Are we ready to design oral PROTACs®?

Are we ready to design oral PROTACs®?

PROTACs® are expected to strongly impact the future of drug discovery. Therefore, in this work we firstly performed a statistical study to highlight the distribution of E3 ligases and POIs collected in PROTAC-DB, the main online database focused on degraders. Moreover, since the emerging technology...

Full description

Bibliographic Details
Main Authors:	Diego Garcia Jimenez, Matteo Rossi Sebastiano, Giulia Caron, Giuseppe Ermondi
Format:	Article
Language:	English
Published:	International Association of Physical Chemists (IAPC) 2021-08-01
Series:	ADMET and DMPK
Online Access:	https://pub.iapchem.org/ojs/index.php/admet/article/view/1037

Similar Items

PROTACs and Building Blocks: The 2D Chemical Space in Very Early Drug Discovery
by: Giuseppe Ermondi, et al.
Published: (2021-01-01)

Block relevance (BR) analysis and polarity descriptors in property-based drug design
by: Giuseppe Ermondi, et al.
Published: (2018-09-01)

Novel approaches for the rational design of PROTAC linkers
by: Almaz Zagidullin, et al.
Published: (2020-10-01)

Development of biophysical methods for characterization of PROTACs
by: Oskar, Westlin
Published: (2021)

Degradation of proteins by PROTACs and other strategies
by: Yang Wang, et al.
Published: (2020-02-01)

Targeting Protein Kinases Degradation by PROTACs
by: Fei Yu, et al.
Published: (2021-06-01)

Solubility prediction in the bRo5 chemical space: where are we right now?
by: Giuseppe Ermondi, et al.
Published: (2020-07-01)

Current strategies for the design of PROTAC linkers: a critical review
by: Robert I. Troup, et al.
Published: (2020-10-01)

Mutant-selective degradation by BRAF-targeting PROTACs
by: Shanique Alabi, et al.
Published: (2021-02-01)

Proteolysis targeting chimeras (PROTACs) in cancer therapy
by: Alberto Ocaña, et al.
Published: (2020-09-01)

Tubulin Resists Degradation by Cereblon-Recruiting PROTACs
by: Ivana Gasic, et al.
Published: (2020-04-01)

Photocontrollable PROTAC molecules: Structure and mechanism of action
by: Koravović Mladen, et al.
Published: (2021-01-01)

Blended-learning for courses in Pharmaceutical Analysis
by: Giulia Caron, et al.
Published: (2011-05-01)

Light-Controllable PROTACs for Temporospatial Control of Protein Degradation
by: Jing Liu, et al.
Published: (2021-07-01)

Degrading AR-Dependent Cancers: Expanding the Role of PROTACs
by: Anna R. Michmerhuizen, et al.
Published: (2020-10-01)

Specific MHC-I Peptides Are Induced Using PROTACs
by: Stephanie M. Jensen, et al.
Published: (2018-11-01)

Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation
by: Liang Jiang, et al.
Published: (2021-05-01)

Editorial: Application of PROTACs as a Novel Strategy for Drug Discovery
by: Hany S. Ibrahim, et al.
Published: (2021-07-01)

Reversible Covalent PROTACs: Novel and Efficient Targeted Degradation Strategy
by: Minghua Yuan, et al.
Published: (2021-07-01)

PROTAC: An Effective Targeted Protein Degradation Strategy for Cancer Therapy
by: Si-Min Qi, et al.
Published: (2021-05-01)

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
by: Yonghan He, et al.
Published: (2020-07-01)

Targeted Protein Degradation by Chimeric Small Molecules, PROTACs and SNIPERs
by: Mikihiko Naito, et al.
Published: (2019-12-01)

Development of Agonist-Based PROTACs Targeting Liver X Receptor
by: Hanqiao Xu, et al.
Published: (2021-05-01)

Exploring the Ubiquitin-Proteasome System (UPS) through PROTAC Technology
by: Carlotta Cecchini, et al.
Published: (2020-04-01)

Discovery of an orally active VHL-recruiting PROTAC that achieves robust HMGCR degradation and potent hypolipidemic activity in vivo
by: Guoshun Luo, et al.
Published: (2021-05-01)

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy
by: Xin Li, et al.
Published: (2020-05-01)

Developing potent PROTACs tools for selective degradation of HDAC6 protein
by: Zixuan An, et al.
Published: (2019-01-01)

PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
by: Peiyi Zhang, et al.
Published: (2020-08-01)

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry
by: Wen-Hao Guo, et al.
Published: (2020-08-01)

Semiconducting polymer nano-PROTACs for activatable photo-immunometabolic cancer therapy
by: Chi Zhang, et al.
Published: (2021-05-01)

Activity of BET-proteolysis targeting chimeric (PROTAC) compounds in triple negative breast cancer
by: María del Mar Noblejas-López, et al.
Published: (2019-08-01)

Proteasomal Degradation of Zn-Dependent Hdacs: The E3-Ligases Implicated and the Designed Protacs That Enable Degradation
by: Laura Márquez-Cantudo, et al.
Published: (2021-09-01)

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
by: Blake E. Smith, et al.
Published: (2019-01-01)

Selective Degradation of Target Proteins by Chimeric Small-Molecular Drugs, PROTACs and SNIPERs
by: Minoru Ishikawa, et al.
Published: (2020-04-01)

Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs
by: Sainan An, et al.
Published: (2018-10-01)

Correction to: Developing potent PROTACs tools for selective degradation of HDAC6 protein
by: Zixuan An, et al.
Published: (2019-02-01)

Chemical Degradation of Androgen Receptor (AR) Using Bicalutamide Analog—Thalidomide PROTACs
by: Ga-Yeong Kim, et al.
Published: (2021-04-01)

Development of PROTACs to address clinical limitations associated with BTK-targeted kinase inhibitors
by: Rachael Arthur, et al.
Published: (2020-06-01)

Design, Synthesis, and Biological Evaluation of Proteolysis Targeting Chimeras (PROTACs) for the Dual Degradation of IGF-1R and Src
by: Sudhakar Manda, et al.
Published: (2020-04-01)

Are We Ready for Migrastatics?
by: Jonathan Solomon, et al.
Published: (2021-07-01)

Cannot write session to /tmp/vufind_sessions/sess_93ev783v4fha82cfbgbfah69ui