Results 141 to 150 of about 2,071 (166)
Small molecule inhibition of protein depalmitoylation as a new approach towards downregulation of oncogenic Ras signalling [PDF]
Bioorganic and Medicinal Chemistry, 2011 The H- and N-Ras GTPases are prominent examples of proteins, whose localizations and signalling capacities are regulated by reversible palmitoylations and depalmitoylations. Recently, the novel small molecule inhibitor palmostatin B has been described to
Frank Dekker, Christian Hedberg
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Depalmitoylation rewires FLT3-ITD signaling and exacerbates leukemia progression
Blood, 2021 Abstract Internal tandem duplication within FLT3 (FLT3-ITD) is one of the most frequent mutations in acute myeloid leukemia (AML) and correlates with a poor prognosis. Whereas the FLT3 receptor tyrosine kinase is activated at the plasma membrane to transduce PI3K/AKT and RAS/MAPK signaling, FLT3-ITD resides in the endoplasmic ...
Xu Han, Kaosheng Lv, Wei Tong
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Effects of Depalmitoylation on Physicochemical Properties of Rhodopsin
Biochemistry, 1994In an effort to determine the functionality of palmitoylation in rhodopsin, a number of physicochemical properties of depalmitoylated rhodopsin were monitored. Approximately 70% of the rhodopsin was depalmitoylated in rod outer segments by a mild hydroxylamine treatment that resulted in minimal bleaching of rhodopsin.
T Gregory Dewey
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FKBP12 Binds to Acylated H-Ras and Promotes Depalmitoylation [PDF]
Molecular Cell, 2011 A cycle of palmitoylation/depalmitoylation of H-Ras mediates bidirectional trafficking between the Golgi apparatus and the plasma membrane, but nothing is known about how this cycle is regulated. We show that the prolyl isomerase (PI) FKBP12 binds to H-Ras in a palmitoylation-dependent fashion and promotes depalmitoylation.
Frederick Tsai, Mo Zhou, Philips Mark
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Targeting LYPLAL1-mediated cGAS depalmitoylation enhances the response to anti-tumor immunotherapy
Molecular Cell, 2023 Cyclic GMP-AMP synthase (cGAS) binds pathogenic and other cytoplasmic double-stranded DNA (dsDNA) to catalyze the synthesis of cyclic GMP-AMP (cGAMP), which serves as the secondary messenger to activate the STING pathway and innate immune responses.
Weichao Dan
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A fluorescent probe for cysteine depalmitoylation reveals dynamic APT signaling [PDF]
Nature Chemical Biology, 2016 Hundreds of human proteins are modified by reversible palmitoylation of cysteine residues (S-palmitoylation), but the regulation of depalmitoylation is poorly understood. Here, we develop 'depalmitoylation probes' (DPPs), small-molecule fluorophores, to monitor the endogenous activity levels of 'erasers' of S-palmitoylation, acylprotein thioesterases ...
Rahul Singh Kathayat, Bryan Dickinson
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Enzymatic protein depalmitoylation by acyl protein thioesterases
Biochemical Society Transactions, 2015Protein palmitoylation is a dynamic post-translational modification, where the 16-carbon fatty acid, palmitate, is added to cysteines of proteins to modulate protein sorting, targeting and signalling. Palmitate removal from proteins is mediated by acyl protein thioesterases (APTs).
David T S, Lin, Elizabeth, Conibear
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Targeting the Ras palmitoylation/depalmitoylation cycle in cancer
Biochemical Society Transactions, 2017The Ras proteins are well-known drivers of many cancers and thus represent attractive targets for the development of anticancer therapeutics. Inhibitors that disrupt the association of the Ras proteins with membranes by blocking the addition of the farnesyl lipid moiety to the Ras C-terminus failed in clinical trials.
David Tse Shen, Lin +2 more
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Measuring S-Depalmitoylation Activity In Vitro and In Live Cells with Fluorescent Probes [PDF]
Methods in Molecular Biology, 2019 S-palmitoylation is a reversible lipid posttranslational modification (PTM) that can mediate protein localization, trafficking, interaction with membranes, and a host of other biophysical characteristics. Over the past decade, a suite of chemoproteomic strategies have uncovered the breadth of S-palmitoylation, revealing widespread susceptibility to ...
Rahul Singh Kathayat, Bryan Dickinson
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Protein Depalmitoylation Is Induced by Wnt5a and Promotes Polarized Cell Behavior [PDF]
Journal of Biological Chemistry, 2015 Wnt5a signaling regulates polarized cell behavior, but the downstream signaling events that promote cell polarity are not well understood. Our results show that Wnt5a promotes depalmitoylation of the melanoma cell adhesion molecule (MCAM) at cysteine 590.
Eric Witze
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