Výsledky vyhledávání - "Zenon Konteatis"

Akademický článek

MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis

Autor: Katya Marjon, Michael J. Cameron, Phong Quang, Michelle F. Clasquin, Everton Mandley, Kaiko Kunii, Michael McVay, Sung Choe, Andrew Kernytsky, Stefan Gross, Zenon Konteatis, Joshua Murtie, Michelle L. Blake, Jeremy Travins, Marion Dorsch, Scott A. Biller, Kevin M. Marks

Publikováno v: Cell Reports, Vol 15, Iss 3, Pp 574-587 (2016)

Homozygous deletions of p16/CDKN2A are prevalent in cancer, and these mutations commonly involve co-deletion of adjacent genes, including methylthioadenosine phosphorylase (MTAP). Here, we used shRNA screening and identified the metabolic enzyme, met

Externí odkaz: https://doaj.org/article/bd77de65b22f4da89618bc5269d7f141

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Supplementary Figures 1 - 11 from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Supplementary Figure 1. Synthesis and pharmacokinetic characterization of AG-221. Supplementary Figure 2. Biochemical attributes of AG-221. Supplementary Figure 3. Biochemistry of AG-221 with respect to substrate and cofactor. Supplementary Figure 4.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::11d97954935b2f34d5dfe50e66a1f7f5
https://doi.org/10.1158/2159-8290.22531945.v1

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Supplementary Tables 1 - 8 from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Supplementary Table 1. Drug metabolism and pharmacokinetic attributes of AG-221. Supplementary Table 2. Selectivity of AG-221 confirmed by testing against a panel of kinases. Supplementary Table 3. Clinical characteristics of patients with IDH2R140Q-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9bd472a11c8ff29b3f26438ea494ea5d
https://doi.org/10.1158/2159-8290.22531936

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Supplementary Methods from AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic IDH2 Mutations

Supplementary Methods

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0bf9f6f1fb6d2a1049263137b504fc3a
https://doi.org/10.1158/2159-8290.22531939

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Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads

Publikováno v: Journal of medicinal chemistry. 65(6)

Inhibition of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6dd4665a566b3b92c2d5c0229953dea0
https://pubmed.ncbi.nlm.nih.gov/35293760

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Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous

Publikováno v: Journal of medicinal chemistry. 64(8)

The metabolic enzyme methionine adenosyltransferase 2A (MAT2A) was recently implicated as a synthetic lethal target in cancers with deletion of the methylthioadenosine phosphorylase (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::6ec9204e0504cb32589dbe975f9a1cd3
https://pubmed.ncbi.nlm.nih.gov/33829783

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AG-221, a First-in-Class Therapy Targeting Acute Myeloid Leukemia Harboring Oncogenic

Publikováno v: Cancer discovery. 7(5)

AG-221 or enasidenib is a first-in-class selective inhibitor of mutated isocitrate dehydrogenase 2 (IDH2) with early demonstrated clinical efficacy in acute myeloid leukemia as a single agent, yet with persistence of mutant IDH2 clones. Two papers in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::0d30618427a82a8efe6855ead5edc951
https://pubmed.ncbi.nlm.nih.gov/28461409

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Fragment and protein simulation methods in fragment based drug design

Autor: Anthony E. Klon, Jinming Zou, Zenon Konteatis, Siavash N. Meshkat, Charles H. Reynolds

Publikováno v: Drug Development Research. 72:130-137

Fragment-based drug design (FBDD) has become an important and successful approach to drug discovery. In this review, we discuss two classes of simulation technologies that we routinely employ as part our of computational FBDD efforts. The first class

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::136d12228975936aaf035b24bc8fb653
https://doi.org/10.1002/ddr.20409

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Transplant−Insert−Constrain−Relax−Assemble (TICRA): Protein−Ligand Complex Structure Modeling and Application to Kinases

Autor: Jeffrey S. Wiseman, Siavash Meshkat, Jinming Zou, Zenon Konteatis, Anthony E. Klon

Publikováno v: Journal of Chemical Information and Modeling. 51:52-60

We introduce TICRA (transplant-insert-constrain-relax-assemble), a method for modeling the structure of unknown protein-ligand complexes using the X-ray crystal structures of homologous proteins and ligands with known activity. We present results fro

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b904e9fe3582307a8728d8cca8b1d49c
https://doi.org/10.1021/ci100256u

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Developing technologies in biodefense research: computational drug design

Autor: Steven J. Freedman, Matthew Clark, Jinming Zou, Jeffrey S. Wiseman, Jennifer L. Ludington, George Talbot, Sia Meshkat, Zenon Konteatis

Publikováno v: Drug Development Research. 70:279-287

The development of small-molecule drugs to counter the threat of bioterrorism will differ from classical drug discovery because it will be impossible to evaluate efficacy in clinical trials for many agents. This difference focuses biodefense on the i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::78c08cdc8f5a8ea3d7b680d427268f69
https://doi.org/10.1002/ddr.20305

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