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
Robert Casero
Casero Robert / Robert A. Casero, Jr.
ORCID: 0000-0001-5653-3306
Mammalian polyamine catabolism 10.1007/978-4-431-55212-3_5
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
Knockdown of ornithine decarboxylase antizyme 1 causes loss of uptake regulation leading to increased N 1, N 11-bis(ethyl) norspermine (BENSpm) accumulation and toxicity in NCI H157 lung cancer cells 10.1007/s00726-011-1030-z
The novel polyamine analogue CGC-11093 enhances the antimyeloma activity of bortezomib 10.1158/0008-5472.CAN-07-6483
Cyclooxygenase-independent Induction of Apoptosis by Sulindac Sulfone Is Mediated by Polyamines in Colon Cancer 10.1074/jbc.M307265200
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
The role of spermidine/spermine N1-acetyltransferase in determining response to chemotherapeutic agents in colorectal cancer cells 10.1158/1535-7163.MCT-06-0303
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
Spermine oxidase is a regulator of macrophage host response to Helicobacter pylori: Enhancement of antimicrobial nitric oxide generation by depletion of spermine 10.1007/s00726-013-1531-z
The Effect of Polyamine Depletion on the Cytotoxic Response to PUVA, Gamma Rays, and UVC in V79 Cells in Vitro 10.1006/bbrc.1994.1661
DFMO and 5-azacytidine increase M1 macrophages in the tumor microenvironment of murine ovarian cancer 10.1158/0008-5472.CAN-18-4018
Id1 overexpression is independent of repression and epigenetic silencing of tumor suppressor genes in melanoma 10.4161/epi.5.5.11929
Polyamine metabolism and cancer: treatments, challenges and opportunities 10.1038/s41568-018-0050-3
L-arginine supplementation improves responses to injury and inflammation in dextran sulfate sodium colitis 10.1371/journal.pone.0033546
Differential transcription of the human spermidine/spermine N1-acetyltransferase (SSAT) gene in human lung carcinoma cells 10.1042/bj3130691
Spermine oxidase (SMO) activity in breast tumor tissues and biochemical analysis of the anticancer spermine analogues BENSpm and CPENSpm 10.1186/1471-2407-10-555
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/p21Waf1/Cip1 in the regulation of polyamine analogue-induced growth inhibition and cell death in human breast cancer cells 10.4161/cbt.4.9.1970
Difluoromethylornithine is a novel inhibitor of helicobacter pylori growth, cagA translocation, and interleukin-8 induction 10.1371/journal.pone.0017510
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
Characterization of a full-length cDNA which codes for the human spermidine/spermine N1-acetyltransferase 10.1016/0006-291X(91)91385-P
Polyamine catabolism contributes to enterotoxigenic Bacteroides fragilis-induced colon tumorigenesis 10.1073/pnas.1010203108
Polyamines impair immunity to helicobacter pylori by inhibiting L-Arginine uptake required for nitric oxide production 10.1053/j.gastro.2010.06.060
Activation of EGFR and ERBB2 by helicobacter pylori results in survival of gastric epithelial cells with DNA damage 10.1053/j.gastro.2014.02.005
Role of ornithine decarboxylase in regulation of estrogen receptor alpha expression and growth in human breast cancer cells 10.1007/s10549-012-2235-x
Spermine oxidation induced by Helicobacter pylori results in apoptosis and DNA damage: Implications for gastric carcinogenesis 10.1158/0008-5472.CAN-04-3511
Nuclear localization of human spermine oxidase isoforms - Possible implications in drug response and disease etiology 10.1111/j.1742-4658.2008.06419.x
Implication of SSAT by gene expression and genetic variation in suicide and major depression 10.1001/archpsyc.63.1.35
Spermidine/spermine N1-acetyltransferase (SSAT) activity in human small-cell lung carcinoma cells following transfection with a genomic SSAT construct 10.1042/BJ20021895
Placental polyamine metabolism differs by fetal sex, fetal growth restriction, and preeclampsia 10.1172/jci.insight.120723
Induction of the PAOh1/SMO polyamine oxidase by polyamine analogues in human lung carcinoma cells 10.1007/s00280-003-0662-4
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
Polyamines and cancer: implications for chemotherapy and chemoprevention. 10.1017/erm.2013.3
Design of polyamine-based therapeutic agents: New targets and new directions 10.1042/BSE0460006
Structure of the human spermidine/spermine N1-acetyltransferase gene. Kxon/intron gene organization and localization to Xp22.1 10.1016/0006-291X(92)90471-V
Polyamine-Regulated translation of spermidine/spermine-N1-Acetyltransferase 10.1128/MCB.06444-11
A charge-deficient analogue of spermine with chelating properties 10.1007/s11171-005-0037-1
Arginase 2 deletion leads to enhanced M1 macrophage activation and upregulated polyamine metabolism in response to Helicobacter pylori infection 10.1007/s00726-016-2231-2
Suppression of exogenous gene expression by spermidine/spermine N 1-acetyltransferase 1 (SSAT1) cotransfection 10.1074/jbc.M109.092007
Polyamine analogues targeting epigenetic gene regulation 10.1042/BSE0460007
Proximal tubule epithelial cell specific ablation of the spermidine/spermine N1-acetyltransferase gene reduces the severity of renal ischemia/reperfusion injury 10.1371/journal.pone.0110161
Metabolism of N-alkylated spermine analogues by polyamine and spermine oxidases 10.1007/s00726-009-0429-2
Inhibition of the LSD1 (KDM1A) demethylase reactivates the all-trans-retinoic acid differentiation pathway in acute myeloid leukemia 10.1038/nm.2661
The identification of a cis-element and a trans-acting factor involved in the response to polyamines and polyamine analogues in the regulation of the human spermidine/spermine N1-acetyltransferase gene transcription 10.1074/jbc.273.51.34623
Cloning and characterization of human polyamine-modulated factor-1, a transcriptional cofactor that regulates the transcription of the spermidine/spermine N1-acetyltransferase gene 10.1074/jbc.274.31.22095
Histone demethylation mediated by the nuclear amine oxidase homolog LSD1 10.1016/j.cell.2004.12.012
The role of polyamine catabolism in anti-tumour drug response 10.1042/BST0310361
Translation of ODC mRNA and polyamine transport are suppressed in ras-transformed CREF cells by depleting translation initiation factor 4E 10.1006/bbrc.1997.7592
The role of polyamine catabolism in polyamine analogue-induced programmed cell death 10.1073/pnas.94.21.11557
Helicobacter pylori-induced macrophage apoptosis requires activation of ornithine decarboxylase by c-Myc 10.1074/jbc.C500122200
Structural comparison of alkylpolyamine analogues with potent in vitro antitumor or antiparasitic activity 10.1016/S0960-894X(96)00510-0
Structural specificity of polyamines and polyamine analogues in the protection of DNA from strand breaks induced by reactive oxygen species 10.1006/bbrc.1998.8258
Targeting hexokinase 2 inhibition promotes radiosensitization in HPV16 E7-induced cervical cancer and suppresses tumor growth 10.3892/ijo.2017.3979
Dual inhibitors of LSD1 and spermine oxidase 10.1039/c8md00610e
Suppression of Polyamine Catabolism by Activated Ki-ras in Human Colon Cancer Cells 10.1002/mc.10166
Oxidative Damage Targets Complexes Containing DNA Methyltransferases, SIRT1, and Polycomb Members to Promoter CpG Islands 10.1016/j.ccr.2011.09.012
Polyamine-based analogues as biochemical probes and potential therapeutics 10.1042/BST0350356
Terminally alkylated polyamine analogues as chemotherapeutic agents 10.1021/jm000084m
Induction of spermidine/spermine N1-acetyltransferase in breast cancer tissues treated with the polyamine analogue N1,N 11-diethylnorspermine 10.1007/s00280-004-0786-1
Molecular mechanisms of polyamine analogs in cancer cells 10.1097/00001813-200503000-00002
Polyamines and their metabolizing enzymes in human frontal cortex and hippocampus: Preliminary measurements in affective disorders 10.1016/0006-3223(94)00256-3
Loss of LSD1 (lysine-specific demethylase 1) suppresses growth and alters gene expression of human colon cancer cells in a p53- and DNMT1 (DNA methyltransferase 1)-independent manner 10.1042/BJ20121360
Polyamine catabolism is enhanced after traumatic brain injury 10.1089/neu.2009.1097
Structure-activity study for (bis)ureidopropyl- and (bis)thioureidopropyldiamine LSD1 inhibitors with 3-5-3 and 3-6-3 carbon backbone architectures 10.1016/j.bmc.2015.01.049
Induction of spermidine/spermine N1-acetyltransferase (SSAT) by aspirin in Caco-2 colon cancer cells 10.1042/BJ20051298
A selective phenelzine analogue inhibitor of histone demethylase LSD1 10.1021/cb500018s
Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity 10.1016/S0960-894X(01)00315-8
Inhibition of lysine-specific demethylase 1 by polyamine analogues results in reexpression of aberrantly silenced genes 10.1073/pnas.0700720104
Synthesis and Evaluation of Unsymmetrically Substituted Polyamine Analogues as Modulators of Human Spermidine/Spermine-N1-Acetyltransferase (SSAT) and as Potential Antitumor Agents 10.1021/jm00072a020
Pentamines as substrate for human spermine oxidase 10.1248/bpb.b12-00818
Polyamine-based small molecule epigenetic modulators 10.1039/c1md00220a
Spermine oxidase mediates the gastric cancer risk associated with Helicobacter pylori CagA 10.1053/j.gastro.2011.07.045
The effects of DFMO on polyamine metabolism in the inner ear 10.1016/0378-5955(91)90057-G
Polyamine analogs modulate gene expression by inhibiting lysine-specific demethylase 1 (LSD1) and altering chromatin structure in human breast cancer cells 10.1007/s00726-011-1004-1
Metabolism links bacterial biofilms and colon carcinogenesis 10.1016/j.cmet.2015.04.011
Induction of human spermine oxidase SMO(PAOh1) is regulated at the levels of new mRNA synthesis, mRNA stabilization and newly synthesized protein 10.1042/BJ20041084
Polyaminohydroxamic acids and polyaminobenzamides as isoform selective histone deacetylase inhibitors 10.1021/jm701384x
Nucleotide sequence of hamster spermidine/spermine-N1-acetyltransferase cDNA 10.1016/0167-4781(92)90148-S
Efficacy and Safety of Curcumin in Treatment of Intestinal Adenomas in Patients With Familial Adenomatous Polyposis 10.1053/j.gastro.2018.05.031
Growth and biochemical effects of unsymmetrically substituted polyamine analogues in human lung tumor cells 1 10.1007/BF00685735
Oligoamine analogues in combination with 2-difluoromethylornithine synergistically induce re-expression of aberrantly silenced tumour-suppressor genes 10.1042/BJ20111271
Spermine and spermidine mediate protection against oxidative damage caused by hydrogen peroxide 10.1007/s00726-007-0513-4
Spermine causes loss of innate immune response to Helicobacter pylori by inhibition of inducible nitric-oxide synthase translation 10.1074/jbc.C400498200
Effects of glutathione or polyamine depletion on in vivo thermosensitization 10.3109/02656739209021775
Chronic lithium treatment prevents the dexamethasone-induced increase of brain polymine metabolizing enzymes 10.1016/0024-3205(92)90289-2
Reduction in polyamine catabolism leads to spermine-mediated airway epithelial injury and induces asthma features 10.1111/all.13472
Largazole and analogues with modified metal-binding motifs targeting histone deacetylases: Synthesis and biological evaluation 10.1021/jm200432a
Modulation of growth gene expression by selective alteration of polyamines in human colon carcinoma cells 10.1016/0006-291X(89)91082-6
Tumor necrosis factor α induces spermidine/spermine N 1 -acetyltransferase through nuclear factor κB in non-small cell lung cancer cells 10.1074/jbc.M601871200
Properties of purified recombinant human polyamine oxidase, PAOh1/SMO 10.1016/S0006-291X(03)00636-3
Prostanoids, Ornithine Decarboxylase, and Polyamines in Primary Chemoprevention of Familial Adenomatous Polyposis 10.1053/j.gastro.2003.11.013
N 1 -Nonyl-1,4-diaminobutane ameliorates brain infarction size in photochemically induced thrombosis model mice 10.1016/j.neulet.2018.01.054
Cloning and characterization of multiple human polyamine oxidase splice variants that code for isoenzymes with different biochemical characteristics 10.1042/BJ20021587
Overexpression of SSAT in kidney cells recapitulates various phenotypic aspects of kidney ischemia-reperfusion injury 10.1097/01.ASN.0000131525.77636.D5
Polyamine catabolism and oxidative damage 10.1074/jbc.TM118.003337
Combination therapy with vidaza and entinostat suppresses tumor growth and reprograms the epigenome in an orthotopic lung cancer model 10.1158/0008-5472.CAN-10-3184
Recent advances in the development of polyamine analogues as antitumor agents 10.1021/jm900187v
RGFGIGS is an amino acid sequence required for acetyl coenzyme A binding and activity of human spermidine/spermine N1acetyltransferase 10.1074/jbc.271.31.18920
Polyamine catabolism in carcinogenesis: Potential targets for chemotherapy and chemoprevention 10.1007/s00726-013-1529-6
Tumor necrosis factor-α increases reactive oxygen species by inducing spermine oxidase in human lung epithelial cells: A potential mechanism for inflammation-induced carcinogenesis 10.1158/0008-5472.CAN-06-3174
Induction of phase 2 enzymes by serum oxidized polyamines through activation of Nrf2: Effect of the polyamine metabolite acrolein 10.1016/S0006-291X(03)00834-9
Polyamine catabolism and disease 10.1042/BJ20090598
Epigenetic silencing of miR-124 prevents spermine oxidase regulation: Implications for Helicobacter pylori-induced gastric cancer 10.1038/onc.2016.91
Activation of endoplasmic reticulum stress response by enhanced polyamine catabolism is important in the mediation of cisplatin-induced acute kidney injury 10.1371/journal.pone.0184570
Polyamine analogues down-regulate estrogen receptor α expression in human breast cancer cells 10.1074/jbc.M600910200
Inhibition of cell growth in CaCO2 cells by the polyamine analogue N1,N12-bis(ethyl)spermine is preceded by a reduction in MYC oncoprotein levels 10.1002/(SICI)1097-4652(199803)174:3<380::AID-JCP12>3.0.CO;2-D
Polyamines in rat brain extracellular space after ischemia 10.1007/BF03160020
1-(N-alkylamino)-11-(N-ethylamino)-4,8-diazaundecanes: Simple synthetic polyamine analogues that differentially alter tubulin polymerization 10.1021/jm980603+
Alkyl-substituted polyaminohydroxamic acids: A novel class of targeted histone deacetylase inhibitors 10.1021/jm0505009
Hepatocyte-specific ablation of spermine/spermidine-N 1 -acetyltransferase gene reduces the severity of CCL 4 -induced acute liver injury 10.1152/ajpgi.00431.2011
Self-immolative nanoparticles for simultaneous delivery of microRNA and targeting of polyamine metabolism in combination cancer therapy 10.1016/j.jconrel.2016.12.017
Induction of polyamine oxidase 1 by Helicobacter pylori causes macrophage apoptosis by hydrogen peroxide release and mitochondrial membrane depolarization 10.1074/jbc.M401370200
Histone deacetylase inhibition overcomes drug resistance through a miRNA-dependent mechanism 10.1158/1535-7163.MCT-13-0418
A simple assay for mammalian spermine oxidase: a polyamine catabolic enzyme implicated in drug response and disease. 10.1007/978-1-61779-034-8_10
Increased expression and cellular localization of spermine oxidase in ulcerative colitis and relationship to disease activity 10.1002/ibd.21224
MOF Acetylates the Histone Demethylase LSD1 to Suppress Epithelial-to-Mesenchymal Transition 10.1016/j.celrep.2016.05.050
Metabolomic studies identify changes in transmethylation and polyamine metabolism in a brain-specific mouse model of tuberous sclerosis complex 10.1093/hmg/ddy118
Polyamine-modulated c-Myc expression in normal intestinal epithelial cells regulates p21Cip1 transcription through a proximal promoter region 10.1042/BJ20060217
Novel oligoamine analogues inhibit lysine-specific demethylase 1 and induce reexpression of epigenetically silenced genes 10.1158/1078-0432.CCR-09-1293
Inflammation and polyamine catabolism: The good, the bad and the ugly 10.1042/BST0350300
Significant induction of spermidine/spermine N1‐acetyltransferase without cytotoxicity by the growth‐supporting polyamine analogue 1,12‐dimethylspermine 10.1002/jcp.1041650109
Say what? The activity of the polyamine biosynthesis inhibitor difluoromethylornithine in chemoprevention is a result of reduced thymidine pools? 10.1158/2159-8290.CD-13-0427
High specific induction of spermidine/spermine N1-acetyltransferase in a human large cell lung carcinoma. 10.1042/bj2700615
Low molecular weight amidoximes that act as potent inhibitors of lysine-specific demethylase 1 10.1021/jm3002845
In vitro and in vivo effects of the conformationally restricted polyamine analogue CGC-11047 on small cell and non-small cell lung cancer cells 10.1007/s00280-008-0706-x
Curcumin mediates polyamine metabolism and sensitizes gastrointestinal cancer cells to antitumor polyamine-targeted therapies 10.1371/journal.pone.0202677
Cloning and characterization of the mouse polyamine-modulated factor-1 (mPMF-1) gene: An alternatively spliced homologue of the human transcription factor 10.1042/0264-6021:3590387
(Bis)urea and (Bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators 10.1021/jm100217a
Properties of recombinant human N1-acetylpolyamine oxidase (hPAO): Potential role in determining drug sensitivity 10.1007/s00280-004-0936-5
Lithium exerts a time-dependent and tissue-selective attenuation of the dexamethasone-induced polyamine response in rat brain and liver 10.1016/0006-8993(94)91016-2
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
Mutagenesis studies of the 14 Å internal cavity of histone deacetylase 1: Insights toward the acetate-escape hypothesis and selective inhibitor design 10.1021/jm401837e
Development of an ELISA-based HDAC activity assay for characterization of isoform-selective inhibitors 10.1177/1087057115598118
Largazole Analogues Embodying Radical Changes in the Depsipeptide Ring: Development of a More Selective and Highly Potent Analogue 10.1021/acs.jmedchem.6b01271
Structural Requirements of HDAC Inhibitors: SAHA Analogues Modified at the C2 Position Display HDAC6/8 Selectivity 10.1021/acsmedchemlett.6b00124
The structural requirements of histone deacetylase inhibitors: SAHA analogs modified at the C5 position display dual HDAC6/8 selectivity 10.1016/j.bmcl.2017.06.033
Design, synthesis, and screening of ortho-amino thiophene carboxamide derivatives on hepatocellular carcinomaas VEGFR-2Inhibitors 10.1080/14756366.2018.1503654
The structural requirements of histone deacetylase inhibitors: C4-modified SAHA analogs display dual HDAC6/HDAC8 selectivity 10.1016/j.ejmech.2017.10.076
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
Hiding in Plain Sight: The Bimetallic Magnesium Covalent Bond in Enzyme Active Sites 10.1021/acs.inorgchem.6b02189
GATA3 zinc finger 2 mutations reprogram the breast cancer transcriptional network 10.1038/s41467-018-03478-4
Identification of the effector domain of biglycan that facilitates BMP-2 osteogenic function 10.1038/s41598-018-25279-x
Probing Dominant Negative Behavior of Glucocorticoid Receptor beta through a Hybrid Structural and Biochemical Approach 10.1128/MCB.00453-17
Differential in Vitro Biological Action, Coregulator Interactions, and Molecular Dynamic Analysis of Bisphenol A (BPA), BPAF, and BPS Ligand-ER alpha Complexes 10.1289/EHP2505
A Bioactive Resveratrol Trimer from the Stem Bark of the Sri Lankan Endemic Plant Vateria copallifera 10.1021/acs.jnatprod.7b00892
A finite field method for calculating molecular polarizability tensors for arbitrary multipole rank 10.1002/jcc.21914
A proposed structural model of human protein Z [4] 10.1111/j.1538-7836.2007.02597.x
A reconsideration of the evidence for structural reorganization in FVII zymogen [8] 10.1111/j.1538-7836.2005.01433.x
A smooth particle mesh Ewald method 10.1063/1.470117
An all-atom solution-equilibrated model for human extrinsic blood coagulation complex (sTF-VIIa-Xa): A protein-protein docking and molecular dynamics refinement study 10.1111/j.1538-7836.2003.00421.x
Atomic forces for geometry-dependent point multipole and Gaussian multipole models 10.1002/jcc.21563
Binding of 5-phospho-D-arabinonohydroxamate and 5-phospho-D-arabinonate inhibitors to zinc phosphomannose isomerase from Candida albicans studied by polarizable molecular mechanics and quantum mechanics 10.1002/jcc.20586
Binuclear manganese(II) complexes in biological systems 10.1080/00268970701747199
Catalytic mechanism of human DNA polymerase λ with Mg 2+ and Mn 2+ from ab initio quantum mechanical/molecular mechanical studies 10.1016/j.dnarep.2008.07.007
Charge localization in negative ion dynamics: Effect on caging of Br−2 in Arn and (CO2)n clusters 10.1063/1.456215
Computational study of the putative active form of protein Z (PZa): Sequence design and structural modeling 10.1110/ps.034801.108
Conformational dependence of 13C shielding and coupling constants for methionine methyl groups 10.1007/s10858-010-9436-6
Cooperative damage recognition by UvrA and UvrB: Identification of UvrA residues that mediate DNA binding 10.1016/j.dnarep.2007.11.013
Cube to cage transitions in (H2O)n (n=12, 16, and 20) 10.1063/1.472190
Dephosphorylation of threonine 38 Is required for nuclear translocation and activation of human xenobiotic receptor CAR (NR1I3) 10.1074/jbc.M109.048108
Dynamics of ion solvation in a Stockmayer fluid 10.1063/1.461954
Early unfolding response of a stable protein domain to environmental changes 10.1021/jp0483851
Effect of the treatment of long-range forces on the dynamics of ions in aqueous solutions 10.1063/1.469422
Energetics and structure in I 2 -(CO 2) n clusters 10.1007/BF01543966
Four loops of the catalytic domain of factor VIIa mediate the effect of the first EGF-like domain substitution on factor VIIa catalytic activity 10.1006/jmbi.2001.4556
HPAM: Hirshfeld partitioned atomic multipoles 10.1016/j.cpc.2011.10.003
Ion solvation in water clusters 10.1007/BF01429132
Many-body effects in molecular dynamics simulations of Na+(H2O)n and Cl−(H2O)n clusters 10.1063/1.460992
Mobility of stretched water 10.1063/1.464364
Modeling Zymogen Protein C 10.1016/S0006-3495(00)76530-1
Modeling of the DNA-binding site of yeast Pms1 by mass spectrometry 10.1016/j.dnarep.2011.01.010
Molecular dynamics simulation of sodium dodecyl sulfate micelle in water: Micellar structural characteristics and counterion distribution 10.1021/jp013616z
Molecular dynamics simulations of sodium dodecyl sulfate micelle in water: The behavior of water 10.1021/jp025872x
Molecular insights into DNA polymerase deterrents for ribonucleotide insertion 10.1074/jbc.M111.253401
New tricks for modelers from the crystallography toolkit: The particle mesh Ewald algorithm and its use in nucleic acid simulations 10.1016/S0969-2126(99)80033-1
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
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