-targeting chimeras (PROTACs) in cancer therapy

X Li, W Pu, Q Zheng, M Ai, S Chen, Y Peng - Molecular cancer, 2022 - Springer
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein
degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits …

The PROTACtable genome

M Schneider, CJ Radoux, A Hercules… - Nature reviews Drug …, 2021 - nature.com
Proteolysis-targeting chimeras (PROTACs) are an emerging drug modality that may offer
new opportunities to circumvent some of the limitations associated with traditional small …

[HTML][HTML] PROTACs: great opportunities for academia and industry

X Sun, H Gao, Y Yang, M He, Y Wu, Y Song… - Signal transduction and …, 2019 - nature.com
Although many kinds of therapies are applied in the clinic, drug-resistance is a major and
unavoidable problem. Another disturbing statistic is the limited number of drug targets, which …

Developments of CRBN-based PROTACs as potential therapeutic agents

C Wang, Y Zhang, Y Wu, D Xing - European journal of medicinal chemistry, 2021 - Elsevier
Protease-targeted chimeras (PROTACs) are a new technology that is receiving much
attention in the treatment of diseases. The mechanism is to inhibit protein function by …

[HTML][HTML] Multiple myeloma: the (r) evolution of current therapy and a glance into the future

KC Anderson - Haematologica, 2020 - ncbi.nlm.nih.gov
Over the past 20 years, the regulatory approval of several novel agents to treat multiple
myeloma (MM) has prolonged median patient survival from 3 to 8-10 years. Increased …

[HTML][HTML] Harnessing the power of proteolysis for targeted protein inactivation

R Verma, D Mohl, RJ Deshaies - Molecular cell, 2020 - cell.com
Two decades into the twenty-first century, a confluence of breakthrough technologies
wielded at the molecular level is presenting biologists with unique opportunities to unravel …

[HTML][HTML] Structure, dynamics and function of the 26S proteasome

Y Mao - Macromolecular protein complexes III: structure and …, 2021 - Springer
The 26S proteasome is the most complex ATP-dependent protease machinery, of~ 2.5 MDa
mass, ubiquitously found in all eukaryotes. It selectively degrades ubiquitin-conjugated …

[HTML][HTML] Relapsed/refractory multiple myeloma in 2020/2021 and beyond

K Podar, X Leleu - Cancers, 2021 - mdpi.com
Simple Summary During the last two decades, collaborative translational studies utilizing
novel methodologies have dramatically advanced our understanding of multiple myeloma …

Covalent small molecules as enabling platforms for drug discovery

SE Dalton, S Campos - ChemBioChem, 2020 - Wiley Online Library
Covalent drugs have experienced significant renewed interest in drug discovery. This
resurgence has been accompanied by a better understanding of the reactivity relationships …