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Relevant bibliographies by topics / ATP-competitive

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Journal articles

Academic literature on the topic 'ATP-competitive'

Author: Grafiati

Published: 1 April 2023

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Journal articles on the topic "ATP-competitive"

1

Lebakken, Connie S., Laurie J. Reichling, Jason M. Ellefson, and Steven M. Riddle. "Detection of Allosteric Kinase Inhibitors by Displacement of Active Site Probes." Journal of Biomolecular Screening 17, no. 6 (2012): 813–21. http://dx.doi.org/10.1177/1087057112439889.

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Non–adenosine triphosphate (ATP) competitive, allosteric inhibitors provide a promising avenue to develop highly selective small-molecule kinase inhibitors. Although this class of compounds is growing, detection of such inhibitors can be challenging as standard kinase activity assays preferentially detect compounds that bind to active kinases in an ATP competitive manner. We have previously described a time-resolved fluorescence resonance energy transfer (TR-FRET)–based kinase binding assay using the competitive displacement of ATP competitive active site fluorescent probes (“tracers”). Although this format has gained acceptance, published data with this and related formats are almost entirely without examples of non-ATP competitive compounds. Thus, this study addresses whether this format is useful for non-ATP competitive inhibitors. To this end, 15 commercially available non-ATP competitive inhibitors were tested for their ability to displace ATP competitive probes. Despite the diversity of both compound structures and their respective targets, 14 of the 15 compounds displaced the tracers with IC50 values comparable to literature values. We conclude that such binding assays are well suited for the study of non-ATP competitive inhibitors. In addition, we demonstrate that allosteric inhibitors of BCR-Abl and MEK bind preferentially to the nonphosphorylated (i.e., inactive) form of the kinase, indicating that binding assays may be a preferred format in some cases.

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2

Agius, Michael P., Kristin Ko, Taylor K. Johnson, Sameer Phadke, and Matthew B. Soellner. "Conformation-tunable ATP-competitive kinase inhibitors." Chemical Communications 58, no. 21 (2022): 3541–44. http://dx.doi.org/10.1039/d1cc06893h.

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3

Garuti, L., M. Roberti, and G. Bottegoni. "Non-ATP Competitive Protein Kinase Inhibitors." Current Medicinal Chemistry 17, no. 25 (2010): 2804–21. http://dx.doi.org/10.2174/092986710791859333.

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4

Lee, Byung-Il, Hyung-Jun Ahn, Ki-Cheol Han, Dae-Ro Ahn, and Dong-Yun Shin. "Pyrogallin, an ATP-Competitive Inhibitor of JAK3." Bulletin of the Korean Chemical Society 32, no. 3 (2011): 1077–79. http://dx.doi.org/10.5012/bkcs.2011.32.3.1077.

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5

Schenone, S., C. Brullo, F. Musumeci, M. Radi, and M. Botta. "ATP-Competitive Inhibitors of mTOR: An Update." Current Medicinal Chemistry 18, no. 20 (2011): 2995–3014. http://dx.doi.org/10.2174/092986711796391651.

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6

Lazaro, Glorianne, Eleftherios Kostaras, and Igor Vivanco. "Inhibitors in AKTion: ATP-competitive vs allosteric." Biochemical Society Transactions 48, no. 3 (2020): 933–43. http://dx.doi.org/10.1042/bst20190777.

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Aberrant activation of the PI3K pathway is one of the commonest oncogenic events in human cancer. AKT is a key mediator of PI3K oncogenic function, and thus has been intensely pursued as a therapeutic target. Multiple AKT inhibitors, broadly classified as either ATP-competitive or allosteric, are currently in various stages of clinical development. Herein, we review the evidence for AKT dependence in human tumours and focus on its therapeutic targeting by the two drug classes. We highlight the future prospects for the development and implementation of more effective context-specific AKT inhibitors aided by our increasing knowledge of both its regulation and some previously unrecognised non-canonical functions.

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7

Parrish, Cynthia A., Nicholas D. Adams, Kurt R. Auger, et al. "Novel ATP-Competitive Kinesin Spindle Protein Inhibitors." Journal of Medicinal Chemistry 50, no. 20 (2007): 4939–52. http://dx.doi.org/10.1021/jm070435y.

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8

Ito, Masahiro, Misa Iwatani, Yusuke Kamada, et al. "Discovery of selective ATP-competitive eIF4A3 inhibitors." Bioorganic & Medicinal Chemistry 25, no. 7 (2017): 2200–2209. http://dx.doi.org/10.1016/j.bmc.2017.02.035.

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9

Zarębska, Ewa A., Krzysztof Kusy, Ewa M. Słomińska, Łukasz Kruszyna, and Jacek Zieliński. "Plasma Nucleotide Dynamics during Exercise and Recovery in Highly Trained Athletes and Recreationally Active Individuals." BioMed Research International 2018 (October 9, 2018): 1–11. http://dx.doi.org/10.1155/2018/4081802.

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Circulating plasma ATP is able to regulate local skeletal muscle blood flow and 02 delivery causing considerable vasodilatation during exercise. We hypothesized that sport specialization and specific long-term training stimuli have an impact on venous plasma [ATP] and other nucleotides concentration. Four athletic groups consisting of sprinters (n=11; age range 21–30 yr), endurance-trained athletes (n=16; age range 18–31 yr), futsal players (n=14; age range 18–30 yr), and recreationally active individuals (n=12; age range 22–33 yr) were studied. Venous blood samples were collected at rest, during an incremental treadmill test, and during recovery. Baseline [ATP] was 759±80 nmol·l−1 in competitive athletes and 680±73 nmol·l−1 in controls and increased during exercise by ~61% in competitive athletes and by ~31% in recreationally active participants. We demonstrated a rapid increase in plasma [ATP] at exercise intensities of 83–87% of VO2max in competitive athletes and 94% in controls. Concentrations reported after 30 minutes of recovery were distinct from those obtained preexercise in competitive athletes (P<0.001) but not in controls (P=0.61). We found a correlation between total-body skeletal muscle mass and resting and maximal plasma [ATP] in competitive athletes (r=0.81 and r=0.75, respectively). In conclusion, sport specialization is significantly related to plasma [ATP] at rest, during exercise, and during maximal effort. Intensified exercise-induced plasma [ATP] increases may contribute to more effective vessel dilatation during exercise in highly trained athletes than in recreational runners. The most rapid increase in ATP concentration was associated with the respiratory compensation point. No differences between groups of competitive athletes were observed during the recovery period suggesting a similar pattern of response after exercise. Total-body skeletal muscle mass is indirectly related to plasma [ATP] in highly trained athletes.

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10

Lyle, S., D. H. Geller, K. Ng, J. Stanczak, J. Westley, and N. B. Schwartz. "Kinetic mechanism of adenosine 5′-phosphosulphate kinase from rat chondrosarcoma." Biochemical Journal 301, no. 2 (1994): 355–59. http://dx.doi.org/10.1042/bj3010355.

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Biosynthesis of the activated sulphate donor adenosine 3′-phosphate 5′-phosphosulphate (PAPS) involves the sequential action of two enzyme activities. ATP-sulphurylase catalyses the formation of APS (adenosine 5′-phosphosulphate) from ATP and free sulphate, and APS is then phosphorylated by APS kinase to produce PAPS. Initial-velocity patterns for rat chondrosarcoma APS kinase indicate a single-displacement formal mechanism with KmAPS 76 nM and KmATP = 24 microM. Inhibition studies using analogues of substrates and products were carried out to determine the reaction mechanism. An analogue of PAPS, adenosine 3′-phosphate 5′-[beta-methylene]phosphosulphate, exhibited competitive inhibition with APS and non-competitive inhibition with ATP. An analogue of APS, adenosine 5′-[beta-methylene]phosphosulphate was also competitive with APS and non-competitive with ATP. Adenosine 5′-[beta gamma-imido]triphosphate showed competitive inhibition with respect to ATP and produced mixed-type inhibition, with a pronounced intercept effect and a small slope effect, with respect to APS. These results are in accord with the formulation of the predominant pathway as a steady-state ordered mechanism with APS as the leading substrate and PAPS as the final product released.

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