Results 61 to 70 of about 11,341 (256)

MDM2-BCL-XL PROTACs enable degradation of BCL-XL and stabilization of p53

Acta Materia Medica, 2022
Inhibition or degradation of the anti-apoptotic protein BCL-XL is a viable strategy for cancer treatment. Despite the recent development of PROTACs for degradation of BCL-XL, the choice of E3 ligase has been restricted to VHL and CRBN.
Mengyang Chang, Feng Gao, Jing Chen, Giri Gnawali, Wei Wang   +4 more
doaj   +1 more source

Recognition of substrate degrons by E3 ubiquitin ligases and modulation by small-molecule mimicry strategies [PDF]

, 2017
The ubiquitin-proteasome system is a master regulator of protein homeostasis, by which proteins are initially targeted for poly-ubiquitination by E3 ligases and then degraded into short peptides by the proteasome.
Alessio Ciulli, Bachmair, Balchin, Basham, Bondeson, Buckley, Buckley, Bulatov, Bullock, Calderon Villalobos, Caramelo, Chamberlain, Chang, Choi, Ciechanover, Condon, DaRosa, Davies, Deshaies, Dou, Elumalai, Feng, Finley, Fischer, Fischer, Frost, Galdeano, Guharoy, Hao, Hennighausen, Herhaus, Hershko, Hon, Ito, Ito, Ivan, Jaakkola, Jiang, Komander, Kraft, Kronke, Kussie, Lai, Lo, Loenarz, Long, Lu, Lu, Matyskiela, Min, Natsume, Neklesa, Nishimura, Orlicky, Orlicky, Petroski, Petzold, Rao, Ravid, Reinhardt, Riedl, Roman-Hernandez, Schuenemann, Sheard, Shi, Skaar, Sriram, Tan, Tasaki, Taxis, Toure, Van Molle, Varshavsky, Vu, Welcker, Wilkins, Winter, Wu, Xavier Lucas, Xie, Zengerle   +80 more
core   +2 more sources

PROTACs: The Future of Leukemia Therapeutics

Frontiers in Cell and Developmental Biology, 2022
The fight to find effective, long-lasting treatments for cancer has led many researchers to consider protein degrading entities. Recent developments in PROteolysis TArgeting Chimeras (PROTACs) have signified their potential as possible cancer therapies.
Anwar, Zubair, Ali, Muhammad Shahzad, Galvano, Antonio, Perez, Alessandro, La Mantia, Maria, Bukhari, Ihtisham, Swiatczak, Bartlomiej   +6 more
openaire   +4 more sources

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

Characteristic roadmap of linker governs the rational design of PROTACs

Acta Pharmaceutica Sinica B
Proteolysis targeting chimera (PROTAC) technology represents a groundbreaking development in drug discovery, leveraging the ubiquitin‒proteasome system to specifically degrade proteins responsible for the disease.
Yawen Dong, Tingting Ma, Ting Xu, Zhangyan Feng, Yonggui Li, Lingling Song, Xiaojun Yao, Charles R. Ashby, Jr, Ge-Fei Hao   +8 more
doaj   +1 more source

The Potential of Proteolytic Chimeras as Pharmacological Tools and Therapeutic Agents

Molecules, 2020
The induction of protein degradation in a highly selective and efficient way by means of druggable molecules is known as targeted protein degradation (TPD).
Bernat Coll-Martínez, Antonio Delgado, Bernat Crosas   +2 more
doaj   +1 more source

Chemical-Mediated Targeted Protein Degradation in Neurodegenerative Diseases

Life, 2021
Neurodegenerative diseases, including Alzheimer’s disease, Huntington’s disease, and Parkinson’s disease, are a class of diseases that lead to dysfunction of cognition and mobility.
Soonsil Hyun, Dongyun Shin
doaj   +1 more source

Engineering of Glioblastoma‐Derived Biomimetic Vesicles and Their Structural and Molecular Features

Advanced Healthcare Materials, EarlyView.
ABSTRACT Biomimetic nanosystems and vesicles have arisen as a novel approach to design vesicular transport systems with diverse therapeutic potential. The ‘biomimetic’ strategy involves the integration of cell membrane components into lipid bilayers, conferring them with biological properties originating from the cell of origin. Until now, most studies
Noelia Hernández‐Lobato, Hanan Abumanhal‐Masarweh, Martí de Cabo, Pablo Guerra, Marilena Hadjidemetriou, Neus Lozano, Kostas Kostarelos   +6 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

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

Exploration of Targeted Anti-tumor Therapy, 2020
PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to bind to a protein of interest, connected by a chemical linker.
Robert I. Troup, Charlene Fallan, Matthias G. J. Baud   +2 more
doaj   +1 more source