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... by Shuai Wang (109515)

“…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 (IC₅₀ = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”

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... by Shuai Wang (109515)

“…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 (IC₅₀ = 5.0, 3.67, and 3.68 nM, respectively), more potent than verapamil and zosuquidar. …”

Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors by Mirko Scortichini (4007366)

“…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i>_i = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i>_i = 0.436 nM) substitution of the <i>N</i>⁴-benzyloxy group decreased <i>K</i>_i by ∼20-fold. …”

Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors by Mirko Scortichini (4007366)

“…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i>_i = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i>_i = 0.436 nM) substitution of the <i>N</i>⁴-benzyloxy group decreased <i>K</i>_i by ∼20-fold. …”

Structure–Activity Relationship of 3‑Methylcytidine-5′-α,β-methylenediphosphates as CD73 Inhibitors by Mirko Scortichini (4007366)

“…We now expand the structure–activity relationship of pyrimidine nucleotides as human CD73 inhibitors. 4-Chloro (MRS4598 <b>16</b>; <i>K</i>_i = 0.673 nM) and 4-iodo (MRS4620 <b>18</b>; <i>K</i>_i = 0.436 nM) substitution of the <i>N</i>⁴-benzyloxy group decreased <i>K</i>_i by ∼20-fold. …”

Loss of <i>SLC4A11</i> expression in hCEnC leads to decreased cell barrier function. by Doug D. Chung (3611387)

Oxytocin decreases postsynaptic CeA spontaneous GABAergic transmission and blocks presynaptic alcohol effects. by Brendan J. Tunstall (6593357)

“…<p>(A, Top) Representative GABA_A-mediated sIPSCs of CeA neurons from nondependent and dependent rats prior to (baseline) and during application of oxytocin (500 nM). …”

Mean absolute SHAP values of the most important predictors for APM_MN in each of the five folds of the first repeat. by Shubhayu Bhattacharyay (11242977)

SARS-CoV-2 specific T cell frequencies analysis comparing pre-existing conditions show no significant differences. by Katherine M. Littlefield (12647420)

Panel probit models: Dummy variable which takes a value of 1 for a top 5 publication. by Sergey V. Popov (6719075)

Delayed boosting with ALVAC-HIV/AIDSVAX B/E or AIDSVAX B/E increases V1V2-specific IgG concentration and breadth. by LaTonya D. Williams (3140490)

Magnitude-breadth of linear V2 hotspot binding response. by LaTonya D. Williams (3140490)

Pyrimidine nucleotides are decreased in hypoxia, while precursors accumulate. by Emily B. Cohen (9106088)

The decrease or inhibition of Hsp90 induced REST degradation. by Raúl Orozco-Díaz (7067624)

“…<p>(A) Effect of Hsp90α ASO on cell viability. Differentiated SH-SY5Y cells were transfected with different concentrations of Hsp90α ASO. …”

GSK343 decreased neuroblastoma viability, proliferation, and motility. by Laura V. Bownes (10276762)

“…<p>(A) SK-N-AS, SK-N-BE(2), SH-EP and WAC(2) cells (1.5 × 10³ cells) were treated with increasing concentrations of GSK343 (0, 5, 15, 25 μM) for 24 hours and viability was measured using alamarBlue^® assay. …”

Bortezomib decreases osteoclasts and improves fracture repair in mice. by Hengwei Zhang (2397610)

Foldases and holdases each decrease the level of unfolded protein. by Adam MR de Graff (9767829)

MigC interacts with and decreases the activity of MurD. by Jeanette M. Critchlow (21553796)

Germ cell size decreases before corpse formation. by Tea Kohlbrenner (19476160)

MMR mutants show decreased mating-type silencing. by Qian Liu (135614)

“…Cells were five-fold serially diluted and grown at 30℃ followed by storage in 4℃ until clear red pigment formation could be seen (15 days). …”