Search alternatives:
ng decrease » _ decrease (Expand Search), a decrease (Expand Search), gy decreased (Expand Search)
nn decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
we decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
nm decrease » _ decrease (Expand Search), a decrease (Expand Search), gy decreased (Expand Search)
50 ng » 50 mg (Expand Search), 10 ng (Expand Search), 5 ng (Expand Search)
5 nm » 5 mm (Expand Search), 5 cm (Expand Search)
ng decrease » _ decrease (Expand Search), a decrease (Expand Search), gy decreased (Expand Search)
nn decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
we decrease » _ decrease (Expand Search), a decrease (Expand Search), mean decrease (Expand Search)
nm decrease » _ decrease (Expand Search), a decrease (Expand Search), gy decreased (Expand Search)
50 ng » 50 mg (Expand Search), 10 ng (Expand Search), 5 ng (Expand Search)
5 nm » 5 mm (Expand Search), 5 cm (Expand Search)
-
41
-
42
<i>In vitro</i> susceptibility responses of field isolates to antimalarials during the study period.
Published 2024Subjects: -
43
-
44
Discovery of the Triazolo[1,5‑<i>a</i>]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance...
Published 2021“…Targeting P-glycoprotein (ABCB1 or P-gp) has been recognized as a promising strategy to overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo[1,5-<i>a</i>]pyrimidine derivative <b>WS-898</b> as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC<sub>50</sub> = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”
-
45
Discovery of the Triazolo[1,5‑<i>a</i>]Pyrimidine-Based Derivative WS-898 as a Highly Efficacious and Orally Bioavailable ABCB1 Inhibitor Capable of Overcoming Multidrug Resistance...
Published 2021“…Targeting P-glycoprotein (ABCB1 or P-gp) has been recognized as a promising strategy to overcome multidrug resistance. Here, we reported our medicinal chemistry efforts that led to the discovery of the triazolo[1,5-<i>a</i>]pyrimidine derivative <b>WS-898</b> as a highly effective ABCB1 inhibitor capable of reversing paclitaxel (PTX) resistance in drug-resistant SW620/Ad300, KB-C2, and HEK293/ABCB1 cells (IC<sub>50</sub> = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”
-
46
Structure-Based Design of a Chemical Probe Set for the 5‑HT<sub>5A</sub> Serotonin Receptor
Published 2022“…Docking over 6 million molecules against a 5-HT<sub>5A</sub>R homology model identified 5 mid-μM ligands, one of which was optimized to <b>UCSF678</b>, a 42 nM arrestin-biased partial agonist at the 5-HT<sub>5A</sub>R with a more restricted off-target profile and decreased assay liabilities versus SB-699551. …”
-
47
Structure-Based Design of a Chemical Probe Set for the 5‑HT<sub>5A</sub> Serotonin Receptor
Published 2022“…Docking over 6 million molecules against a 5-HT<sub>5A</sub>R homology model identified 5 mid-μM ligands, one of which was optimized to <b>UCSF678</b>, a 42 nM arrestin-biased partial agonist at the 5-HT<sub>5A</sub>R with a more restricted off-target profile and decreased assay liabilities versus SB-699551. …”
-
48
-
49
-
50
Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors
Published 2022“…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i><sub>i</sub> = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i><sub>i</sub> = 0.436 nM) substitution of the <i>N</i><sup>4</sup>-benzyloxy group decreased <i>K</i><sub>i</sub> by ∼20-fold. …”
-
51
Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors
Published 2022“…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i><sub>i</sub> = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i><sub>i</sub> = 0.436 nM) substitution of the <i>N</i><sup>4</sup>-benzyloxy group decreased <i>K</i><sub>i</sub> by ∼20-fold. …”
-
52
Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors
Published 2022“…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i><sub>i</sub> = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i><sub>i</sub> = 0.436 nM) substitution of the <i>N</i><sup>4</sup>-benzyloxy group decreased <i>K</i><sub>i</sub> by ∼20-fold. …”
-
53
-
54
-
55
-
56
-
57
High resolution structures visible with the 25 nm zone plate objective.
Published 2022“…(<b>F</b>) The width of nuclear capsids was remeasured after imaging with the 25 nm zone plate: 124.5 nm ± 0.96 nm SEM (n = 80 from 4 tomograms; 8.55 nm SD). …”
-
58
-
59
-
60