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Targeting the C-Terminal Domain Small Phosphatase 1

Department of Medicinal Biosciences and Nanotechnology Research Center, Konkuk University, Chungju 27478, Korea
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Life 2020, 10(5), 57; https://doi.org/10.3390/life10050057
Received: 29 March 2020 / Revised: 5 May 2020 / Accepted: 7 May 2020 / Published: 8 May 2020
(This article belongs to the Section Biochemistry, Biophysics and Computational Biology)
The human C-terminal domain small phosphatase 1 (CTDSP1/SCP1) is a protein phosphatase with a conserved catalytic site of DXDXT/V. CTDSP1’s major activity has been identified as dephosphorylation of the 5th Ser residue of the tandem heptad repeat of the RNA polymerase II C-terminal domain (RNAP II CTD). It is also implicated in various pivotal biological activities, such as acting as a driving factor in repressor element 1 (RE-1)-silencing transcription factor (REST) complex, which silences the neuronal genes in non-neuronal cells, G1/S phase transition, and osteoblast differentiation. Recent findings have denoted that negative regulation of CTDSP1 results in suppression of cancer invasion in neuroglioma cells. Several researchers have focused on the development of regulating materials of CTDSP1, due to the significant roles it has in various biological activities. In this review, we focused on this emerging target and explored the biological significance, challenges, and opportunities in targeting CTDSP1 from a drug designing perspective. View Full-Text
Keywords: CTDSP1; drug design; allosteric docking; ensemble docking CTDSP1; drug design; allosteric docking; ensemble docking
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Rallabandi, H.R.; Ganesan, P.; Kim, Y.J. Targeting the C-Terminal Domain Small Phosphatase 1. Life 2020, 10, 57.

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