Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity
Gregory M. LaMonte
Jehad Almaliti
Betsaida Bibo-Verdugo
Lena Keller
Bing Yu Zou
Jennifer Yang
Yevgeniya Antonova-Koch
Pamela Orjuela-Sanchez
Colleen A. Boyle
Edgar Vigil
Lawrence Wang
Gregory M. Goldgof
Lena Gerwick
Anthony J. O’Donoghue
Elizabeth A. Winzeler
William H. Gerwick
Sabine Ottilie
Elizabeth Winzeler
Winzeler Elizabeth
ORCID: 0000-0002-4049-2113
Large-Scale Annotation of Small-Molecule Libraries Using Public Databases.
10.1002/chin.200740208
Perspectives: The missing pieces
10.1038/484s22a
Use of Flow cytometry to identify aCaulobacter4.5 S RNA Temperature-sensitive Mutant Defective in the Cell Cycle
10.1006/jmbi.1995.0439
Noncoding RNA, antigenic variation, and the virulence genes of Plasmodium falciparum
10.1186/1741-7007-9-50
Fluorescence anisotropy decay of ethidium bound to nucleosome core particles. 2. The Torsional Motion of the DNA is highly constrained and sensitive to pH
10.1021/bi00235a025
Biochips in Malaria for Antiparasitic Discovery
10.1201/9781420015607.ch3
Chapter 4. Human Targets Repositioning and Cell-based Approaches for Antimalarial Discovery
10.1039/9781849733496-00088
Mining High-Throughput Screening Data by Novel Knowledge-Based Optimization Analysis
10.1002/9780470567623.ch7
Further strategies for signature-tagged mutagenesis and the application of oligonucleotide microarrays for the quantification of DNA-tagged strains
10.1016/s0580-9517(02)33011-3
Functional Analysis of the Yeast Genome by Precise Deletion and Parallel Phenotypic Characterization
10.1002/047084664x.ch14
Treasures and traps in genome-wide data sets: case examples from yeast
10.1038/nrg886
Using expression information to discover new drug and vaccine targets in the malaria parasite Plasmodium falciparum
10.1517/14622416.6.1.17
The Activities of Current Antimalarial Drugs on the Life Cycle Stages of Plasmodium: A Comparative Study with Human and Rodent Parasites
10.1371/journal.pmed.1001169
Na+ Regulation in the Malaria Parasite Plasmodium falciparum Involves the Cation ATPase PfATP4 and Is a Target of the Spiroindolone Antimalarials
10.1016/j.chom.2012.12.006
Antimalarial drug discovery — approaches and progress towards new medicines
10.1038/nrmicro3183
Antimalarial drug discovery-approaches and progress towards new medicines
10.1038/nrmicro3138
Plasmodium falciparum: Genome wide perturbations in transcript profiles among mixed stage cultures after chloroquine treatment
10.1016/j.exppara.2007.03.001
The paradoxical population genetics of Plasmodium falciparum
10.1016/s1471-4922(02)02268-7
Applied systems biology and malaria
10.1038/nrmicro1327
Genome-Wide Analysis of Gene Expression
10.1016/b0-12-443710-9/00264-7
Malaria research in the post-genomic era
10.1038/nature07361
Epidemiology: Resistance mapping in malaria
10.1038/498446b
A Novel Promoter Motif forCaulobacterCell Cycle-controlled DNA Replication Genes
10.1006/jmbi.1996.0650
Techniques
10.1016/s1369-5274(00)00090-4
Large-scale mutagenesis and functional genomics in yeast
10.1007/s10142-002-0057-3
Genomics, systems biology and drug development for infectious diseases
10.1039/b703924g
Elucidating genetic diversity with oligonucleotide arrays
10.1007/s10577-005-1503-6
[1] Fluorescence-based expression monitoring using microarrays
10.1016/s0076-6879(99)06003-6
Advances in Parasite Genomics
10.1201/b13131-12
Target identification and validation of novel antimalarials
10.2217/fmb.11.45
Using the genome to dissect the molecular basis of drug resistance
10.2217/17460913.1.2.185
Advances in Parasite Genomics: From Sequences to Regulatory Networks
10.1371/journal.ppat.1000649
Functional analysis of the yeast genome
10.1016/s0959-437x(97)80039-1
Mitotic Evolution of Plasmodium falciparum Shows a Stable Core Genome but Recombination in Antigen Families
10.1371/journal.pgen.1003293
Transcriptional analysis of the Caulobacter 4.5 S RNA ffs gene and the physiological basis of an ffs mutant with a ts phenotype
10.1006/jmbi.1997.1261
A Systems-Based Analysis of Plasmodium vivax Lifecycle Transcription from Human to Mosquito
10.1371/journal.pntd.0000653
A Genome-Wide Transcriptional Analysis of the Mitotic Cell Cycle
10.1016/s1097-2765(00)80114-8
Regulatory motifs uncovered among gene expression clusters in Plasmodium falciparum
10.1016/j.molbiopara.2007.01.011
Genome-wide nucleosome mapping of Plasmodium falciparum reveals histone-rich coding and histone-poor intergenic regions and chromatin remodeling of core and subtelomeric genes
10.1186/1471-2164-10-610
Identification of the Plasmodium berghei resistance locus 9 linked to survival on chromosome 9
10.1186/1475-2875-12-316
The Plasmodium falciparum sexual development transcriptome: A microarray analysis using ontology-based pattern identification
10.1016/j.molbiopara.2005.05.007
Plasmodium Circumsporozoite Protein Promotes the Development of the Liver Stages of the Parasite
10.1016/j.cell.2008.03.022
Exposure of Plasmodium sporozoites to the intracellular concentration of potassium enhances infectivity and reduces cell passage activity
10.1016/j.molbiopara.2007.07.004
In Vivo Transcriptome of Plasmodium falciparum Reveals Overexpression of Transcripts That Encode Surface Proteins
10.1086/428289
Microarray-based comparative genomic analyses of the human malaria parasite Plasmodium falciparum using Affymetrix arrays
10.1016/j.molbiopara.2005.08.010
Plasmodium Circumsporozoite Protein Promotes the Development of the Liver Stages of the Parasite
10.1016/j.cell.2007.09.013
In silico discovery of transcription regulatory elements in Plasmodium falciparum
10.1186/1471-2164-9-70
Evidence-Based Annotation of the Malaria Parasite's Genome Using Comparative Expression Profiling
10.1371/journal.pone.0001570
Identification of non-CSP antigens bearing CD8 epitopes in mice immunized with irradiated sporozoites
10.1016/j.vaccine.2011.07.081
Direct transfer of whole genomes from bacteria to yeast
10.1038/nmeth.2433
Using Genetic Methods To Define the Targets of Compounds with Antimalarial Activity
10.1021/jm400325j
Genome Wide Analysis of Inbred Mouse Lines Identifies a Locus Containing Ppar-γ as Contributing to Enhanced Malaria Survival
10.1371/journal.pone.0010903
Nuclear Repositioning Precedes Promoter Accessibility and Is Linked to the Switching Frequency of a Plasmodium falciparum Invasion Gene
10.1016/j.chom.2012.11.004
Whole genome sequencing analysis of Plasmodium vivax using whole genome capture
10.1186/1471-2164-13-262
Genetic Analysis of Primaquine Tolerance in a Patient with Relapsing Vivax Malaria
10.3201/eid1905.121852
Correction: A Systematic Map of Genetic Variation in Plasmodium falciparum
10.1371/journal.ppat.0020096
Systems biology and malaria
10.1145/974614.974627
A Chemical Genomic Analysis of Decoquinate, a Plasmodium falciparum Cytochrome b Inhibitor
10.1021/cb200105d
Use of high-density tiling microarrays to identify mutations globally and elucidate mechanisms of drug resistance in Plasmodium falciparum
10.1186/gb-2009-10-2-r21
A systematic approach to understand the mechanism of action of the bisthiazolium compound T4 on the human malaria parasite, Plasmodium falciparum
10.1186/1471-2164-9-513
Cell-based optimization of novel benzamides as potential antimalarial leads
10.1016/j.bmcl.2009.10.050
A key role for lipoic acid synthesis during Plasmodium liver stage development
10.1111/cmi.12137
Imidazolopiperazines: Hit to Lead Optimization of New Antimalarial Agents
10.1021/jm2003359
Selective and Specific Inhibition of the Plasmodium falciparum Lysyl-tRNA Synthetase by the Fungal Secondary Metabolite Cladosporin
10.1016/j.chom.2012.04.015
Spirotetrahydro β-Carbolines (Spiroindolones): A New Class of Potent and Orally Efficacious Compounds for the Treatment of Malaria
10.1021/jm100410f
Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility
10.1038/nchembio.87
Imidazolopiperazines: Lead Optimization of the Second-Generation Antimalarial Agents
10.1021/jm300041e
Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials
10.1016/j.bmcl.2010.05.095
Synthesis and biological evaluation of epidithio-, epitetrathio-, and bis-(methylthio)diketopiperazines: Synthetic methodology, enantioselective total synthesis of epicoccin G, 8,8′-epi-ent-rostratin B, gliotoxin, gliotoxin G, emethallicin E, and haematocin and discovery of new antiviral and antimalarial agents
10.1021/ja308429f
Identification and localization of molecular markers linked to the Lr9 leaf rust resistance gene of wheat
10.1007/bf00222402
Analysis of disease resistance and quality characters of F1 hybrids of crosses between wheat (Triticum aestivum) and spelt (Triticum spelta)
10.1007/bf00024537
Analysis of the Meiotic Transcriptome in Genetically Distinct Budding Yeasts Using High Density Oligonucleotide Arrays
10.1007/978-3-662-04050-8_1
Direct Allelic Variation Scanning of the Yeast Genome
10.1126/science.281.5380.1194
3-Hydroxy-N′-arylidenepropanehydrazonamides with Halo-Substituted Phenanthrene Scaffolds Cure P. berghei Infected Mice When Administered Perorally
10.1021/acs.jmedchem.7b00140
Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity
10.1021/acs.jmedchem.7b00671
Using in Vitro Evolution and Whole Genome Analysis To Discover Next Generation Targets for Antimalarial Drug Discovery
10.1021/acsinfecdis.7b00276
Targeted disruption of a ring-infected erythrocyte surface antigen (RESA)-like export protein gene in Plasmodium falciparum confers stable chondroitin 4-sulfate cytoadherence capacity
10.1074/jbc.M114.615393
A comparison of match-only algorithms for the analysis of Plasmodium falciparum oligonucleotide arrays
10.1016/j.ijpara.2005.02.010
Mutations in the P-type cation-transporter ATPase 4, PfATP4, mediate resistance to both aminopyrazole and spiroindolone antimalarials
10.1021/cb500616x
Distinct physiological states of Plasmodium falciparum in malaria-infected patients
10.1038/nature06311
Next-Generation Sequencing of Plasmodium vivax Patient Samples Shows Evidence of Direct Evolution in Drug-Resistance Genes
10.1021/acsinfecdis.5b00049
Piperaquine resistance is associated with a copy number variation on chromosome 5 in drug-pressured Plasmodium falciparum parasites
10.1128/AAC.01793-10
Protein pathway and complex clustering of correlated mRNA and protein expression analyses in Saccharomyces cerevisiae
10.1073/pnas.0634629100
Mapping the malaria parasite druggable genome by using in vitro evolution and chemogenomics
10.1126/science.aan4472
Whole genome shotgun sequencing shows selection on leptospira regulatory proteins during in vitro culture attenuation
10.4269/ajtmh.15-0401
Parallel identification of new genes in Saccharomyces cerevisiae
10.1101/gr.226802
Validation of isoleucine utilization targets in Plasmodium falciparum
10.1073/pnas.1011560108
Functional profiling of the Saccharomyces cerevisiae genome
10.1038/nature00935
A novel multiple-stage antimalarial agent that inhibits protein synthesis
10.1038/nature14451
Large-scale identification of single-feature polymorphisms in complex genomes
10.1101/gr.541303
Experimentally induced blood-stage plasmodium vivax infection in healthy volunteers
10.1093/infdis/jit394
High-Throughput Assay and Discovery of Small Molecules that Interrupt Malaria Transmission
10.1016/j.chom.2015.12.001
Open source drug discovery: Highly potent antimalarial compounds derived from the tres cantos arylpyrroles
10.1021/acscentsci.6b00086
In silico gene function prediction using ontology-based pattern identification
10.1093/bioinformatics/bti111
CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs
10.1111/mmi.13397
Replication dynamics of the yeast genome
10.1126/science.294.5540.115
Targeting the ERAD pathway via inhibition of signal peptide peptidase for antiparasitic therapeutic design
10.1073/pnas.1216016110
Large-scale annotation of small-molecule libraries using public databases
10.1021/ci700092v
A broad analysis of resistance development in the malaria parasite
10.1038/ncomms11901
KAF156 is an antimalarial clinical candidate with potential for use in prophylaxis, treatment, and prevention of disease transmission
10.1128/AAC.02727-13
Trisubstituted Pyrimidines as Efficacious and Fast-Acting Antimalarials
10.1021/acs.jmedchem.6b00028
Global analysis of transcript and protein levels across the Plasmodium falciparum life cycle
10.1101/gr.2523904
KAI407, a potent non-8-aminoquinoline compound that kills Plasmodium cynomolgi early dormant liver stage parasites in vitro
10.1128/AAC.01927-13
Longitudinal study of Plasmodium pathogens identifies new loci associated with artemisinin resistance
10.1186/s13059-017-1219-x
Phenotypic Screens in Antimalarial Drug Discovery
10.1016/j.pt.2016.04.014
Excess polymorphisms in genes for membrane proteins in Plasmodium falciparum
10.1126/science.1075642
Glycophorin alleles link to malaria protection
10.1126/science.aan4184
Infection of laboratory-colonized Anopheles darlingi mosquitoes by Plasmodium vivax
10.4269/ajtmh.13-0708
The Ume6 regulon coordinates metabolic and meiotic gene expression in yeast
10.1073/pnas.202495299
Targeting Plasmodium PI(4)K to eliminate malaria
10.1038/nature12782
Discovery of gene function by expression profiling of the malaria parasite life cycle
10.1126/science.1087025
The core meiotic transcriptome in budding yeasts
10.1038/82539
Aneuploidy - It's more common than you think
10.1038/77273
Identification of a Potential Antimalarial Drug Candidate from a Series of 2-Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle
10.1021/acs.jmedchem.6b01265
Diversity-oriented synthesis yields novel multistage antimalarial inhibitors
10.1038/nature19804
Translation of the leaderless Caulobacter dnaX mRNA
10.1128/jb.179.12.3981-3988.1997
Imaging of plasmodium liver stages to drive next-generation antimalarial drug discovery
10.1126/science.1211936
A Plasmodium gene family encoding maurer's cleft membrane proteins: Structural properties and expression profiling
10.1101/gr.2126104
Spiroindolones, a potent compound class for the treatment of malaria
10.1126/science.1193225
In vivo transcriptional profiling of Plasmodium falciparum
10.1186/1475-2875-3-30
Application of high-density array-based signature-tagged mutagenesis to discover novel Yersinia virulence-associated genes
10.1128/IAI.69.12.7810-7819.2001
In vivo profiles in malaria are consistent with a novel physiological state
10.1073/pnas.0904478106
A plant-like kinase in plasmodium falciparum regulates parasite egress from erythrocytes
10.1126/science.1188191
Kalkipyrone B, a marine cyanobacterial γ-pyrone possessing cytotoxic and anti-fungal activities
10.1016/j.phytochem.2015.11.011
Drug resistance genomics of the antimalarial drug artemisinin
10.1186/s13059-014-0544-6
Microbiology: Molecular mechanism for switching of P. falciparum invasion pathways into human erythrocytes
10.1126/science.1115257
Erratum: A systematic map of genetic variation in Plasmodium falciparum (Plos Pathogens 2, 6 DOI:10.1371/journal.ppat.0020057)
10.1371/journal.ppat.0020057
A novel pyrazolopyridine with in vivo activity in Plasmodium berghei- and Plasmodium falciparum-infected mouse models from structure-activity relationship studies around the core of recently identified antimalarial imidazopyridazines
10.1021/acs.jmedchem.5b01605
Hexahydroquinolines are antimalarial candidates with potent blood-stage and transmission-blocking activity
10.1038/s41564-017-0007-4
Genomics, gene expression and DNA arrays
10.1038/35015701
UDP-galactose and acetyl-CoA transporters as Plasmodium multidrug resistance genes
10.1038/nmicrobiol.2016.166
Selective whole-genome amplification is a robust method that enables scalable whole-genome sequencing of Plasmodium vivax from unprocessed clinical samples
10.1128/mBio.02257-16
Systems analysis of host-parasite interactions
10.1002/wsbm.1311
A variant pfcrt isoform can contribute to plasmodium falciparum resistance to the first-line partner drug piperaquine
10.1128/mBio.00303-17
Lead optimization of imidazopyrazines: A new class of antimalarial with activity on Plasmodium liver stages
10.1021/ml500244m
Leveraging two-way probe-level block design for identifying differential gene expression with high-density oligonucleotide arrays
10.1186/1471-2105-5-42
Discovery of HDAC inhibitors with potent activity against multiple malaria parasite life cycle stages Dedicated to Prof. Dr. Alan R. Katritzky, in memoriam.
10.1016/j.ejmech.2014.05.050
In silico activity profiling reveals the mechanism of action of antimalarials discovered in a high-throughput screen
10.1073/pnas.0802982105
Functional characterization of the S. cerevisiae genome by gene deletion and parallel analysis
10.1126/science.285.5429.901
Design and Synthesis of Terephthalic Acid-Based Histone Deacetylase Inhibitors with Dual-Stage Anti-Plasmodium Activity
10.1002/cmdc.201700360
A High Resolution Case Study of a Patient with Recurrent Plasmodium vivax Infections Shows That Relapses Were Caused by Meiotic Siblings
10.1371/journal.pntd.0002882
Whole-genome sequencing and microarray analysis of ex vivo Plasmodium vivax reveal selective pressure on putative drug resistance genes
10.1073/pnas.1003776107
Discovery of a Quinoline-4-carboxamide Derivative with a Novel Mechanism of Action, Multistage Antimalarial Activity, and Potent in Vivo Efficacy
10.1021/acs.jmedchem.6b00723
Plasmodium falciparum Cyclic Amine Resistance Locus (PfCARL), a Resistance Mechanism for Two Distinct Compound Classes
10.1021/acsinfecdis.6b00025
Identification of pathogen genomic variants through an integrated pipeline
10.1186/1471-2105-15-63
Monitoring the chromosome 2 intraerythrocytic transcriptome of Plasmodium falciparum using oligonucleotide arrays
10.4269/ajtmh.2002.67.233
Synthesis of (+)-7,20-Diisocyanoadociane and Liver-Stage Antiplasmodial Activity of the Isocyanoterpene Class
10.1021/jacs.6b03899
Previously uncharacterized genes in the UV- and MMS-induced DNA damage response in yeast
10.1073/pnas.152264899
The Plasmodium eukaryotic initiation factor-2α kinase IK2 controls the latency of sporozoites in the mosquito salivary glands
10.1084/jem.20091975
Genomic profiling of drug sensitivities via induced haploinsufficiency
10.1038/6791
Bacterial genome reduction using the progressive clustering of deletions via yeast sexual cycling
10.1101/gr.182477.114
Mutations in the Plasmodium falciparum cyclic amine resistance locus (PfCARL) confer multidrug resistance
10.1128/mBio.00696-16
Genome scanning of Amazonian Plasmodium falciparum shows subtelomeric instability and clindamycin-resistant parasites
10.1101/gr.105163.110
Comparative chemical genomics reveal that the spiroindolone antimalarial KAE609 (Cipargamin) is a P-type ATPase inhibitor
10.1038/srep27806
Coordinated functions of WSS1, PSY2 and TOF1 in the DNA damage response
10.1093/nar/gkh994
Rapid Chagas Disease Drug Target Discovery Using Directed Evolution in Drug-Sensitive Yeast
10.1021/acschembio.6b01037
malERA: An updated research agenda for malaria elimination and eradication
10.1371/journal.pmed.1002456
Esterase mutation is a mechanism of resistance to antimalarial compounds
10.1038/ncomms14240
Developing Plasmodium vivax Resources for Liver Stage Study in the Peruvian Amazon Region
10.1021/acsinfecdis.7b00198
Continuous Supply of Plasmodium vivax Sporozoites from Colonized Anopheles darlingi in the Peruvian Amazon
10.1021/acsinfecdis.7b00195
An improbable journey: Creativity helped me make the transition from art to curing malaria
10.1074/jbc.AW118.005229
Plasmodium Niemann-Pick type C1-related protein is a druggable target required for parasite membrane homeostasis
10.7554/eLife.40529
The proteasome as a target:How not tidying up can have toxic consequences for parasitic protozoa
10.1073/pnas.1904694116
Covalent Plasmodium falciparum-selective proteasome inhibitors exhibit a low propensity for generating resistance in vitro and synergize with multiple antimalarial agents
10.1371/journal.ppat.1007722
In vitro selection predicts malaria parasite resistance to dihydroorotate dehydrogenase inhibitors in a mouse infection model
10.1126/scitranslmed.aav1636
Evolution of resistance in vitro reveals mechanisms of artemisinin activity inToxoplasma gondii
10.1073/pnas.1914732116
Synthesis and Bioactivity of Phthalimide Analogs as Potential Drugs to Treat Schistosomiasis, a Neglected Disease of Poverty
10.3390/ph13020025
Target deconvolution using in vitro evolution in haploid human cells
10.1101/2020.03.17.982181
Cyclization-blocked proguanil as a strategy to improve the antimalarial activity of atovaquone
10.1038/s42003-019-0397-3
One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria parasites
10.1016/j.ejmech.2018.09.018
Accessible and distinct decoquinate derivatives active against Mycobacterium tuberculosis and apicomplexan parasites
10.1038/s42004-018-0062-7
8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity
10.1002/cmdc.201800691
A Novel Antiparasitic Compound Kills Ring-Stage Plasmodium falciparum and Retains Activity against Artemisinin-Resistant Parasites
10.1093/infdis/jiz534
Open-source discovery of chemical leads for next-generation chemoprotective antimalarials
10.1126/science.aat9446
A high throughput screen for next-generation leads targeting malaria parasite transmission
10.1038/s41467-018-05777-2
Structure–Activity and Structure–Toxicity Relationships of Peptoid-Based Histone Deacetylase Inhibitors with Dual-Stage Antiplasmodial Activity
10.1002/cmdc.201800808
Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or Plasmodium vivax malaria infection: a proof-of-concept, open-label, phase 2a study
10.1016/S1473-3099(18)30309-8
Probing the Open Global Health Chemical Diversity Library for Multistage-Active Starting Points for Next-Generation Antimalarials
10.1021/acsinfecdis.9b00482
Advances in omics-based methods to identify novel targets for malaria and other parasitic protozoan infections
10.1186/s13073-019-0673-3
Validation of the protein kinase PfCLK3 as a multistage cross-species malarial drug target
10.1126/science.aau1682
Synthesis, Profiling, and in Vivo Evaluation of Cyclopeptides Containing N-Methyl Amino Acids as Antiplasmodial Agents
10.1021/acsmedchemlett.8b00543
Substituted Aminoacetamides as Novel Leads for Malaria Treatment
10.1002/cmdc.201900329
Common PIEZO1 Allele in African Populations Causes RBC Dehydration and Attenuates Plasmodium Infection
10.1016/j.cell.2018.02.047
High-Throughput Luciferase-Based Assay for the Discovery of Therapeutics That Prevent Malaria
10.1021/acsinfecdis.5b00143
Dual RNA-seq identifies human mucosal immunity protein Mucin-13 as a hallmark of Plasmodium exoerythrocytic infection
10.1038/s41467-019-08349-0
Target Validation and Identification of Novel Boronate Inhibitors of the Plasmodium falciparum Proteasome
10.1021/acs.jmedchem.8b01161
Lysyl-tRNA synthetase as a drug target in malaria and cryptosporidiosis
10.1073/pnas.1814685116
Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway
10.1038/s41467-020-15440-4
A Sleeping Area of Malaria Research Awakes
10.1016/j.chom.2018.02.008
Combining Stage Specificity and Metabolomic Profiling to Advance Antimalarial Drug Discovery
10.1016/j.chembiol.2019.11.009
Optimal 10-Aminoartemisinins With Potent Transmission-Blocking Capabilities for New Artemisinin Combination Therapies–Activities Against Blood Stage P. falciparum Including PfKI3 C580Y Mutants and Liver Stage P. berghei Parasites
10.3389/fchem.2019.00901
The genomic architecture of antimalarial drug resistance
10.1093/bfgp/elz008
Exploration of Plasmodium vivax transmission dynamics and recurrent infections in the Peruvian Amazon using whole genome sequencing
10.1186/s13073-018-0563-0
A roadmap for malaria research
10.1126/science.aay5963
Genome-Wide Dynamic Evaluation of the UV-Induced DNA Damage Response
10.1534/g3.120.401417
Genomic Approaches to Drug Resistance in Malaria
10.1146/annurev-micro-012220-064343
Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway
10.1101/735894
Failure of in vitro differentiation of Plasmodium falciparum gametocytes into ookinetes arises because of poor gamete fertilisation
10.1101/216721
Human Aurora kinase inhibitor Hesperadin reveals epistatic interaction between Plasmodium falciparum PfArk1 and PfNek1 kinases
10.1038/s42003-020-01424-z
Validation of the protein kinase PfCLK3 as a multi-stage cross species malarial drug target
10.1101/404459
Defining the yeast resistome through in vitro evolution and whole genome sequencing
10.1101/2021.02.17.430112
Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity
10.1016/j.chembiol.2020.04.001
PfMFR3: A Multidrug-Resistant Modulator in Plasmodium falciparum
10.1021/acsinfecdis.0c00676
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series
10.1021/acs.jmedchem.1c00173
Common Piezo1 allele in African populations causes xerocytosis and attenuates Plasmodium infection
10.1101/159830
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts
10.1021/acs.jmedchem.1c00034
Mapping the malaria parasite drug-able genome using in vitro evolution and chemogenomics
10.1101/139386
A consensus-based and readable extension of Linear Code for Reaction Rules (LiCoRR)
10.3762/BJOC.16.215
Dual RNAseq shows the human mucosal immunity protein, MUC13, is a hallmark of Plasmodium exoerythrocytic infection
10.1101/183764
The key glycolytic enzyme phosphofructokinase is involved in resistance to antiplasmodial glycosides
10.1128/mBio.02842-20
Synthesis and Structure-Activity Relationship of Dual-Stage Antimalarial Pyrazolo[3,4- b]pyridines
10.1021/acs.jmedchem.0c01152
Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in Plasmodium falciparum
10.1021/acs.jmedchem.0c02022
Chemoprotective antimalarials identified through quantitative high-throughput screening of Plasmodium blood and liver stage parasites
10.1038/s41598-021-81486-z
Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box
10.1038/s41467-020-20629-8
SnapShot: Antimalarial Drugs
10.1016/j.cell.2020.09.006
The antimalarial resistome – finding new drug targets and their modes of action
10.1016/j.mib.2020.06.004
Multistage and transmission-blocking targeted antimalarials discovered from the open-source MMV Pandemic Response Box
10.1101/2020.06.05.133405
Evolution of resistance in vitro reveals a novel mechanism of artemisinin activity in Toxoplasma gondii
10.1101/746065
MalDA, Accelerating Malaria Drug Discovery
10.1016/j.pt.2021.01.009
Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity
10.1016/j.ejmech.2020.113065
Plasmodium falciparum Niemann-Pick Type C1-Related Protein is a Druggable Target Required for Parasite Membrane Homeostasis
10.1101/371484
Lena Keller
Keller Lena
/ Lena Etzbach
ORCID: 0000-0003-2899-1232
Biosynthesis and Heterologous Production of Vioprolides: Rational Biosynthetic Engineering and Unprecedented 4-Methylazetidinecarboxylic Acid Formation.
10.1002/anie.201802479
Biosynthetic Studies of Telomycin Reveal New Lipopeptides with Enhanced Activity.
10.1021/jacs.5b01794
Macyranones: Structure, Biosynthesis, and Binding Mode of an Unprecedented Epoxyketone that Targets the 20S Proteasome.
10.1021/jacs.5b03833
Structure-function analysis for the hydroxylation of Δ4 C21-steroids by the myxobacterial CYP260B1.
10.1002/1873-3468.12217
Cystomanamides: structure and biosynthetic pathway of a family of glycosylated lipopeptides from myxobacteria.
10.1021/ol500779s
Molluscicidal metabolites from an assemblage of Palmyra Atoll cyanobacteria.
10.1021/np200106b
Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity.
10.1021/acs.jmedchem.7b00671
Chemical Biology of Marine Cyanobacteria
10.1201/9781315117089-2
Tutuilamides A–C: Vinyl-Chloride-Containing Cyclodepsipeptides from Marine Cyanobacteria with Potent Elastase Inhibitory Properties
10.1021/acschembio.9b00992
Palstimolide A: A Complex Polyhydroxy Macrolide with Antiparasitic Activity
10.3390/molecules25071604
Biosynthese und heterologe Expression der Vioprolide: rationale gentechnische Eingriffe in die Biosynthese und 4-Methylazetidincarbonsäure-Bildung
10.1002/ange.201802479
Applying a Chemogeographic Strategy for Natural Product Discovery from the Marine Cyanobacterium Moorena bouillonii
10.3390/md18100515
William Gerwick
Gerwick William
ORCID: 0000-0003-1403-4458
Laucysteinamide A, a Hybrid PKS/NRPS Metabolite from a Saipan Cyanobacterium, cf. Caldora penicillata
10.3390/md15040121
Characterization of Rhamnolipids Produced by an Arctic Marine Bacterium from the Pseudomonas fluorescence Group
10.3390/md16050163
Identification of a 3-Alkylpyridinium Compound from the Red Sea Sponge Amphimedon chloros with In Vitro Inhibitory Activity against the West Nile Virus NS3 Protease
10.3390/molecules23061472
MS/MS-Based Molecular Networking Approach for the Detection of Aplysiatoxin-Related Compounds in Environmental Marine Cyanobacteria
10.3390/md16120505
Integrated Genomic and Metabolomic Approach to the Discovery of Potential Anti-Quorum Sensing Natural Products from Microbes Associated with Marine Samples from Singapore
10.3390/md17010072
Epicortical Brevetoxin Treatment Promotes Neural Repair and Functional Recovery after Ischemic Stroke
10.3390/md18070374
A Multi-Omics Characterization of the Natural Product Potential of Tropical Filamentous Marine Cyanobacteria
10.3390/md19010020
Kalkitoxin Reduces Osteoclast Formation and Resorption and Protects against Inflammatory Bone Loss
10.3390/ijms22052303
Dudawalamides A–D, Antiparasitic Cyclic Depsipeptides from the Marine Cyanobacterium Moorea producens
10.1021/acs.jnatprod.7b00034
Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity
10.1021/acs.jmedchem.7b00671
5-Hydroxycyclopenicillone, a New β-Amyloid Fibrillization Inhibitor from a Sponge-Derived Fungus Trichoderma sp. HPQJ-34
10.3390/md15080260
The Face of a Molecule
10.1021/acs.jnatprod.7b00624
Small Molecule Accurate Recognition Technology (SMART) to Enhance Natural Products Research
10.1038/s41598-017-13923-x
A Mononuclear Iron-Dependent Methyltransferase Catalyzes Initial Steps in Assembly of the Apratoxin A Polyketide Starter Unit
10.1021/acschembio.7b00746
Bastimolide B, an Antimalarial 24-Membered Marine Macrolide Possessing a tert-Butyl Group
10.1021/acs.jnatprod.7b00917
Samholides, Swinholide-Related Metabolites from a Marine Cyanobacterium cf. Phormidium sp.
10.1021/acs.joc.8b00028
Eckmaxol, a Phlorotannin Extracted from Ecklonia maxima, Produces Anti-β-amyloid Oligomer Neuroprotective Effects Possibly via Directly Acting on Glycogen Synthase Kinase 3β
10.1021/acschemneuro.7b00527
Biosynthesis of t-Butyl in Apratoxin A: Functional Analysis and Architecture of a PKS Loading Module
10.1021/acschembio.8b00252
Ketoreductase Domain Dysfunction Expands Chemodiversity: Malyngamide Biosynthesis in the Cyanobacterium Okeania hirsuta
10.1021/acschembio.8b00910
Structural Basis of Polyketide Synthase O-Methylation
10.1021/acschembio.8b00687
Dragocins A−D, Structurally Intriguing Cytotoxic Metabolites from a Panamanian Marine Cyanobacterium
10.1021/acs.orglett.8b03712
Marine natural products as potential anti-tubercular agents
10.1016/j.ejmech.2019.01.026
Highly Convergent Total Synthesis and Assignment of Absolute Configuration of Majusculamide D, a Potent and Selective Cytotoxic Metabolite from Moorea sp.
10.1021/acs.orglett.8b04050
Nature's Combinatorial Biosynthesis Produces Vatiamides A–F
10.1002/anie.201902571
Nature's Combinatorial Biosynthesis Produces Vatiamides A–F
10.1002/ange.201902571
Cytotoxic Microcolin Lipopeptides from the Marine Cyanobacterium Moorea producens
10.1021/acs.jnatprod.9b00549
Design of Gallinamide A Analogs as Potent Inhibitors of the Cysteine Proteases Human Cathepsin L and Trypanosoma cruzi Cruzain
10.1021/acs.jmedchem.9b00294
Commensal oralRothia mucilaginosaproduces enterobactin – a metal chelating siderophore
10.1101/2020.02.20.956391
Palstimolide A: A Complex Polyhydroxy Macrolide with Antiparasitic Activity
10.3390/molecules25071604
Commensal Oral Rothia mucilaginosa Produces Enterobactin, a Metal-Chelating Siderophore
10.1128/mSystems.00161-20
Correction to “Highly Convergent Total Synthesis and Assignment of Absolute Configuration of Majusculamide D, a Potent and Selective Cytotoxic Metabolite from Moorea sp.”
10.1021/acs.orglett.0c02252
The Chemistry, Biochemistry and Pharmacology of Marine Natural Products from Leptolyngbya, a Chemically Endowed Genus of Cyanobacteria
10.3390/md18100508
Natural Products with Potential to Treat RNA Virus Pathogens Including SARS-CoV-2
10.1021/acs.jnatprod.0c00968
Total Synthesis of Laucysteinamide A, a Monomeric Congener of Somocystinamide A
10.1021/acs.jnatprod.0c01317
Cyanobacteria-shrimp colonies in the Mariana Islands
10.1007/s10452-021-09837-6
Portobelamides A and B and Caciqueamide, Cytotoxic Peptidic Natural Products from a Caldora sp. Marine Cyanobacterium
10.1021/acs.jnatprod.0c01383
SIRT1 Activation Enhancing 8,3′-Neolignans from the Twigs of Corylopsis coreana Uyeki
10.3390/plants10081684
First Total Synthesis and Structure–Activity Relationship of Iheyamide A, an Antitrypanosomal Linear Peptide Isolated from a Dapis sp. Marine Cyanobacterium
10.1021/acs.jnatprod.1c00792
Gregory Goldgof
Goldgof Gregory
/ Gregory M. Goldgof
ORCID: 0000-0001-8732-9834
SARS-CoV-2 seroprevalence and neutralizing activity in donor and patient blood.
10.1038/s41467-020-18468-8
Evaluation of SARS-CoV-2 serology assays reveals a range of test performance.
10.1038/s41587-020-0659-0
Pan-active imidazolopiperazine antimalarials target the Plasmodium falciparum intracellular secretory pathway.
10.1038/s41467-020-15440-4
Two inhibitors of yeast plasma membrane ATPase 1 (ScPma1p): toward the development of novel antifungal therapies.
10.1186/s13321-018-0261-3
Mycobacterium tuberculosis Exploits a Molecular Off Switch of the Immune System for Intracellular Survival.
10.1038/s41598-017-18528-y
A broad analysis of resistance development in the malaria parasite.
10.1038/ncomms11901
Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity.
10.1021/acs.jmedchem.7b00671
Direct transfer of whole genomes from bacteria to yeast.
10.1038/nmeth.2433
Rapid Chagas Disease Drug Target Discovery Using Directed Evolution in Drug-Sensitive Yeast.
10.1021/acschembio.6b01037
Childhood tuberculosis is associated with decreased abundance of T cell gene transcripts and impaired T cell function.
10.1371/journal.pone.0185973
Kalkipyrone B, a marine cyanobacterial γ-pyrone possessing cytotoxic and anti-fungal activities.
10.1016/j.phytochem.2015.11.011
Bacterial genome reduction using the progressive clustering of deletions via yeast sexual cycling.
10.1101/gr.182477.114
Comparative chemical genomics reveal that the spiroindolone antimalarial KAE609 (Cipargamin) is a P-type ATPase inhibitor.
10.1038/srep27806
Open Source Drug Discovery with the Malaria Box Compound Collection for Neglected Diseases and Beyond.
10.1371/journal.ppat.1005763
Magnitude and Kinetics of Anti-Severe Acute Respiratory Syndrome Coronavirus 2 Antibody Responses and Their Relationship to Disease Severity.
10.1093/cid/ciaa979
A diagnostic host response biosignature for COVID-19 from RNA profiling of nasal swabs and blood.
10.1126/sciadv.abe5984
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