Results 81 to 90 of about 600,294 (239)

The cooperative regulation of miR‐221 by APE1 and AUF1 impacts p27Kip1 defining a miR signature relevant for cervical cancer

FEBS Open Bio, EarlyView.
A regulatory axis involving APE1, AUF1, and miR‐221 is proposed. Pri‐miR‐221 is processed by DROSHA and DICER to generate mature miR‐221, which targets p27Kip1 mRNA. APE1 and AUF1 compete for pre‐miR‐221 binding. Reduced APE1/AUF1 levels impair miR‐221 biogenesis, decrease p27Kip1 mRNA degradation, and promote cell cycle progression, chemoresistance ...
Matilde Clarissa Malfatti, Nicolò Gualandi, Gianluca Tell, Giulia Antoniali   +3 more
wiley   +1 more source

Highly multiplexed and quantitative cell-surface protein profiling using genetically barcoded antibodies. [PDF]

, 2018
Human cells express thousands of different surface proteins that can be used for cell classification, or to distinguish healthy and disease conditions.
Adams, Jarrett J, Geng, Huimin, Hornsby, Michael, Hu, Amy, Julien, Olivier, Martinko, Alexander J, Moffat, Jason, Mou, Yun, Müschen, Markus, Ploder, Lynda, Pollock, Samuel B, Sidhu, Sachdev S, Wells, James A   +12 more
core   +1 more source

Identification of functional murine mitochondrial formyl peptides and their effects on myeloid‐derived suppressor cell generation

FEBS Open Bio, EarlyView.
We first identified functional murine mitochondrial N‐formyl peptides (MT‐FPs) and investigated their effects on the in vitro myeloid‐derived suppressor cell (MDSC) generation from bone marrow cells. We demonstrated that MT‐FPs acted directly on bone marrow cells to promote MDSC generation and modulated the polymorphonuclear (PMN)‐MDSC/monocyte (M ...
Miyako Ozawa, Saori Kagoshima, Akira Yamada   +2 more
wiley   +1 more source

Target‐Mediated Drug Disposition (TMDD) Revisited: High Versus Low‐Affinity Approximations of the TMDD Model

CPT: Pharmacometrics & Systems Pharmacology
Target‐mediated drug disposition (TMDD) is often associated with high‐affinity binding to a target resulting in nonlinear pharmacokinetics. For large molecules, such as monoclonal antibodies, this can lead to increased clearance at sub‐saturating ...
Ronny Straube
doaj   +1 more source

The therapeutic potential of allosteric ligands for free fatty acid sensitive GPCRs [PDF]

, 2013
G protein coupled receptors (GPCRs) are the most historically successful therapeutic targets. Despite this success there are many important aspects of GPCR pharmacology and function that have yet to be exploited to their full therapeutic potential.
Hudson, Brian D., Milligan, Graeme, Ulven, Trond   +2 more
core   +1 more source

Development of human monoclonal antibodies against TARM1 by yeast display

FEBS Open Bio, EarlyView.
Human monoclonal antibodies against TARM1 are generated by yeast display‐guided selection. These antibodies bind to soluble and cell‐surface forms of TARM1. Also, these antibodies exhibit agonistic activity in the NFAT‐GFP reporter assay, indicating that TARM1 signaling can be functionally modulated by antibodies and suggesting TARM1 as a potential ...
Rikio Yabe, Mayumi Saeki, Masaaki Hashiguchi, Sayaka Ono, Kazuhisa Aoki, Hidetaka Tanno   +5 more
wiley   +1 more source

DTA Atlas: A massive-scale drug repurposing database

Artificial Intelligence in the Life Sciences
The drug development process is costly and time-consuming. Repurposing existing approved drugs, an efficient and cost-effective strategy, involves assessing numerous drug-protein pairs to uncover new interactions.
Madina Sultanova, Elizaveta Vinogradova, Alisher Amantay, Ferdinand Molnár, Siamac Fazli   +4 more
doaj   +1 more source

Structure-guided design and optimization of small molecules targeting the protein-protein interaction between the von hippel-lindau (VHL) E3 ubiquitin ligase and the hypoxia inducible factor (HIF) alpha subunit with in vitro nanomolar affinities [PDF]

, 2014
E3 ubiquitin ligases are attractive targets in the ubiquitin-proteasome system, however, the development of small-molecule ligands has been rewarded with limited success.
Adams J., Alessio Ciulli, Bochevarov A. D., Buckley D. L., Buckley D. L., Buckley D. L., Bunnage M. E., Carles Galdeano, Ciechanover A., Cohen P., David M. Dias, Demo S. D., Dias D. M., Hon W. C., Inge Van Molle, Ipek Birced, Louie R. J., Manalo D. J., Morgan S. Gadd, Muchnik E., Nalepa G., Pedro Soares, Pellecchia M., Rabinowitz M. H., Rentsch A., Salvatore Scaffidi, Sarah Hewitt, Semenza G.L., Tetko I. V., Van Molle I., Wells J. A., Zhang W.   +31 more
core   +5 more sources

Digital twins to accelerate target identification and drug development for immune‐mediated disorders

FEBS Open Bio, EarlyView.
Digital twins integrate patient‐derived molecular and clinical data into personalised computational models that simulate disease mechanisms. They enable rapid identification and validation of therapeutic targets, prediction of drug responses, and prioritisation of candidate interventions.
Anna Niarakis, Philippe Moingeon
wiley   +1 more source

Temperature-sensitive protein–DNA dimerizers [PDF]

, 2005
Programmable DNA-binding polyamides coupled to short peptides have led to the creation of synthetic artificial transcription factors. A hairpin polyamide-YPWM tetrapeptide conjugate facilitates the binding of a natural transcription factor Exd to an ...
Ansari, Aseem Z., Arndt, Hans-Dieter, Dervan, Peter B., Hauschild, Karl E., Metzler, Renee E., Moretti, Rocco, Raffaelle, Marni   +6 more
core   +1 more source