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61
Targeting IGF perturbs global replication through ribonucleotide reductase dysfunction
Published 2021“…Reciprocal screens of ATM-proficient/deficient fibroblasts identified an IGF1R inhibitor as the top hit. IGF inhibition selectively compromised growth of ATM-null cells and spheroids and caused regression of ATM-null xenografts. …”
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62
RASSF1A regulation of transcription factors in tumourigenesis and stem cell fate determination
Published 2014“…By performing a genetic screen in mice using Sleeping Beauty (SB) transposon-mediated insertional mutagenesis, we identified candidate genes associated with tumourigenesis in the absence of Rassf1a. A top hit in our screen was the terminal differentiation transcription factor Runx2. …”
Thesis -
63
Identifying regulators of chronic myeloid leukaemic (CML) stem cell quiescence and discovering effective novel therapies for CML relapse
Published 2022“…Growth Arrest Specific 2 (GAS2) was the ‘top hit’ and therefore the candidate I took forward for functional validation.…”
Thesis -
64
Diverse inhibitor chemotypes targeting Trypanosoma cruzi CYP51.
Published 2012-01-01“…Two pools of hits partially overlapped. The top hit inhibited T. cruzi with EC(50) of 17 nM and was trypanocidal at 40 nM. …”
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65
In silicoCharacterization of UGT74G1Protein in Stevia rebaudianaBertoni Accession MS007
Published 2021-09-01“…Homologous search using BLASTp shows high sim-ilarity to Q6VAA6 RecName: Full=UDP-glycosyltransferase 74G1 (S. rebaudiana) as the top hit sequence. InterPro family and domain protein motif search revealed UDP-glucuronosyl/UDP-glucosyltransferase (IPR002213) and UDP-glycosyltrans-ferase family, conserved site (IPR035595). …”
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66
Accommodating receptor flexibility and free energy calculation to reduce false positive binders in the discovery of natural products blockers of SARS-COV-2 spike RBD-ACE2 interface
Published 2021-09-01“…Owing to their desirable pharmacokinetic properties, the presented top hit natural products are suggested for further SARS-COV-2 molecular targets and subsequent in vitro and in vivo evaluations.…”
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67
Computational Screening of Plant-Derived Natural Products against SARS-CoV-2 Variants
Published 2022-11-01“…Results showed that rutin, EGCG, hesperidin, withanolide G, rosmarinic acid, diosmetin, myricetin, epicatechin and quercetin were the top hit compounds against each of the SARS-CoV-2 variants. …”
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68
Drug repurposing in psoriasis, performed by reversal of disease-associated gene expression profiles
Published 2022-01-01“…The drugs with most negative connectivity scores are ranked efficient and vice versa. The top hit drugs are verified using the literature survey of the peer reviewed journal, electronic health records, patents, and hospital database. …”
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69
Identification of BACE2 as an avid ß-amyloid-degrading protease
Published 2012-09-01“…</p> <p>Results</p> <p>The top hit emerging from the screen was ß-site amyloid precursor protein-cleaving enzyme 2 (BACE2), a rather unexpected finding given the well-established role of its close homolog, BACE1, in the production of Aß. …”
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70
Characterization of the transcriptome of an ecologically important avian species, the Vinous-throated Parrotbill <it>Paradoxornis webbianus bulomachus</it> (Paradoxornithidae; Aves...
Published 2012-04-01“…Of 7,779 contigs retained for a top-hit species distribution analysis, the majority (about 86%) were matched to known Zebra Finch and chicken transcripts. …”
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71
First Report of Aeromonas schubertii Infection in Striped Snakehead Channa striata (Bloch, 1793) Fingerlings in Malaysia
Published 2024-04-01“…The isolated strain was identified as Aeromonas schubertii based on the assembled 16S rRNA sequence showing nucleotide identity of 99.73% (top hit) to A. schubertii (GenBank Accession: NR_037014.2) while only a nucleotide identity of 97.55% was observed against Aeromonas hydrophila (GenBank Accession: NR_119190.1-), respectively. …”
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72
Mendelian randomization integrating GWAS and eQTL data revealed genes pleiotropically associated with major depressive disorder
Published 2021-04-01“…The prime-specific gene BTN3A2 (corresponding probe: ENSG00000186470.9) was the top hit showing pleiotropic association with MDD in 9 of the 13 brain regions and in brain-eMeta, after correction for multiple testing. …”
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73
Secretome Analyses Identify FKBP4 as a <i>GBA1</i>-Associated Protein in CSF and iPS Cells from Parkinson’s Disease Patients with <i>GBA1</i> Mutations
Published 2024-01-01“…Reduced intracellular level of the top hit, FKPB4, was confirmed via Western Blot. In conclusion, our findings identify significantly altered CSF GBA1-PD-associated proteins with FKPB4 being firmly attributed to mDA neurons.…”
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74
Eltrombopag inhibits the proliferation of Ewing sarcoma cells via iron chelation and impaired DNA replication
Published 2020-11-01“…We then tested the effects of a top hit from the screen on cell proliferation, cell cycle progression, and activation of the DNA damage pathway using Ewing sarcoma cell lines. …”
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75
A Chemical Screen Identifies Compounds Capable of Selecting for Haploidy in Mammalian Cells
Published 2019-07-01“…Based on this property, we have now performed a phenotypic chemical screen in human haploid HAP1 cells aiming to identify compounds that facilitate the maintenance of haploid cells. Our top hit was 10-Deacetyl-baccatin-III (DAB), a chemical precursor in the synthesis of Taxol, which selects for haploid cells in HAP1 and mouse haploid embryonic stem cultures. …”
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76
Structure Prediction of Human Fatty Acid Synthase–Dehydratase: A Plausible Model for Understanding Active Site Interactions
Published 2016-01-01“…The inhibitory efficacy of the top hit ligands was validated by performing molecular dynamics simulation for 20 ns, where in the ligand NSC71039 exhibited good enzyme inhibition characteristics and exhibited dose-dependent anticancer cytotoxicity in retinoblastoma cancer cells in vitro.…”
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77
Epigenome-wide DNA methylation in obsessive-compulsive disorder
Published 2022-06-01“…After quality control, nine epigenome-wide significant quantitative trait methylation sites (QTMs) and 21 suggestive hits were discerned in the final sample of 68 patients and 68 controls. The top hit (cg24159721) and four other significant QTMs (cg11894324, cg01070250, cg11330075, cg15174812) map to the region of the microRNA 12136 gene (MIR12136). …”
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78
MyosinA is a druggable target in the widespread protozoan parasite Toxoplasma gondii.
Published 2023-05-01“…To this end, we first sought to identify inhibitors of TgMyoA by screening a collection of 50,000 structurally diverse small molecules for inhibitors of the recombinant motor's actin-activated ATPase activity. The top hit to emerge from the screen, KNX-002, inhibited TgMyoA with little to no effect on any of the vertebrate myosins tested. …”
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79
First report of Aeromonas schubertii infection in Striped Snakehead Channa striata (Bloch, 1793) fingerlings in Malaysia
Published 2024“…The isolated strain was identified as Aeromonas schubertii based on the assembled 16S rRNA sequence showing nucleotide identity of 99.73% (top hit) to A. schubertii (GenBank Accession: NR_037014.2) while only a nucleotide identity of 97.55% was observed against Aeromonas hydrophila (GenBank Accession: NR_119190.1-), respectively. …”
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80
Molecular Mimicry Analyses Unveiled the Human Herpes Simplex and Poxvirus Epitopes as Possible Candidates to Incite Autoimmunity
Published 2022-11-01“…The vast majority of these top-hit homolog epitopic peptides belong to the herpes simplex and poxvirus families. …”
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Article