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Millipore mefloquine mq
Identification of 3D7-E182D mutant active, equally potent, and wild-type active DHODH inhibitors. (a) A high-throughput screen of select GSK libraries using wild-type and E182D recombinant Pf DHODH identified 118 primary hits. On the basis of the IC 50 ratio of E182D/WT, compounds were classified as E182D mutant active ( n = 18), equally potent ( n = 21), or wild-type active ( n = 69). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 (red), wild-type active control. (b) Cell-based validation of 85 active compounds. Compounds were classified into three groups based on the EC 50 ratio of E182D/WT: equally potent ( n = 17), mutant active ( n = 7), or wild-type active ( n = 59). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 and Genz-669178 (red), wild-type active controls; dihydroartemisinin (DHA) and <t>mefloquine</t> (MQ) (white), non-DHODH inhibitor controls.
Mefloquine Mq, supplied by Millipore, used in various techniques. Bioz Stars score: 94/100, based on 8 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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1) Product Images from "Identification of Collateral Sensitivity to Dihydroorotate Dehydrogenase Inhibitors in Plasmodium falciparum"

Article Title: Identification of Collateral Sensitivity to Dihydroorotate Dehydrogenase Inhibitors in Plasmodium falciparum

Journal: ACS Infectious Diseases

doi: 10.1021/acsinfecdis.7b00217

Identification of 3D7-E182D mutant active, equally potent, and wild-type active DHODH inhibitors. (a) A high-throughput screen of select GSK libraries using wild-type and E182D recombinant Pf DHODH identified 118 primary hits. On the basis of the IC 50 ratio of E182D/WT, compounds were classified as E182D mutant active ( n = 18), equally potent ( n = 21), or wild-type active ( n = 69). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 (red), wild-type active control. (b) Cell-based validation of 85 active compounds. Compounds were classified into three groups based on the EC 50 ratio of E182D/WT: equally potent ( n = 17), mutant active ( n = 7), or wild-type active ( n = 59). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 and Genz-669178 (red), wild-type active controls; dihydroartemisinin (DHA) and mefloquine (MQ) (white), non-DHODH inhibitor controls.
Figure Legend Snippet: Identification of 3D7-E182D mutant active, equally potent, and wild-type active DHODH inhibitors. (a) A high-throughput screen of select GSK libraries using wild-type and E182D recombinant Pf DHODH identified 118 primary hits. On the basis of the IC 50 ratio of E182D/WT, compounds were classified as E182D mutant active ( n = 18), equally potent ( n = 21), or wild-type active ( n = 69). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 (red), wild-type active control. (b) Cell-based validation of 85 active compounds. Compounds were classified into three groups based on the EC 50 ratio of E182D/WT: equally potent ( n = 17), mutant active ( n = 7), or wild-type active ( n = 59). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 and Genz-669178 (red), wild-type active controls; dihydroartemisinin (DHA) and mefloquine (MQ) (white), non-DHODH inhibitor controls.

Techniques Used: Mutagenesis, High Throughput Screening Assay, Recombinant

2) Product Images from "Identification of Collateral Sensitivity to Dihydroorotate Dehydrogenase Inhibitors in Plasmodium falciparum"

Article Title: Identification of Collateral Sensitivity to Dihydroorotate Dehydrogenase Inhibitors in Plasmodium falciparum

Journal: ACS Infectious Diseases

doi: 10.1021/acsinfecdis.7b00217

Identification of 3D7-E182D mutant active, equally potent, and wild-type active DHODH inhibitors. (a) A high-throughput screen of select GSK libraries using wild-type and E182D recombinant Pf DHODH identified 118 primary hits. On the basis of the IC 50 ratio of E182D/WT, compounds were classified as E182D mutant active ( n = 18), equally potent ( n = 21), or wild-type active ( n = 69). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 (red), wild-type active control. (b) Cell-based validation of 85 active compounds. Compounds were classified into three groups based on the EC 50 ratio of E182D/WT: equally potent ( n = 17), mutant active ( n = 7), or wild-type active ( n = 59). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 and Genz-669178 (red), wild-type active controls; dihydroartemisinin (DHA) and mefloquine (MQ) (white), non-DHODH inhibitor controls.
Figure Legend Snippet: Identification of 3D7-E182D mutant active, equally potent, and wild-type active DHODH inhibitors. (a) A high-throughput screen of select GSK libraries using wild-type and E182D recombinant Pf DHODH identified 118 primary hits. On the basis of the IC 50 ratio of E182D/WT, compounds were classified as E182D mutant active ( n = 18), equally potent ( n = 21), or wild-type active ( n = 69). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 (red), wild-type active control. (b) Cell-based validation of 85 active compounds. Compounds were classified into three groups based on the EC 50 ratio of E182D/WT: equally potent ( n = 17), mutant active ( n = 7), or wild-type active ( n = 59). Control compounds are indicated on the plot: IDI-6273 (blue), mutant active control; DSM74 and Genz-669178 (red), wild-type active controls; dihydroartemisinin (DHA) and mefloquine (MQ) (white), non-DHODH inhibitor controls.

Techniques Used: Mutagenesis, High Throughput Screening Assay, Recombinant

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    Millipore mefloquine hydrochloride mq
    Sensitization to several quinoline antimalarials by PF3D7_0629500 expression and reversal with the T162E SNP. ( A ) Yeast trp1Δ cells transformed with pCM190 vector, either empty (ev) or expressing PF3D7-0629500 (Pf protein) or the same protein carrying the T162E SNP (Pf-T162E), were cultured with either 1 mM chloroquine (CQ), 1 mM amodiaquine (AQ), 25 μM <t>mefloquine</t> (MQ) or 3 mM quinine (QN). Mean data are shown from at least three independent experiments ± SEM. ( B ) RNA was extracted from wild type yeast transformed as in ( A ) and mRNA corresponding to the wild type PF3D7-0629500 ORF or SNP (T162E) version was analysed with qRT-PCR, performed in triplicate for each condition. The same amount of RNA extract was used for each reaction. There was not a significant difference (ns, according to Student’s t -test, two tailed) between the conditions either when compared by raw counts (as shown) or after normalization against ACT1 mRNA. au, arbitrary units.
    Mefloquine Hydrochloride Mq, supplied by Millipore, used in various techniques. Bioz Stars score: 98/100, based on 1 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
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    Average 98 stars, based on 1 article reviews
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    mefloquine hydrochloride mq - by Bioz Stars, 2022-12
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    Sensitization to several quinoline antimalarials by PF3D7_0629500 expression and reversal with the T162E SNP. ( A ) Yeast trp1Δ cells transformed with pCM190 vector, either empty (ev) or expressing PF3D7-0629500 (Pf protein) or the same protein carrying the T162E SNP (Pf-T162E), were cultured with either 1 mM chloroquine (CQ), 1 mM amodiaquine (AQ), 25 μM mefloquine (MQ) or 3 mM quinine (QN). Mean data are shown from at least three independent experiments ± SEM. ( B ) RNA was extracted from wild type yeast transformed as in ( A ) and mRNA corresponding to the wild type PF3D7-0629500 ORF or SNP (T162E) version was analysed with qRT-PCR, performed in triplicate for each condition. The same amount of RNA extract was used for each reaction. There was not a significant difference (ns, according to Student’s t -test, two tailed) between the conditions either when compared by raw counts (as shown) or after normalization against ACT1 mRNA. au, arbitrary units.

    Journal: Scientific Reports

    Article Title: Heterologous Expression of a Novel Drug Transporter from the Malaria Parasite Alters Resistance to Quinoline Antimalarials

    doi: 10.1038/s41598-018-20816-0

    Figure Lengend Snippet: Sensitization to several quinoline antimalarials by PF3D7_0629500 expression and reversal with the T162E SNP. ( A ) Yeast trp1Δ cells transformed with pCM190 vector, either empty (ev) or expressing PF3D7-0629500 (Pf protein) or the same protein carrying the T162E SNP (Pf-T162E), were cultured with either 1 mM chloroquine (CQ), 1 mM amodiaquine (AQ), 25 μM mefloquine (MQ) or 3 mM quinine (QN). Mean data are shown from at least three independent experiments ± SEM. ( B ) RNA was extracted from wild type yeast transformed as in ( A ) and mRNA corresponding to the wild type PF3D7-0629500 ORF or SNP (T162E) version was analysed with qRT-PCR, performed in triplicate for each condition. The same amount of RNA extract was used for each reaction. There was not a significant difference (ns, according to Student’s t -test, two tailed) between the conditions either when compared by raw counts (as shown) or after normalization against ACT1 mRNA. au, arbitrary units.

    Article Snippet: Antimalarial drugs used were amodiaquine dihydrochloride dihydrate (AMQ), chloroquine diphosphate salt (CQ), mefloquine hydrochloride (MQ) and quinine dihydrochloride (QN) (Sigma).

    Techniques: Expressing, Transformation Assay, Plasmid Preparation, Cell Culture, Quantitative RT-PCR, Two Tailed Test