HSP70 multi-functionality in cancer
Z Albakova, GA Armeev, LM Kanevskiy, EI Kovalenko… - Cells, 2020 - mdpi.com
The 70-kDa heat shock proteins (HSP70s) are abundantly present in cancer, providing
malignant cells selective advantage by suppressing multiple apoptotic pathways, regulating …
malignant cells selective advantage by suppressing multiple apoptotic pathways, regulating …
Lysine‐targeting covalent inhibitors
J Pettinger, K Jones… - Angewandte Chemie …, 2017 - Wiley Online Library
Targeted covalent inhibitors have gained widespread attention in drug discovery as a
validated method to circumvent acquired resistance in oncology. This strategy exploits small …
validated method to circumvent acquired resistance in oncology. This strategy exploits small …
[HTML][HTML] The remarkable multivalency of the Hsp70 chaperones
ERP Zuiderweg, LE Hightower, JE Gestwicki - Cell Stress and Chaperones, 2017 - Elsevier
Hsp70 proteins are key to maintaining intracellular protein homeostasis. To carry out this
task, they employ a large number of cochaperones and adapter proteins. Here, we review …
task, they employ a large number of cochaperones and adapter proteins. Here, we review …
Pyrrolo[2,3‐d]pyrimidine (7‐deazapurine) as a privileged scaffold in design of antitumor and antiviral nucleosides
P Perlíková, M Hocek - Medicinal Research Reviews, 2017 - Wiley Online Library
Deazapurine (pyrrolo [2, 3‐d] pyrimidine) nucleosides are important analogues of biogenic
purine nucleosides with diverse biological activities. Replacement of the N7 atom with a …
purine nucleosides with diverse biological activities. Replacement of the N7 atom with a …
Hsp multichaperone complex buffers pathologically modified Tau
A Moll, LM Ramirez, M Ninov, J Schwarz… - Nature …, 2022 - nature.com
Alzheimer's disease is a neurodegenerative disorder in which misfolding and aggregation of
pathologically modified Tau is critical for neuronal dysfunction and degeneration. The two …
pathologically modified Tau is critical for neuronal dysfunction and degeneration. The two …
Kinetic optimization of lysine-targeting covalent inhibitors of HSP72
J Pettinger, M Carter, K Jones… - Journal of Medicinal …, 2019 - ACS Publications
The covalent inhibition mechanism of action, which overcomes competition with high-affinity,
high-abundance substrates of challenging protein targets, can deliver effective chemical …
high-abundance substrates of challenging protein targets, can deliver effective chemical …
Combination of anti-cancer drugs with molecular chaperone inhibitors
M Shevtsov, G Multhoff, E Mikhaylova… - International journal of …, 2019 - mdpi.com
Most molecular chaperones belonging to heat shock protein (HSP) families are known to
protect cancer cells from pathologic, environmental and pharmacological stress factors and …
protect cancer cells from pathologic, environmental and pharmacological stress factors and …
An irreversible inhibitor of HSP72 that unexpectedly targets lysine‐56
J Pettinger, YV Le Bihan, M Widya… - Angewandte …, 2017 - Wiley Online Library
The stress‐inducible molecular chaperone, HSP72, is an important therapeutic target in
oncology, but inhibiting this protein with small molecules has proven particularly …
oncology, but inhibiting this protein with small molecules has proven particularly …
Reflections and outlook on targeting HSP90, HSP70 and HSF1 in cancer: a personal perspective
P Workman - HSF1 and Molecular Chaperones in Biology and …, 2020 - Springer
This personal perspective focuses on small-molecule inhibitors of proteostasis networks in
cancer—specifically the discovery and development of chemical probes and drugs acting on …
cancer—specifically the discovery and development of chemical probes and drugs acting on …
A fragment-based approach applied to a highly flexible target: Insights and challenges towards the inhibition of HSP70 isoforms
AM Jones, IM Westwood, JD Osborne, TP Matthews… - Scientific reports, 2016 - nature.com
The heat shock protein 70s (HSP70s) are molecular chaperones implicated in many cancers
and of significant interest as targets for novel cancer therapies. Several HSP70 inhibitors …
and of significant interest as targets for novel cancer therapies. Several HSP70 inhibitors …