Targeting CDK4 and CDK6 in cancer

S Goel, JS Bergholz, JJ Zhao - Nature Reviews Cancer, 2022 - nature.com
Abstract Cyclin-dependent kinase 4 (CDK4) and CDK6 are critical mediators of cellular
transition into S phase and are important for the initiation, growth and survival of many …

Cell cycle on the crossroad of tumorigenesis and cancer therapy

J Liu, Y Peng, W Wei - Trends in cell biology, 2022 - cell.com
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …

PROTACs: an emerging therapeutic modality in precision medicine

DA Nalawansha, CM Crews - Cell chemical biology, 2020 - cell.com
Targeted protein degradation (TPD) has emerged as an exciting new era in chemical
biology and drug discovery. PROteolysis TArgeting Chimera (PROTAC) technology targets …

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 …

[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review

RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …

Mechanisms of sensitivity and resistance to CDK4/6 inhibition

M Álvarez-Fernández, M Malumbres - Cancer cell, 2020 - cell.com
Inhibiting the cell-cycle kinases CDK4 and CDK6 results in significant therapeutic effect in
patients with advanced hormone-positive breast cancer. The efficacy of this strategy is …

E3 ligase ligand chemistries: from building blocks to protein degraders

I Sosič, A Bricelj, C Steinebach - Chemical Society Reviews, 2022 - pubs.rsc.org
In recent years, proteolysis-targeting chimeras (PROTACs), capable of achieving targeted
protein degradation, have proven their great therapeutic potential and usefulness as …

E3 ligase ligands in successful PROTACs: an overview of syntheses and linker attachment points

A Bricelj, C Steinebach, R Kuchta, M Gütschow… - Frontiers in …, 2021 - frontiersin.org
Proteolysis-targeting chimeras (PROTACs) have received tremendous attention as a new
and exciting class of therapeutic agents that promise to significantly impact drug discovery …

Development of a BCL-xL and BCL-2 dual degrader with improved anti-leukemic activity

D Lv, P Pal, X Liu, Y Jia, D Thummuri, P Zhang… - Nature …, 2021 - nature.com
Abstract PROteolysis-TArgeting Chimeras (PROTACs) have emerged as an innovative drug
development platform. However, most PROTACs have been generated empirically because …

Signaling pathways in cancer: therapeutic targets, combinatorial treatments, and new developments

HYK Yip, A Papa - Cells, 2021 - mdpi.com
Molecular alterations in cancer genes and associated signaling pathways are used to inform
new treatments for precision medicine in cancer. Small molecule inhibitors and monoclonal …