Results 81 to 90 of about 714,957 (298)

Targeted Protein Degradation for Kinase Selectivity [PDF]

Cell Chemical Biology, 2019
Targeted protein degradation offers considerable promise for the discovery of new therapeutics. In Cell Chemical Biology, Brand et al. (2019) identify selective degraders of CDK6 derived from clinically approved CDK4/6 inhibitors. This approach offers the possibility of a differentiated therapeutic profile with potential to treat acute myeloid leukemia.
openaire   +2 more sources

Targeted Protein Degradation by Small Molecules [PDF]

Annual Review of Pharmacology and Toxicology, 2017
Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of disease-relevant proteins.
Daniel P, Bondeson, Craig M, Crews
openaire   +2 more sources

Transferrin receptor 1‐mediated iron uptake supports thermogenic activation in human cervical‐derived adipocytes

FEBS Letters, EarlyView.
In this study, we found that human cervical‐derived adipocytes maintain intracellular iron level by regulating the expression of iron transport‐related proteins during adrenergic stimulation. Melanotransferrin is predicted to interact with transferrin receptor 1 based on in silico analysis.
Rahaf Alrifai, Mizuki Seo, Gyath Karadsheh, Fachrur Rizal Mahendra, Máté Á Demény, Ferenc Győry, János András Mótyán, László Fésüs, Endre Kristóf, Rini Arianti   +9 more
wiley   +1 more source

The autophagic degradation of cytosolic pools of peroxisomal proteins by a new selective pathway. [PDF]

, 2019
Damaged or redundant peroxisomes and their luminal cargoes are removed by pexophagy, a selective autophagy pathway. In yeasts, pexophagy depends mostly on the pexophagy receptors, such as Atg30 for Pichia pastoris and Atg36 for Saccharomyces cerevisiae ...
Farré, Jean-Claude, Li, Xuezhi, Ma, Changle, Subramani, Suresh, Wang, Pingping, Wang, Ruonan, Wang, Xiaofeng, Xia, Zhijie, Zhang, Zhuangzhuang   +8 more
core   +2 more sources

The planar cell polarity protein Vangl2 interacts with the PDZ‐domains of Scribble but not with a unique PDZ‐like domain in Inturned

FEBS Letters, EarlyView.
Structural and biochemical characterisations show that the planar cell polarity (PCP) protein Inturned harbours a unique PDZ‐like domain that does not bind canonical PDZ‐binding motifs (PBMs) like that of another PCP protein Vangl2. In contrast, the apical‐basal polarity protein Scribble contains four PDZ domains that bind Vangl2, but one PDZ domain ...
Stephan Wilmes, Jan Brysch, Carmen Gelze, Lilli Meier, Daniel Kümmel   +4 more
wiley   +1 more source

Gut microbiome and aging—A dynamic interplay of microbes, metabolites, and the immune system

FEBS Letters, EarlyView.
Age‐dependent shifts in microbial communities engender shifts in microbial metabolite profiles. These in turn drive shifts in barrier surface permeability of the gut and brain and induce immune activation. When paired with preexisting age‐related chronic inflammation this increases the risk of neuroinflammation and neurodegenerative diseases.
Aaron Mehl, Eran Blacher
wiley   +1 more source

Expanding The Scope of AKT Modulation Through Targeted Protein Degradation

CHIMIA
AKT is a critical mediator of the phosphoinositide 3-kinase (PI3K) signalling cascade, playing a key role in regulating essential cellular processes. The identification of AKT as one of the most dysregulated pathways in cancer led to the development of ...
Marco Serafini, Rui Moreira
doaj   +1 more source

Proteolysis-targeting chimeras (PROTACs) in cancer therapy

Molecular Cancer, 2022
Proteolysis-targeting chimeras (PROTACs) are engineered techniques for targeted protein degradation. A bifunctional PROTAC molecule with two covalently-linked ligands recruits target protein and E3 ubiquitin ligase together to trigger proteasomal ...
Xinyi Li, Wenchen Pu, Qingquan Zheng, Min Ai, Song Chen, Yong Peng   +5 more
doaj   +1 more source

Drosophila Parkin requires PINK1 for mitochondrial translocation and ubiquitinates Mitofusin [PDF]

, 2010
Loss of the E3 ubiquitin ligase Parkin causes early onset Parkinson's disease, a neurodegenerative disorder of unknown etiology. Parkin has been linked to multiple cellular processes including protein degradation, mitochondrial homeostasis, and autophagy;
A. J. Whitworth, Bueler, Chu, Clark, De Vos, E. Ziviani, Exner, Fallon, Gasser, Geisler, Kim, Koshiba, Liesa, Lim, Moore, Morais, Mortiboys, Narendra, Park, Park, Popp, R. N. Tao, Sandebring, Shimura, Soubannier, Steinbrink, Tatsuta, Twig, Whitworth   +28 more
core   +2 more sources

Chemical Inducers of Targeted Protein Degradation [PDF]

Journal of Biological Chemistry, 2010
The functions of many cellular proteins have been elucidated by selective gene inactivation and subsequent phenotypic analysis. For example, genetic mutations, gene knock-out generation, and the use of RNA interference to target mRNA for degradation can all result in decreased production of a specific protein, yielding informative cellular phenotypes ...
Kanak, Raina, Craig M, Crews
openaire   +2 more sources