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Structure–Activity Relationship Studies of Venglustat on NTMT1 Inhibition

Journal Article · · Journal of Medicinal Chemistry
 [1];  [1];  [1];  [2];  [1]
  1. Department of Medicinal Chemistry and Molecular Pharmacology, Center for Cancer Research, Institute for Drug Discovery, Purdue University, West Lafayette, Indiana 47907, United States
  2. Department of Biological Sciences, Markey Center for Structural Biology, and the Purdue Institute of Inflammation, Immunology and Infectious Disease, Purdue University, West Lafayette, Indiana 47907, United States

Not provided.

Research Organization:
Argonne National Laboratory (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
USDOE
DOE Contract Number:
AC02-06CH11357
OSTI ID:
2423664
Journal Information:
Journal of Medicinal Chemistry, Journal Name: Journal of Medicinal Chemistry Journal Issue: 2 Vol. 66; ISSN 0022-2623
Publisher:
American Chemical Society (ACS)
Country of Publication:
United States
Language:
English

References (37)

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α-amino trimethylation of CENP-A by NRMT is required for full recruitment of the centromere journal March 2017
NRMT is an α-N-methyltransferase that methylates RCC1 and retinoblastoma protein journal August 2010
A glutamate/aspartate switch controls product specificity in a protein arginine methyltransferase journal February 2016
Improved Cell-Potent and Selective Peptidomimetic Inhibitors of Protein N-Terminal Methyltransferase 1 journal February 2022
Identification of Protein N-Terminal Methyltransferases in Yeast and Humans journal June 2010
NRMT1 knockout mice exhibit phenotypes associated with impaired DNA repair and premature aging journal March 2015
Structure-based Discovery of Cell-Potent Peptidomimetic Inhibitors for Protein N-Terminal Methyltransferase 1 journal March 2021
CREB-mediated transcriptional activation of NRMT1 drives muscle differentiation journal May 2021
Knockdown of NRMT enhances sensitivity of retinoblastoma cells to cisplatin through upregulation of the CENPA/Myc/Bcl2 axis journal January 2022
Versatile Catalysts for the Suzuki Cross-Coupling of Arylboronic Acids with Aryl and Vinyl Halides and Triflates under Mild Conditions journal May 2000
Selective Peptidomimetic Inhibitors of NTMT1/2: Rational Design, Synthesis, Characterization, and Crystallographic Studies journal July 2020
Regulation of transcription factor activity by interconnected post-translational modifications journal February 2014
A Transient Kinetic Analysis of PRMT1 Catalysis journal July 2011
Tazemetostat: EZH2 Inhibitor journal March 2022
The DNA damage response pathways: at the crossroad of protein modifications journal December 2007
Venglustat Inhibits Protein N-Terminal Methyltransferase 1 in a Substrate-Competitive Manner journal September 2022
Design, synthesis, and kinetic analysis of potent protein N-terminal methyltransferase 1 inhibitors journal January 2015
Emerging roles of post‐translational modifications in signal transduction and angiogenesis journal October 2014
Incorporation of Fluorescence Ceramide-Based HPLC Assay for Rapidly and Efficiently Assessing Glucosylceramide Synthase In Vivo journal June 2017
Ueber Verbindungen des Thiazols (Pyridins der Thiophenreihe) journal July 1887
(R)-PFI-2 is a potent and selective inhibitor of SETD7 methyltransferase activity in cells journal August 2014
Discovery of Bisubstrate Inhibitors of Nicotinamide N -Methyltransferase (NNMT) journal January 2018
Discovery of Bisubstrate Inhibitors for Protein N-Terminal Methyltransferase 1 journal February 2019
N-terminal α-methylation of RCC1 is necessary for stable chromatin association and normal mitosis journal April 2007
N-degron and C-degron pathways of protein degradation journal January 2019
Structural Biology of Human H3K9 Methyltransferases journal January 2010
Facile synthesis of SAM–peptide conjugates through alkyl linkers targeting protein N-terminal methyltransferase 1 journal January 2016
Past, present, and perspectives of protein N-terminal methylation journal August 2021
Structural basis for substrate recognition by the human N-terminal methyltransferase 1 journal November 2015
An asparagine/glycine switch governs product specificity of human N-terminal methyltransferase NTMT2 journal November 2018
Methyltransferase-like protein 11A promotes migration of cervical cancer cells via up-regulating ELK3 journal October 2021
Probing the Plasticity in the Active Site of Protein N-terminal Methyltransferase 1 Using Bisubstrate Analogues journal July 2020
α-N-Methylation of Damaged DNA-binding Protein 2 (DDB2) and Its Function in Nucleotide Excision Repair journal June 2014
Post-translational Modifications of RNA-Binding Proteins and their Roles in RNA Granules journal July 2012
The Promise for Histone Methyltransferase Inhibitors for Epigenetic Therapy in Clinical Oncology: A Narrative Review journal May 2020

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