Optimization of 1,2,4-Triazole-Based p97 Inhibitors for the Treatment of Cancer

[1]  Kristijan Ramadan,et al.  Inhibitors of the ATPase p97/VCP: From basic research to clinical applications. , 2023, Cell chemical biology.

[2]  T. Chou,et al.  NMS-873 Leads to Dysfunctional Glycometabolism in A p97-Independent Manner in HCT116 Colon Cancer Cells , 2022, Pharmaceutics.

[3]  Murugaiah A. M. Subbaiah,et al.  Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design. , 2021, Journal of medicinal chemistry.

[4]  Y. Pommier,et al.  The ubiquitin-dependent ATPase p97 removes cytotoxic trapped PARP1 from chromatin , 2021, bioRxiv.

[5]  Lei Liu,et al.  Mechanistic insight into substrate processing and allosteric inhibition of human p97 , 2021, Nature Structural & Molecular Biology.

[6]  I. Cowell,et al.  A Role for VCP/p97 in the Processing of Drug-Stabilized TOP2-DNA Covalent Complexes , 2021, Molecular Pharmacology.

[7]  K. Palczewski,et al.  A p97/Valosin-Containing Protein Inhibitor Drug CB-5083 Has a Potent but Reversible Off-Target Effect on Phosphodiesterase-6 , 2021, The Journal of Pharmacology and Experimental Therapeutics.

[8]  T. Chou,et al.  AAA ATPases as therapeutic targets: Structure, functions, and small-molecule inhibitors. , 2021, European journal of medicinal chemistry.

[9]  S. Carr,et al.  Targeting acute myeloid leukemia dependency on VCP-mediated DNA repair through a selective second-generation small-molecule inhibitor , 2021, Science Translational Medicine.

[10]  Kathryn E. Hamilton,et al.  NMS-873 functions as a dual inhibitor of mitochondrial oxidative phosphorylation. , 2021, Biochimie.

[11]  S. Ciesek,et al.  Proteomics of SARS-CoV-2-infected host cells reveals therapy targets , 2020, Nature.

[12]  P. Wipf,et al.  p97: An Emerging Target for Cancer, Neurodegenerative Diseases and Viral Infections. , 2020, Journal of medicinal chemistry.

[13]  T. Chou,et al.  Allosteric p97 Inhibitors Can Overcome Resistance to ATP‐Competitive p97 Inhibitors for Potential Anticancer Therapy , 2020, ChemMedChem.

[14]  T. Talele Acetylene Group, Friend or Foe in Medicinal Chemistry. , 2020, Journal of medicinal chemistry.

[15]  Xu Zhou,et al.  Identification of NMS‐873, an allosteric and specific p97 inhibitor, as a broad antiviral against both influenza A and B viruses , 2019, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.

[16]  P. Wipf,et al.  Optimization of Phenyl Indole Inhibitors of the AAA+ ATPase p97 , 2018, ACS medicinal chemistry letters.

[17]  J. Prendergast,et al.  The host ubiquitin-dependent segregase VCP/p97 is required for the onset of human cytomegalovirus replication , 2017, PLoS pathogens.

[18]  A. Bartesaghi,et al.  2.3 Å resolution cryo-EM structure of human p97 and mechanism of allosteric inhibition , 2016, Science.

[19]  Vsevolod A. Peshkov,et al.  Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway. , 2016, ACS medicinal chemistry letters.

[20]  P. Wipf,et al.  Structure-Activity Study of Bioisosteric Trifluoromethyl and Pentafluorosulfanyl Indole Inhibitors of the AAA ATPase p97. , 2015, ACS medicinal chemistry letters.

[21]  A. Abdel-Magid Allosteric modulators: an emerging concept in drug discovery. , 2015, ACS medicinal chemistry letters.

[22]  A. Isacchi,et al.  Covalent and allosteric inhibitors of the ATPase VCP/p97 induce cancer cell death. , 2013, Nature chemical biology.

[23]  A. Isacchi,et al.  Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships. , 2013, Journal of medicinal chemistry.

[24]  Steven J Brown,et al.  Reversible inhibitor of p97, DBeQ, impairs both ubiquitin-dependent and autophagic protein clearance pathways , 2011, Proceedings of the National Academy of Sciences.

[25]  P. Prusis,et al.  Evaluation of the human prediction of clearance from hepatocyte and microsome intrinsic clearance for 52 drug compounds , 2010, Xenobiotica; the fate of foreign compounds in biological systems.

[26]  Edward H. Kerns,et al.  Automation in Pharmaceutical Profiling , 2005 .

[27]  K. Lindsten,et al.  Short-lived green fluorescent proteins for quantifying ubiquitin/proteasome-dependent proteolysis in living cells , 2000, Nature Biotechnology.