Preventive Effect of Pharmaceutical Phytochemicals Targeting the Src Family of Protein Tyrosine Kinases and Aryl Hydrocarbon Receptor on Environmental Stress-Induced Skin Disease. [PDF]
Int J Mol Sci, 2023 Paik SJ, Kim DJ, Jung SK.
europepmc +1 more source
MD and EPR studies of the structure and dynamics of the MTSL spin-labelled activation loop of the Aurora-A kinase [PDF]
arXiv, 2015 The understanding of kinase structure is mostly based on protein crystallography, which is limited by the requirement to trap molecules within a crystal lattice. Therefore, characterisations of the conformational dynamics of the activation loop in solution are important to enhance the understanding of molecular processes related to diseases and to ...
arxiv
Intestinal crypt stem cells possess high levels of cytoskeletal-associated phosphotyrosine-containing proteins and tyrosine kinase activity relative to differentiated enterocytes. [PDF]
, 1989 David R. Burgess +3 more
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Arthritis Care &Research, EarlyView.Objective This work aimed to evaluate the pharmacokinetics, efficacy, and safety of upadacitinib, an oral selective JAK inhibitor, in pediatric patients with polyarticular‐course juvenile idiopathic arthritis (pcJIA). Methods In an open‐label, phase 1 study (SELECT‐YOUTH), enrolled patients, aged 2 to <18 years with pcJIA, received body weight–based ...
Hermine I. Brunner +12 more
wiley +1 more source
Artificial Receptor in Synthetic Cells Performs Transmembrane Activation of Proteolysis
Advanced Biology, EarlyView.Transmembrane signaling is the hallmark of living cells and is among the highest challenges for the design of synthetic cells. Herein, an artificial receptor based on the chemistry of self‐immolative linkers is used to communicate information across the lipid bilayer, for transmembrane activation of enzymatic activity. Abstract The design of artificial,
Ane Bretschneider Søgaard +7 more
wiley +1 more source
Single-cell transcriptomic profiling unravels the adenoma-initiation role of protein tyrosine kinases during colorectal tumorigenesis. [PDF]
Signal Transduct Target Ther, 2022 Zheng X +19 more
europepmc +1 more source
Toward Design Principles for Biomolecular Condensates for Metabolic Pathways
Advanced Biology, EarlyView.Biomolecular condensates are membrane‐less compartments found through‐out nature which can serve as reaction crucibles for biochemical processes. This review explores the design strategies underlying how condensates can be used in biotechnology to enhance multistep enzyme cascades including enhancement by mass action and substrate channeling, and ...
Alain A.M. André +3 more
wiley +1 more source
Rule of five violations among the FDA-approved small molecule protein kinase inhibitors
Pharmacological Research, 2023 Because genetic alterations including mutations, overexpression, translocations, and dysregulation of protein kinases are involved in the pathogenesis of many illnesses, this enzyme family is the target of many drug discovery programs in the ...
Robert Roskoski, Jr.
doaj
Empowering AlphaFold2 for protein conformation selective drug discovery with AlphaFold2-RAVE [PDF]
Small molecule drug design hinges on obtaining co-crystallized ligand-protein structures. Despite AlphaFold2's strides in protein native structure prediction, its focus on apo structures overlooks ligands and associated holo structures. Moreover, designing selective drugs often benefits from the targeting of diverse metastable conformations. Therefore,
arxiv +1 more source
Chiral Engineered Biomaterials: New Frontiers in Cellular Fate Regulation for Regenerative Medicine
Advanced Functional Materials, EarlyView.Chiral engineered biomaterials can selectively influence cell behaviors in regenerative medicine. This review covers chiral engineered biomaterials in terms of their fabrication methods, cellular response mechanisms, and applications in directing stem cell differentiation and tissue function.
Yuwen Wang +5 more
wiley +1 more source