Results 31 to 40 of about 11,335 (243)

PROTACs: Walking through hematological malignancies

Frontiers in Pharmacology, 2023
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that uses the proteasome ubiquitin system to target proteins of interest and promote their degradation with remarkable selectivity. Importantly, unlike conventional small molecule inhibitors, PROTACs have proven highly effective in targeting undruggable proteins and those ...
Lara J. Bou Malhab, Habiba Alsafar, Habiba Alsafar, Saleh Ibrahim, Mohamed Rahmani, Mohamed Rahmani   +5 more
openaire   +3 more sources

Specific MHC-I Peptides Are Induced Using PROTACs

Frontiers in Immunology, 2018
Peptides presented by the class-I major histocompatibility complex (MHC-I) are important targets for immunotherapy. The identification of these peptide targets greatly facilitates the generation of T-cell-based therapeutics.
Stephanie M. Jensen, Gregory K. Potts, Damien B. Ready, Melanie J. Patterson   +3 more
doaj   +1 more source

PROTAC Technology: Opportunities and Challenges [PDF]

ACS Medicinal Chemistry Letters, 2020
PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions, large pharmaceutical enterprises (e.g., AstraZeneca, Bayer, Novartis, Amgen, Pfizer, GlaxoSmithKline, Merck, and Boehringer Ingelheim, etc.), and biotechnology companies.
Hongying Gao, Xiuyun Sun, Yu Rao
openaire   +2 more sources

PROTAC-Design-Evaluator (PRODE): An Advanced Method for In-Silico PROTAC Design

ACS Omega, 2023
AbstractPROTAC (proteolysis-targeting chimeras) is a rapidly evolving technology to target undruggable targets. The mechanism by which this happens is when a bifunctional molecule binds to a target protein and also brings in proximity an E3 ubiquitin ligase to trigger ubiquitination and degradation of the target protein. Yet in-silico driven approaches
Ben Geoffrey A S, Deepak Agrawal, Nagaraj M. Kulkarni, Rajappan Vetrivel, Kishan Gurram   +4 more
openaire   +3 more sources

Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs

Pharmaceutics, 2023
Proteolysis-Targeting Chimeras (PROTACs) are a promising new technology in drug development. They have rapidly evolved in recent years, with several of them in clinical trials.
Ponien Kou, Elizabeth S. Levy, An D. Nguyen, Donglu Zhang, Shu Chen, Yusi Cui, Xing Zhang, Fabio Broccatelli, Jennifer Pizzano, Jennifer Cantley, Elizabeth Bortolon, Emma Rousseau, Michael Berlin, Peter Dragovich, Vijay Sethuraman   +14 more
doaj   +1 more source

Decoy-PROTAC for specific degradation of “Undruggable” STAT3 transcription factor

Cell Death and Disease
Signal transducer and activator of transcription 3 (STAT3) is widely recognized as an attractive target for cancer therapy due to its significant role in the initiation and progression of tumorigenesis.
Shiqing Li, Xin Wang, Jiabao Huang, Xiuping Cao, Yana Liu, Shiyan Bai, Tao Zeng, Qi Chen, Chunsen Li, Chunhua Lu, Huanghao Yang   +10 more
semanticscholar   +1 more source

Orthogonal validation of PROTAC mediated degradation of the integral membrane proteins EGFR and c-MET

Scientific Reports
Dysregulation of integral membrane proteins (IMPs) has been linked to a myriad of diseases, making these proteins an attractive target in drug research. Whilst PROTAC technology has had a significant impact in scientific research, its application to IMPs
Camilla Ruffilli, Sascha Röth, Noam Zelcer, Kevin Moreau   +3 more
doaj   +1 more source

PROTAC degraders with ligands recruiting MDM2 E3 ubiquitin ligase: an updated perspective

Acta Materia Medica, 2022
Mouse double minute 2 (MDM2) is an oncogenic E3 ligase that effectively degrades the tumor suppressor p53. In the past two decades, many MDM2 inhibitors that disrupt MDM2-p53 binding have been discovered and developed.
Xin Han, Wenyi Wei, Yi Sun
doaj   +1 more source

Cell wall target fragment discovery using a low‐cost, minimal fragment library

FEBS Letters, EarlyView.
LoCoFrag100 is a fragment library made up of 100 different compounds. Similarity between the fragments is minimized and 10 different fragments are mixed into a single cocktail, which is soaked to protein crystals. These crystals are analysed by X‐ray crystallography, revealing the binding modes of the bound fragment ligands.
Kaizhou Yan, Mathew Stanley, Olawale Raimi, Andrew T. Ferenbach, Helge C Dorfmueller, Daan M. F. van Aalten   +5 more
wiley   +1 more source

FAK inhibition disrupts tumor growth, apoptosis, and transcriptional regulation in GI-NETs

Endocrine Oncology
Background: Gastrointestinal neuroendocrine tumors (GI-NETs) are rare neoplasms with limited therapeutic options and increasing clinical incidence. Focal adhesion kinase (FAK) has been implicated in oncogenic processes across various tumor types; however,
Lara Toffoli, Angeliki Ditsiou, Luca Triboli, Victorine Hamm, Eva Moschioni, Francesca D’Este, Teresa Gagliano   +6 more
doaj   +1 more source