DmCatD, a cathepsin D-like peptidase of the hematophagous insect Dipetalogaster maxima (Hemiptera: Reduviidae): Purification, bioinformatic analyses and the significance of its interaction with lipophorin in the internalization by developing oocytes [PDF]
DmCatD, a cathepsin D-like peptidase of the hematophagous insect Dipetalogaster maxima, is synthesized by the fat body and the ovary and functions as yolk protein precursor. Functionally, DmCatD is involved in vitellin proteolysis.
Arrese, Estela L. +8 more
core +1 more source
Research advances in targeted protein degradation technologies [PDF]
Targeted protein degradation (TPD) technologies leverage the body’s innate protein degradation systems to selectively eliminate protein of interest (POI).
PI Chuan +4 more
doaj +1 more source
Caspase-7 uses an exosite to promote poly(ADP ribose) polymerase 1 proteolysis [PDF]
During apoptosis, hundreds of proteins are cleaved by caspases, most of them by the executioner caspase-3. However, caspase-7, which shares the same substrate primary sequence preference as caspase-3, is better at cleaving poly(ADP ribose) polymerase 1 ...
Blais, Véronique +2 more
core +1 more source
PROTACs are effective in addressing the platelet toxicity associated with BCL-XL inhibitors
BCL-XL is an anti-apoptotic protein that plays an important role in tumorigenesis, metastasis, and intrinsic or therapy-induced cancer drug resistance.
Peiyi Zhang +5 more
doaj +1 more source
BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design [PDF]
Targeting subunits of BAF/PBAF chromatin remodeling complexes has been proposed as an approach to exploit cancer vulnerabilities. Here, we develop proteolysis targeting chimera (PROTAC) degraders of the BAF ATPase subunits SMARCA2 and SMARCA4 using a ...
Arnhof, Heribert +36 more
core +2 more sources
Proteolysis-Targeting Chimeras as Therapeutics and Tools for Biological Discovery [PDF]
New biological tools provide new techniques to probe fundamental biological processes. Here we describe the burgeoning field of proteolysis-targeting chimeras (PROTACs), which are capable of modulating protein concentrations at a post-translational level by co-opting the ubiquitin-proteasome system. We describe the PROTAC technology and its application
George M, Burslem, Craig M, Crews
openaire +2 more sources
Minimal requirements for ubiquitination mediated regulation of thyroid hormone activation [PDF]
Activation of thyroxine by outer ring deiodination is the crucial first step of thyroid hormone action. Substrate-induced ubiquitination of type 2 deiodinase (D2) is the most rapid and sensitive mechanism known to regulate thyroid hormone activation ...
Egri, Péter, Gereben, Balázs
core +1 more source
Proteolysis-targeting chimera against BCL-XL destroys tumor-infiltrating regulatory T cells
Targeting regulatory T cells (Treg) represents a therapeutic option to abrogate tumor-associated immune suppression. Here the authors show that pharmacological degradation of BCL-XL preferentially induces apoptosis of tumor-infiltrating Treg, promoting ...
Ryan Kolb +18 more
doaj +1 more source
Development of KEAP1-targeting PROTAC and its antioxidant properties: In vitro and in vivo
Oxidative stress due to abnormal accumulation of reactive oxygen species (ROS) is an initiator of a large number of human diseases, and thus, the elimination and prevention of excessive ROS are important aspects of preventing the development of such ...
Se Yong Park +10 more
doaj +1 more source
Bridged Proteolysis Targeting Chimera (PROTAC) Enables Degradation of Undruggable Targets. [PDF]
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for degrading disease-causing proteins. While many PROTACs have been developed for numerous protein targets, current small-molecule PROTAC approaches cannot target undruggable proteins that do not have small-molecule binders.
Xiong Y +11 more
europepmc +3 more sources

