Results 51 to 60 of about 11,341 (256)
Modulation of microtubule acetylation by the interplay of TPPP/p25, SIRT2 and new anticancer agents with anti-SIRT2 potency [PDF]
, 2017 The microtubule network exerts multifarious functions controlled by its decoration with various proteins and post-translational modifications. The disordered microtubule associated Tubulin Polymerization Promoting Protein (TPPP/p25) and the NAD ...
Adél Szabó +9 more
core +2 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 +3 more
doaj +1 more source
Advances in targeted degradation of endogenous proteins [PDF]
, 2019 Protein silencing is often employed as a means to aid investigations in protein function and is increasingly desired as a therapeutic approach. Several types of protein silencing methodologies have been developed, including targeting the encoding genes ...
Fulcher, Luke +2 more
core +2 more sources
Targeting IRAK4 for Degradation with PROTACs [PDF]
ACS Medicinal Chemistry Letters, 2019 Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) is a key mediator of innate immunity. IRAK4 overactivation is linked with several autoimmune diseases. To date, many IRAK4 inhibitors have been developed to block the protein's kinase activity with the most advanced reaching Phase II clinical trials.
Joao Nunes +9 more
openaire +2 more sources
Surface probing by fragment-based screening and computational methods identifies ligandable pockets on the von Hippel-Lindau (VHL) E3 ubiquitin ligase [PDF]
, 2018 Beyond the targeting of E3 ubiquitin ligases to inhibit protein homeostasis, E3 ligase binders can be repurposed as targeted protein degraders (PROTACs or molecular glues).
Ciulli, Alessio +2 more
core +4 more sources
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
Targeting protein function: the expanding toolkit for conditional disruption [PDF]
, 2016 A major objective in biological research is to understand spatial and temporal requirements for any given gene, especially in dynamic processes acting over short periods, such as catalytically driven reactions, subcellular transport, cell division, cell ...
Bennett, Daimark, Campbell, Amy E
core +1 more source
Science-Business eXchange, 2012 GSK and Yale researchers have announced a collaboration to develop a platform that selectively tags disease-associated proteins with an E3 ubiquitin ligase ligand, thus targeting them to a cell's protein degradation machinery. GSK hopes the platform could be a cornerstone for a new Discovery Performance Unit at the pharma and the partners are aiming to
openaire +1 more source
PROTAC technology for the treatment of Alzheimer’s disease: advances and perspectives
Acta Materia Medica, 2022 Neurodegenerative diseases are characterized by the progression of neuronal degeneration, resulting in dysfunction of cognition and mobility. Many neurodegenerative diseases are due to proteinopathies arising from unusual protein accumulation and ...
Hiroyuki Inuzuka +3 more
doaj +1 more source
Scientific ReportsDysregulation 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 +3 more
doaj +1 more source