Peripheral Inhibition of Small C‐terminal Domain Phosphatase 1 with Napthoquinone Analogues

Rallabandi, Harikrishna Reddy; Lee, Dongsun; Sung, Jinmo; Kim, Young Jun

doi:10.1002/est2.163

Cited by 1 publication

(2 citation statements)

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“…The N-terminal region of CTDSP1 is required for palmitoylation, to anchor proteins in the plasma membrane, and was identified as a potential targetable allosteric site of CTDSP1. A novel allosteric site may also be found through the [17,18,153] for targeting CTDSP1. The left square represents conventional docking, which targets the active site of human CTDSP1.…”

Section: Resultsmentioning

confidence: 99%

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Targeting the C-Terminal Domain Small Phosphatase 1

Rallabandi

Ganesan

Kim

2020

Life

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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.

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Section: Resultsmentioning

confidence: 99%

“…However, we agree that there could be yet unexplored, better docking methods than allosteric docking and ensemble docking in the targeting of CTDSP1. [17,18,153] for targeting CTDSP1. The left square represents conventional docking, which targets the active site of human CTDSP1.…”

Section: Challenges and Opportunities In Targeting Ctdsp1mentioning

confidence: 99%