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Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue

Almaliti, Jehad Al-Hamashi, Ayad A. Negmeldin, Ahmed T. Hanigan, Christin L. Perera, Lalith Pflum, Mary Kay H. Casero, Robert A., Jr. Tillekeratne, L. M. Viranga

Journal of Medicinal Chemistry, 2016

https://doi.org/10.1021/acs.jmedchem.6b01271

Robert Casero

Casero Robert / Robert A. Casero, Jr.

ORCID: 0000-0001-5653-3306

Mammalian polyamine catabolism 10.1007/978-4-431-55212-3_5

Preface 10.1007/978-1-59745-145-1

Recent advances in the understanding of mammalian polyamine catabolism the regulation and potential role of polyamine catabolism in drug response and disease processes 10.1007/978-1-59745-145-1_12

Characterization of the interaction between the transcription factors human polyamine modulated factor (PMF-1) and NF-E2-related factor 2 (Nrf-2) in the transcriptional regulation of the spermidine/spermine N¹-acetyltransferase (SSAT) gene 10.1042/0264-6021:3550045

Polymeric Prodrugs Targeting Polyamine Metabolism Inhibit Zika Virus Replication 10.1021/acs.molpharmaceut.8b00068

Targeting polyamine metabolism and function in cancer and other hyperproliferative diseases 10.1038/nrd2243

Inhibitors of DNA Methylation, Histone Deacetylation, and Histone Demethylation. A Perfect Combination for Cancer Therapy. 10.1016/bs.acr.2016.01.007

Correction: Biochemical evaluation of the anticancer potential of the polyamine-based nanocarrier Nano11047 (PLoS ONE (2017) 12:4 (e0175917) DOI: 10.1371/journal.pone.0175917) 10.1371/journal.pone.0178102

Clinical aspects of cell death in breast cancer: The polyamine pathway as a new target for treatment 10.1677/erc.0.0060069

Decrease in acrolein toxicity based on the decline of polyamine oxidases 10.1016/j.biocel.2016.08.039

Targeting polyamine metabolism for cancer therapy and prevention 10.1042/BCJ20160383

Current status of the polyamine research field. 10.1007/978-1-61779-034-8_1

Coupling of the polyamine and iron metabolism pathways in the regulation of proliferation: Mechanistic links to alterations in key polyamine biosynthetic and catabolic enzymes 10.1016/j.bbadis.2018.05.007

The re-expression of the epigenetically silenced e-cadherin gene by a polyamine analogue lysine-specific demethylase-1 (LSD1) inhibitor in human acute myeloid leukemia cell lines 10.1007/s00726-013-1485-1

Ethanol‐Associated Alterations in the Kinetics of Putrescine Uptake and Metabolism by the Regenerating Liver 10.1111/j.1530-0277.1992.tb00626.x

Reduction of Murine Colon Tumorigenesis Driven by Enterotoxigenic Bacteroides fragilis Using Cefoxitin Treatment 10.1093/infdis/jiw069

Recent advances in the molecular biology of metazoan polyamine transport 10.1007/s00726-011-0987-y

Isolation of a polyamine transport deficient cell line from the human non-small cell lung carcinoma line NCI H157 10.1002/(SICI)1097-4652(199601)166:1<43::AID-JCP5>3.0.CO;2-G

Cloning and sequence analysis of the gene and cDNA encoding mouse spermidine/spermine N¹-acetyltransferase - a gene uniquely regulated by polyamines and their analogs 10.1016/0167-4781(93)90152-4

Distinct immunomodulatory effects of spermine oxidase in colitis induced by epithelial injury or infection 10.3389/fimmu.2018.01242

Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups 10.1016/j.ejmech.2014.09.009

Increased spermine oxidase expression in human prostate cancer and prostatic intraepithelial neoplasia tissues 10.1002/pros.20735

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Helicobacter pylori induces macrophage apoptosis by activation of arginase II 10.4049/jimmunol.168.9.4692

Synthesis and evaluation of a polyamine phosphinate and phosphonamidate as transition-state analogue inhibitors of spermidine/spermine-N¹-acetyltransferase 10.1016/0968-0896(96)00072-7

The role of the Polyamine catabolic enzymes SSAT and SMO In the synergistic effects of standard chemotherapeutic agents with a Polyamine analogue In human breast cancer cell lines 10.1007/s00280-009-1112-8

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Corrigendum to “Structure–activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures” [Bioorg. Med. Chem. 23 (2015) 1601–1612](S0968089615000735)(10.1016/j.bmc.2015.01.049) 10.1016/j.bmc.2018.05.032

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Differential transcription of the human spermidine/spermine N¹-acetyltransferase (SSAT) gene in human lung carcinoma cells 10.1042/bj3130691

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Biochemical evaluation of the anticancer potential of the polyamine-based nanocarrier Nano 11047 10.1371/journal.pone.0175917

The natural polyamine spermine functions directly as a free radical scavenger 10.1073/pnas.95.19.11140

Polyamine-modulated factor 1 binds to the human homologue of the 7a subunit of the Arabidopsis COP9 signalosome: Implications in gene expression 10.1042/BJ20020211

Stress induction of the spermidine/spermine N¹-acetyltransferase by a post-transcriptional mechanism in mammalian cells 10.1042/bj2940491

Distinct and sequential upregulation of genes regulating cell growth and cell cycle progression during hepatic ischemia-reperfusion injury 10.1152/ajpcell.00629.2004

Role of p53/p21^Waf1/Cip1 in the regulation of polyamine analogue-induced growth inhibition and cell death in human breast cancer cells 10.4161/cbt.4.9.1970

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Targeting the aryl hydrocarbon receptor/polyamine biosynthesis axis of evil for cancer therapy 10.1172/JCI123266

Spermine oxidase SMO(PAOh1), not N ¹ -acetylpolyamine oxidase PAO, is the primary source of Cytotoxic H 2 O 2 in polyamine analogue-treated human breast cancer cell lines 10.1074/jbc.M508177200

Elucidating the Structure of N¹-Acetylisoputreanine: A Novel Polyamine Catabolite in Human Urine 10.1021/acsomega.7b00872

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Mammalian polyamine catabolism: A therapeutic target, a pathological problem, or both? 10.1093/jb/mvj021

Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue 10.1021/acs.jmedchem.6b01271

Increased Helicobacter pylori-associated gastric cancer risk in the Andean region of Colombia is mediated by spermine oxidase 10.1038/onc.2014.273

Protective role of arginase in a mouse model of colitis 10.4049/jimmunol.173.3.2109

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A charge-deficient analogue of spermine with chelating properties 10.1007/s11171-005-0037-1

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Ahmed Negmeldin

Negmeldin Ahmed / Ahmed Thabet Negmeldin

ORCID: 0000-0003-3399-3435

Design, synthesis, and antitumor evaluation of novel pyrazolo[3,4-d]pyrimidine derivatives 10.3797/scipharm.1204-23

Structural Requirements of Histone Deacetylase Inhibitors: SAHA Analogs Modified on the Hydroxamic Acid 10.1002/ardp.201500472

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Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue 10.1021/acs.jmedchem.6b01271

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Molecular docking and statistical optimization of taurocholate-stabilized galactose anchored bilosomes for the enhancement of sofosbuvir absorption and hepatic relative targeting efficiency 10.1080/10717544.2020.1787557

Lalith Perera

Perera Lalith

ORCID: 0000-0003-0823-1631

https://www.niehs.nih.gov/research/atniehs/facilities/compmole/index.cfm

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Plasminogen alleles influence susceptibility to invasive aspergillosis 10.1371/journal.pgen.1000101

Predicted solution structure of zymogen human coagulation FVII 10.1002/jcc.1155

Proposed structural models of human factor Va and prothrombinase 10.1111/j.1538-7836.2007.02821.x

Reaction mechanism of the ε subunit of E. coli DNA polymerase III: Insights into active site metal coordination and catalytically significant residues 10.1021/ja8082818

Role of Water in the Hydration Force Acting between Lipid Bilayers 10.1021/la9515534

Simple formulas for improved point-charge electrostatics in classical force fields and hybrid quantum mechanical/molecular mechanical embedding 10.1002/qua.21675

Solution structure of the Dickerson DNA dodecamer containing a single ribonucleotide 10.1021/bi201710q

Spectral shifts and structural classes in microsolutions of rare gas clusters containing a molecular chromophore 10.1063/1.459686

Stabilization energies of Cl−, Br−, and I− ions in water clusters 10.1063/1.466096

Structural characterization of the conformational change in calbindin-D 28k upon calcium binding using differential surface modification analyzed by mass spectrometry 10.1021/bi900350q

Structure and Dynamics of Zymogen Human Blood Coagulation Factor X 10.1016/S0006-3495(02)75476-3

Structure and dynamics of Cl−(H2O)20 clusters: The effect of the polarizability and the charge of the ion 10.1063/1.462332

Structures of Cl−(H2O)n and F−(H2O)n (n=2,3,...,15) clusters. Molecular dynamics computer simulations 10.1063/1.466450

Surface solvation for an ion in a water cluster 10.1063/1.1829635

Template strand scrunching during DNA gap repair synthesis by human polymerase λ 10.1038/nsmb.1654

The discovery of new coding alleles of human CYP26A1 that are potentially defective in the metabolism of all-trans retinoic acid and their assessment in a recombinant cDNA expression system 10.1097/FPC.0b013e32801152d6

The solvation of Cl−, Br−, and I− in acetonitrile clusters: Photoelectron spectroscopy and molecular dynamics simulations 10.1063/1.472131

The structure of water at platinum/water interfaces Molecular dynamics computer simulations 10.1016/0039-6028(95)00449-1

Total synthesis and selective activity of a new class of conformationally restrained epothilones 10.1002/chem.200701143

Towards accurate solvation dynamics of divalent cations in water using the polarizable amoeba force field: From energetics to structure 10.1063/1.2234774

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Influence of Hydrophobic Cargo Binding on the Structure, Stability, and Allergenicity of the Cockroach Allergen Bla g 1 10.1016/j.jaci.2018.12.649

Transmembrane domain interactions and residue proline 378 are essential for proper structure, especially disulfide bond formation, in the human vitamin K-dependent γ-glutamyl carboxylase 10.1021/bi800235r

Ultrafast solvation dynamics in a Stockmayer fluid 10.1063/1.463826

What causes the enhancement of activity of factor VIIa by tissue factor? 10.1111/j.1538-7836.2006.02222.x

An Ancient Family of RNA-Binding Proteins: Still Important! 10.1016/j.tibs.2016.12.003

Binding of bisphenol A, bisphenol AF, and bisphenol S on the androgen receptor: Coregulator recruitment and stimulation of potential interaction sites 10.1016/j.tiv.2017.07.020

Identification of drivers for the metamorphic transition of HIV-1 reverse transcriptase 10.1042/BCJ20170480

Phosphorylated Nuclear Receptor CAR Forms a Homodimer To Repress Its Constitutive Activity for Ligand Activation 10.1128/MCB.00649-16

Revealing the role of the product metal in DNA polymerase beta catalysis 10.1093/nar/gkw1363

GATA3-dependent cellular reprogramming requires activation-domain dependent recruitment of a chromatin remodeler 10.1186/s13059-016-0897-0

Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue 10.1021/acs.jmedchem.6b01271

Reversal of DNA damage induced Topoisomerase 2 DNA-protein crosslinks by Tdp2 10.1093/nar/gkw228

Serological, genomic and structural analyses of the major mite allergen Der p 23 10.1111/cea.12680

Structural, Serological, and Genomic Analyses of the Major Mite Allergen Der p 23 10.1016/j.jaci.2015.12.1014

Asymmetric conformational maturation of HIV-1 reverse transcriptase 10.7554/eLife.06359

Functional Equivalence of an Evolutionarily Conserved RNA Binding Module 10.1074/jbc.M115.673012

GATA3 modulates chromatin structure to establish active enhancers in breast cancer cells 10.1158/1538-7445.AM2015-964

Requirement for transient metal ions revealed through computational analysis for DNA polymerase going in reverse 10.1073/pnas.1511207112

Uncovering the polymerase-induced cytotoxicity of an oxidized nucleotide 10.1038/nature13886

Applications of Quantum Mechanical/Molecular Mechanical Methods to the Chemical Insertion Step of DNA and RNA Polymerization 10.1016/bs.apcsb.2014.10.001

Characterization of an anti-Bla g 1 scFv: Epitope mapping and cross-reactivity 10.1016/j.molimm.2014.02.003

Molecular Mechanism of Substrate Specificity for Heparan Sulfate 2-O-Sulfotransferase 10.1074/jbc.M113.530535

Molecular mechanisms for the regulation of histone mRNA stem-loop-binding protein by phosphorylation 10.1073/pnas.1406381111

Mutational and Structural Analysis of the Tandem Zinc Finger Domain of Tristetraprolin 10.1074/jbc.M113.466326

Phylogenetic Distribution and Evolution of the Linked RNA-Binding and NOT1-Binding Domains in the Tristetraprolin Family of Tandem CCCH Zinc Finger Proteins 10.1089/jir.2013.0150

Synthesis and biological evaluation of largazole analogues with modified surface recognition cap groups 10.1016/j.ejmech.2014.09.009

The Drosophila Tis11 Protein and Its Effects on mRNA Expression in Flies 10.1074/jbc.M114.593491

Amino Acid Substitution in the Active Site of DNA Polymerase beta Explains the Energy Barrier of the Nucleotidyl Transfer Reaction 10.1021/ja403842j

Genomic, RNAseq, and Molecular Modeling Evidence Suggests That the Major Allergen Domain in Insects Evolved from a Homodimeric Origin 10.1093/gbe/evt182

Phenobarbital Indirectly Activates the Constitutive Active Androstane Receptor (CAR) by Inhibition of Epidermal Growth Factor Receptor Signaling 10.1126/scisignal.2003705

Study design of ASPirin in Reducing Events in the Elderly (ASPREE): A randomized, controlled trial 10.1016/j.cct.2013.09.014

Unusual Fragmentation Pathways in Collagen Glycopeptides 10.1007/s13361-013-0624-y

A ubiquitin-like domain is required for stabilizing the N-terminal ATPase module of human SMCHD1 10.1038/s42003-019-0499-y

Ligand induced dissociation of the AR homodimer precedes AR monomer translocation to the nucleus 10.1038/s41598-019-53139-9

Hydrophobic ligands influence the structure, stability, and processing of the major cockroach allergen Bla g 1 10.1038/s41598-019-54689-8

Preferential DNA Polymerase β Reverse Reaction with Imidodiphosphate 10.1021/acsomega.0c01345

Cryo-EM Structures of the SARS-CoV-2 Endoribonuclease Nsp15 10.1101/2020.08.11.244863

Potential SARS-CoV-2 main protease inhibitors 10.1016/j.drudis.2020.12.005

Cryo-EM structures of the SARS-CoV-2 endoribonuclease Nsp15 reveal insight into nuclease specificity and dynamics 10.1038/s41467-020-20608-z

NCX-4040, a Unique Nitric Oxide Donor, Induces Reversal of Drug-Resistance in Both ABCB1- and ABCG2-Expressing Multidrug Human Cancer Cells 10.3390/cancers13071680

jehad almaliti

almaliti jehad

ORCID: 0000-0002-3562-0846

Apratoxin Kills Cells by Direct Blockade of the Sec61 Protein Translocation Channel 10.1016/j.chembiol.2016.04.008

Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria 10.1021/acs.jnatprod.5b00301

Natural products inspired synthesis of neuroprotective agents against H2O2-induced cell death 10.1016/j.bmcl.2013.01.013

Dudawalamides A–D, Antiparasitic Cyclic Depsipeptides from the Marine Cyanobacterium Moorea producens 10.1021/acs.jnatprod.7b00034

Discovery and Synthesis of Caracolamide A, an Ion Channel Modulating Dichlorovinylidene Containing Phenethylamide from a Panamanian Marine Cyanobacterium cf. Symploca Species 10.1021/acs.jnatprod.7b00367

20S proteasome as a drug target in Trichomonas vaginalis 10.1128/AAC.00448-19

Untargeted mass spectrometry-based metabolomics approach unveils molecular changes in raw and processed foods and beverages 10.1016/j.foodchem.2019.125290

Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity 10.1021/acs.jmedchem.7b00671

The Proteasome as a Drug Target in the Metazoan Pathogen, Schistosoma mansoni 10.1021/acsinfecdis.9b00237

Exploration of the carmaphycins as payloads in antibody drug conjugate anticancer agents 10.1016/j.ejmech.2018.10.024

Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and Trypanosoma cruzi Cruzain 10.1021/acs.jmedchem.9b00294

Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue 10.1021/acs.jmedchem.6b01271