[HTML][HTML] PROTAC: an effective targeted protein degradation strategy for cancer therapy
Proteolysis targeting chimeric (PROTAC) technology is an effective endogenous protein
degradation tool developed in recent years that can ubiquitinate the target proteins through …
degradation tool developed in recent years that can ubiquitinate the target proteins through …
E3 ligase ligands for PROTACs: how they were found and how to discover new ones
T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …
a new modality of chemical tools and potential therapeutics to understand and treat human …
[HTML][HTML] Targeted protein degradation: A promise for undruggable proteins
KTG Samarasinghe, CM Crews - Cell chemical biology, 2021 - cell.com
Summary Protein homeostasis, or" proteostasis," is indispensable for a balanced, healthy
environment within the cell. However, when natural proteostasis mechanisms are …
environment within the cell. However, when natural proteostasis mechanisms are …
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] Targeted degradation of the enhancer lysine acetyltransferases CBP and p300
The enhancer factors CREB-binding protein (CBP) and p300 (also known as KAT3A and
KAT3B) maintain gene expression programs through lysine acetylation of chromatin and …
KAT3B) maintain gene expression programs through lysine acetylation of chromatin and …
[HTML][HTML] Light-controllable PROTACs for temporospatial control of protein degradation
PROteolysis-TArgeting Chimeras (PROTACs) is an emerging and promising approach to
target intracellular proteins for ubiquitination-mediated degradation, including those so …
target intracellular proteins for ubiquitination-mediated degradation, including those so …
Clinical efficacy and molecular response correlates of the WEE1 inhibitor adavosertib combined with cisplatin in patients with metastatic triple-negative breast cancer
Purpose: We report results from a phase II study assessing the efficacy of the WEE1 inhibitor
adavosertib with cisplatin in metastatic triple-negative breast cancer (mTNBC). Patients and …
adavosertib with cisplatin in metastatic triple-negative breast cancer (mTNBC). Patients and …
The therapeutic potential of PROTACs
AB Benowitz, KL Jones, JD Harling - Expert Opinion on …, 2021 - Taylor & Francis
Introduction PROTACs represent a novel class of heterobifunctional molecules that
simultaneously bind to a target protein and to an E3 ligase complex, resulting in the transfer …
simultaneously bind to a target protein and to an E3 ligase complex, resulting in the transfer …
PROTACs, molecular glues and bifunctionals from bench to bedside: Unlocking the clinical potential of catalytic drugs
The vast majority of currently marketed drugs rely on small molecules with an 'occupancy-
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
driven'mechanism of action (MOA). Therefore, the efficacy of these therapeutics depends on …
Treatment of melanoma by nano-conjugate-delivered Wee1 siRNA
X Zhang, A Cai, Y Gao, Y Zhang, X Duan… - Molecular …, 2021 - ACS Publications
Small interfering RNA (siRNA)-based drugs have shown tremendous potential to date in
cancer gene therapy. Despite the considerable efforts in siRNA design and manufacturing …
cancer gene therapy. Despite the considerable efforts in siRNA design and manufacturing …