Correction: Chapman, E.; et al. Inhibitors of the AAA+ Chaperone p97. Molecules 2015, 20, 3027-3049

Chapman, Eli; Maksim, Nick; Cruz, Fabian De La; Clair, James J. La

doi:10.3390/molecules20034357

Cited by 4 publications

(5 citation statements)

References 1 publication

Supporting

Mentioning

Contrasting

Order By: Relevance

“…One p97 inhibitor, CB‐5083, is currently under investigation in two phase 1 human clinical trials for cancer patients: one in patients with advanced solid tumors (NCT02243917), and the other in patients with relapsed multiple myeloma (NCT02223598). Different classes of p97 inhibitors have been developed, and CB‐5083 is the first p97 inhibitor to enter clinical trials.…”

Section: Figurementioning

confidence: 99%

“…More than 30 p97 cofactors are known . Although great effort has been taken to screen for p97 inhibitors, and effects of cofactors on p97 have been studied, only recently have the effects of cofactors on the potencies of p97 inhibitors begun to be investigated. We found that inhibition of p97 ATPase activity by ATP‐competitive and D2‐selective p97 inhibitors, ML240 and ML241, is drastically changed by p47, a major p97 cofactor.…”

Section: Figurementioning

confidence: 99%

See 1 more Smart Citation

Evaluating p97 Inhibitor Analogues for Potency against p97–p37 and p97–Npl4–Ufd1 Complexes

Gui

Zhang

et al. 2016

ChemMedChem

View full text Add to dashboard Cite

We previously found that the p97 cofactor, p47, significantly decreased the potency of some ATP-competitive p97 inhibitors such as ML240 [2-(2-amino-1H-benzo[d]imidazol-1-yl)-N-benzyl-8-methoxyquinazolin-4-amine] and ML241 [2-(2H-benzo[b][1,4]oxazin-4(3H)-yl)-N-benzyl-5,6,7,8 tetrahydroquinazolin-4-amine]. In this study, we aimed to evaluate inhibitor potencies against two additional p97 cofactor complexes, p97-p37 and p97-Npl4-Ufd1. We focused on these two cofactor complexes, because the protein sequence of p37 is 50 % identical to that of p47, and the Npl4-Ufd1 heterodimer (NU) is the most-studied p97 cofactor complex. We screened 200 p97 inhibitor analogues for their ability to inhibit the ATPase activity of p97 alone and of p97-p37 and p97-NU complexes. In contrast to the effect of p47, p37 and NU did not significantly change the potencies of most of the compounds. These results highlight differences among p97 cofactors in influencing p97 conformation and effects of inhibitors on p97 complexes, as compared to p97 alone. Continued efforts are needed to advance the development of complex-specific p97 inhibitors.

show abstract

Section: Figurementioning

confidence: 99%

Section: Figurementioning

confidence: 99%

Evaluating p97 Inhibitor Analogues for Potency against p97–p37 and p97–Npl4–Ufd1 Complexes

Gui

Zhang

et al. 2016

ChemMedChem

View full text Add to dashboard Cite

show abstract

“…A number of systematic comparisons of foreground mitigation methods have been performed. Chapman et al (2015) compared foreground subtraction methods and found that GMCA proves the most robust to realistic foreground spectra. Alonso et al (2015a) unified a number of subtraction methods under a common mathematical framework and showed that for a large suite of fast simulations the methods perform comparably.…”

Section: Discussionmentioning

confidence: 99%

“…The most well-known implementations of this approach are fast independent component analysis (Chapman et al 2012) and generalised morphological component analysis (GMCA;Chapman et al 2013). The latter appears to be the most robust approach in the foreground subtraction category (Chapman et al 2015) and has been used as part of the LOFAR EoR pipeline (Patil et al 2017).…”

Section: Foreground Subtractionmentioning

confidence: 99%

Fundamental physics with the Square Kilometre Array

Weltman

Bull

Camera

et al. 2020

Publ. Astron. Soc. Aust.

314

169

View full text Add to dashboard Cite

The Square Kilometre Array (SKA) is a planned large radio interferometer designed to operate over a wide range of frequencies, and with an order of magnitude greater sensitivity and survey speed than any current radio telescope. The SKA will address many important topics in astronomy, ranging from planet formation to distant galaxies. However, in this work, we consider the perspective of the SKA as a facility for studying physics. We review four areas in which the SKA is expected to make major contributions to our understanding of fundamental physics: cosmic dawn and reionisation; gravity and gravitational radiation; cosmology and dark energy; and dark matter and astroparticle physics. These discussions demonstrate that the SKA will be a spectacular physics machine, which will provide many new breakthroughs and novel insights on matter, energy, and spacetime.

show abstract

“…So far, several inhibitors have been reported to inhibit VCP function (30,31). Previously, Sasazawa et al (20) showed that xanthohumol is a VCP inhibitor by binding to the N-terminal domain of VCP.…”

Section: Inhibitor Of Vcp-dependent Fibroblast Migrationmentioning

confidence: 99%

A small-molecule ligand of valosin-containing protein/p97 inhibits cancer cell–accelerated fibroblast migration

Suvarna

Honda

Muroi

et al. 2019

Journal of Biological Chemistry

View full text Add to dashboard Cite

Edited by George N. DeMartino Carcinoma-associated fibroblasts are fibroblasts activated by surrounding cancer cells. Carcinoma-associated fibroblasts exhibit enhanced cell migration, which plays an important role in cancer metastasis. Previously, we demonstrated enhanced migration of NIH3T3 fibroblasts when they were cultured in the presence of MCF7 breast cancer cells. Human fibroblasts displayed a similar phenomenon even when they were co-cultured with cancer cells other than MCF7 cells. In this study, we screened ϳ16,000 compounds from the RIKEN Natural Products Depository chemical library for inhibitors of enhanced NIH3T3 cell migration in the presence of MCF7. We identified NPD8733 as an inhibitor of cancer cell-enhanced fibroblast migration. This inhibition was observed not only in a woundhealing co-culture assay but also in a Transwell migration assay. Using NPD8733 and a structurally similar but inactive derivative, NPD8126, on immobilized beads, we found that NPD8733, but not NPD8126, specifically binds to valosin-containing protein (VCP)/p97, a member of the ATPase-associated with diverse cellular activities (AAA؉) protein family. Using VCP truncation variants, we found that NPD8733 binds to the D1 domain of VCP. Because VCP's D1 domain is important for its function, we concluded that NPD8733 may act on VCP by binding to this domain. siRNA-mediated silencing of VCP in NIH3T3 fibroblasts, but not in MCF7 cells, reduced the migration of the co-cultured NIH3T3 fibroblasts. These results indicate that MCF7 activates the migration of NIH3T3 cells through VCP and that NPD8733 binds VCP and thereby inhibits its activity.

show abstract

Correction: Chapman, E.; et al. Inhibitors of the AAA+ Chaperone p97. Molecules 2015, 20, 3027-3049

Abstract: The authors wish to make the following correction to paper [1], doi:10.3390/molecules20023027, website: http://www.mdpi.com/1420-3049/20/2/3027/. [...]

Cited by 4 publications

References 1 publication

Evaluating p97 Inhibitor Analogues for Potency against p97–p37 and p97–Npl4–Ufd1 Complexes

Evaluating p97 Inhibitor Analogues for Potency against p97–p37 and p97–Npl4–Ufd1 Complexes

Fundamental physics with the Square Kilometre Array

A small-molecule ligand of valosin-containing protein/p97 inhibits cancer cell–accelerated fibroblast migration

Contact Info

Product

Resources

About