Advancing targeted protein degradation for cancer therapy
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
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 …
resurgence has been accompanied by a better understanding of the reactivity relationships …