Structurally Diverse Histone Deacetylase Photoreactive Probes: Design, Synthesis, and Photolabeling Studies in Live Cells and Tissue.
Shaimaa M Aboukhatwa, Thomas W Hanigan, Taha Y Taha, Jayaprakash Neerasa, Rajeev Ranjan, Eman E El-Bastawissy, Mohamed A Elkersh, Tarek F El-Moselhy, Jonna Frasor, Nadim Mahmud and 2 more
Article in ChemMedChem, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.3field-weighted citation impact, top 41% of its field
1 · What the graph read from it
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
2 · The registry
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
3 · Its place in the literature
Who cites it
2 citing papers in PubMed, 7 citations in OpenAlex.
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
5 · Who and what money
Authors and funding
12 authors at 3 institutions in 2 countries.
Shaimaa M AboukhatwaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.ORCID 0000-0002-5013-7158
Thomas W HaniganDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Taha Y TahaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.ORCID 0000-0002-7344-7490
Jayaprakash NeerasaDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Rajeev RanjanSection of Hematology/Oncology, College of Medicine, University of Illinois at Chicago, Chicago, IL, 60612, USA.
Eman E El-BastawissyDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Tanta University, Tanta, 31527, Egypt.
Mohamed A ElkershDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Tanta University, Tanta, 31527, Egypt.
Tarek F El-MoselhyDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, Tanta University, Tanta, 31527, Egypt.
Jonna FrasorDepartment of Physiology and Biophysics, College of Medicine, University of Illinois at Chicago, Chicago, IL, 60612, USA.
Nadim MahmudSection of Hematology/Oncology, College of Medicine, University of Illinois at Chicago, Chicago, IL, 60612, USA.ORCID 0000-0003-3113-9155
Alan McLachlanDepartment of Microbiology and Immunology, College of Medicine, University of Illinois at Chicago, Chicago, IL, 60612, USA.ORCID 0000-0002-4168-2365
Pavel A PetukhovDepartment of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.ORCID 0000-0003-1554-242X
University of Illinois Chicago · USTanta University · EGPharos University in Alexandria · EG
Funding
Developmental regulation of HBV biosynthesis by FoxA and DNA methylationR01AI125401 · NIAID · UNIVERSITY OF ILLINOIS AT CHICAGO · PI MCLACHLAN, ALAN · 2016 to 2020
$2.0M
Liver lobule zonation, hepatocellular carcinoma (HCC) and β-catenin mediated hepatitis B virus (HBV) biosynthesisR01CA238328 · NCI · UNIVERSITY OF ILLINOIS AT CHICAGO · PI MCLACHLAN, ALAN · 2020 to 2024
$1.8M
Generating Human Cord-Blood-Derived Functional Megakaryocytes and platelets.R01HL130760 · NHLBI · UNIVERSITY OF ILLINOIS AT CHICAGO · PI MAHMUD, NADIM, MILLER, WILLIAM M · 2015 to 2018
$1.7M
Photoaffinity labeling probes for development of novel isoform selective HDAC inhR01CA131970 · NCI · UNIVERSITY OF ILLINOIS AT CHICAGO · PI PETUKHOV, PAVEL A · 2008 to 2011
$1.3M
Photoreactive histone deacetylase probes for chromatin immunoprecipitation in canR21CA183627 · NCI · UNIVERSITY OF ILLINOIS AT CHICAGO · PI FRASOR, JONNA, PETUKHOV, PAVEL A · 2014 to 2016
Histone deacetylase (HDAC) activity is modulated in vivo by post-translational modifications and formation of multiprotein complexes. Novel chemical tools to study how these factors affect engagement of HDAC isoforms by HDAC inhibitors (HDACi) in cells and tissues are needed. In this study, a synthetic strategy to access chemically diverse photoreactive probes (PRPs) was developed and used to prepare seven novel HDAC PRPs 9-15. The class I HDAC isoform engagement by PRPs was determined in biochemical assays and photolabeling experiments in live SET-2, HepG2, HuH7, and HEK293T cell lines and in mouse liver tissue. Unlike the HDAC protein abundance and biochemical activity against recombinant HDACs, the chemotype of the PRPs and the type of cells were key in defining the engagement of HDAC isoforms in live cells. Our findings suggest that engagement of HDAC isoforms by HDACi in vivo may be substantially modulated in a cell- and tissue-type-dependent manner.
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.
Structurally Diverse Histone Deacetylase Photoreactive Probes: Design, Synthesis, and Photolabeling Studies in Live Cells and Tissue. · full record | OpenQuestion