Coassembly of Mgm1 isoforms requires cardiolipin and mediates mitochondrial inner membrane fusion [PDF]
Two dynamin-related protein (DRP) families are essential for fusion of the outer and inner mitochondrial membranes, Fzo1 (yeast)/Mfn1/Mfn2 (mammals) and Mgm1 (yeast)/Opa1 (mammals), respectively.
Rachel M. DeVay +50 more
core +2 more sources
Natural product-based PROteolysis TArgeting Chimeras (PROTACs)
Natural products exert their action by direct interaction with specific protein targets. Thus, they provide valuable starting points for the design of novel PROTAC molecules, as they present biologically pre-validated protein–ligand pairs.
Miaomiao Liu +2 more
openaire +5 more sources
Proteolysis‐targeting chimeras in drug development: A safety perspective [PDF]
Proteolysis‐targeting chimeras are a new drug modality that exploits the endogenous ubiquitin proteasome system to degrade a protein of interest for therapeutic benefit. As the first‐generation of proteolysis‐targeting chimeras have now entered clinical trials for oncology indications, it is timely to consider the theoretical safety risks inherent with
Kevin Moreau +8 more
openaire +3 more sources
Advances in targeted degradation of endogenous proteins [PDF]
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
Proteolysis of HCF-1 by Ser/Thr glycosylation-incompetent O-GlcNAc transferase:UDP-GlcNAc complexes [PDF]
In complex with the cosubstrate UDP-N-acetylglucosamine (UDP-GlcNAc),O-linked-GlcNAc transferase (OGT) catalyzes Ser/ThrO-GlcNAcylation of many cellular proteins and proteolysis of the transcriptional coregulator HCF-1.
Bhuiyan, Tanja +6 more
core +3 more sources
Matrix metalloproteinases at key junctions in the pathomechanism of stroke [PDF]
Matrix metalloproteinases play a crucial role in the remodelling of the extracellular matrix through direct degradation of its structural proteins and control of extracellular signaling.
Amento +91 more
core +1 more source
Targeting Protein Kinases Degradation by PROTACs
Kinase dysregulation is greatly associated with cell proliferation, migration and survival, indicating the importance of kinases as therapeutic targets for anticancer drug development.
Fei Yu +3 more
doaj +1 more source
Modulation of microtubule acetylation by the interplay of TPPP/p25, SIRT2 and new anticancer agents with anti-SIRT2 potency [PDF]
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
Targeted degradation of LRG1 to attenuate renal fibrosis
Leucine-rich α-2 glycoprotein 1 (LRG1), a secreted glycoprotein, has been identified as significantly upregulated in renal fibrosis, potentially exacerbating the condition by enhancing TGF-β-Smad3-dependent signaling pathways.
Linyao Fan +11 more
doaj +1 more source
Molecular architecture of human polycomb repressive complex 2. [PDF]
Polycomb Repressive Complex 2 (PRC2) is essential for gene silencing, establishing transcriptional repression of specific genes by tri-methylating Lysine 27 of histone H3, a process mediated by cofactors such as AEBP2.
Aebersold, Ruedi +5 more
core +1 more source

