Conformational Entropy of FK506 Binding to FKBP12 Determined by Nuclear Magnetic Resonance Relaxation and Molecular Dynamics Simulations.
Sign Up to like & getrecommendations! Published in 2018 at "Biochemistry"
DOI: 10.1021/acs.biochem.7b01256
Abstract: FKBP12 (FK506 binding protein 12 kDa) is an important drug target. Nuclear magnetic resonance (NMR) order parameters, describing amplitudes of motion on the pico- to nanosecond time scale, can provide estimates of changes in conformational… read more here.
Keywords: fk506 binding; conformational entropy; fkbp12; nuclear magnetic ... See more keywords
Blocking the FKBP12 induced dendrimeric burst in aberrant aggregation of α-synuclein by using the ElteN378 synthetic inhibitor
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2019.1667342
Abstract: Abstract α-Synuclein (α-syn), a disordered cytoplasmatic protein, plays a fundamental role in the pathogenesis of Parkinson’s disease (PD). Here, we have shown, using photophysical measurements, that addition of FKBP12 to α-syn solutions, dramatically accelerates protein… read more here.
Keywords: blocking fkbp12; aggregation; synuclein; synthetic inhibitor ... See more keywords
FKBP12 binds to the cardiac ryanodine receptor with negative cooperativity: implications for heart muscle physiology in health and disease
Sign Up to like & getrecommendations! Published in 2023 at "Philosophical Transactions of the Royal Society B: Biological Sciences"
DOI: 10.1098/rstb.2022.0169
Abstract: Cardiac ryanodine receptors (RyR2) release the Ca2+ from intracellular stores that is essential for cardiac myocyte contraction. The ion channel opening is tightly regulated by intracellular factors, including the FK506 binding proteins, FKBP12 and FKBP12.6.… read more here.
Keywords: physiology; fkbp12; negative cooperativity; cardiac ryanodine ... See more keywords
Targeting the BMP Receptor Inhibitor FKBP12 to Upregulate Hepcidin in Wild-Type and Hemojuvelin-Hemochromatosis Models
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DOI: 10.1182/blood-2019-126496
Abstract: Introduction Iron homeostasis is tightly regulated by the liver hormone hepcidin, whose expression is controlled by the BMP-SMAD pathway. Activation of this pathway requires ligands (BMP2 and BMP6), type I (ALK2 and ALK3) and type… read more here.
Keywords: bmp smad; expression; hepcidin; mice ... See more keywords