Special Issue "State of Art in Protein Degraders and Autophagy Modulators in the Cancer Treatment"
Deadline for manuscript submissions: closed (10 December 2022) | Viewed by 6980
Interests: protein aggregation; neurobiology; Parkinson’s disease; autophagy
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2. Centro de Investigación Biomédica en Red Sobre Enfermedades Neurodegenerativas, Consorcio CIBER, Instituto de Salud Carlos III, 28029 Madrid, Spain
Interests: autophagy; pharmacology; cancer
Almost all cellular functions depend on the steady state of the proteome, achieved through a balance between protein synthesis and degradation. Dysregulation in protein homeostasis is emerging as a causative event in a number of diseases, including cancer. The imbalance in protein homeostasis may overload the cellular protein handling machinery and, eventually, brings proteotoxic stress. The proteotoxic stress is harmful: eukaryotic cells can rely on multiple protein quality control pathways for resolving the proteotoxic stress, including autophagy. Numerous tumor suppressor oncogenes interfere with autophagy, including the oncosuppressor p53. The role of autophagy in cancer is now emerging: autophagy deregulation is among the key features for tumor progression. Indeed, the dysregulation of protein levels, such as the overexpression of oncoproteins can trigger the neoplastic process. The selective degradation of target proteins is an attractive approach to tackle cancer progression. Following a long and also tragic history, thalidomide was discovered to drive proteins towards proteasomal degradation upon coupling to an E3 ubiquitin ligase. This discovery lead to the development of chemical platforms allowing the targeted degradation of previously undruggable proteins.
This Special Issue invites international researchers in the area of new strategies to induce targeted protein degradation and modulate autophagy in therapeutic, authentic models. We welcome original research articles and reviews focused on the identification of natural and synthetic pharmacological leads from HTS campaigns, on the rational design and structure–activity relationships of small molecules, alternative systems to deliver pro-drugs, and preclinical evaluation of promising leads.
I look forward to receiving your contributions.
Prof. Dr. Giovanni Piccoli
Dr. María Dolores Pérez-Carrión
Dr. Fabrizia Claudia Guarnieri
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- degrader therapeutic
- in vitro models
- in vivo models
- Proteolysis Targeting Chimeric Molecules
- delivery systems
- rational drug design