In Vitro Screening for ToxCast Chemicals Binding to Thyroxine-Binding Globulin by Stephanie A. Eytcheson (4284421)

Subjects:

Antimicrobial activity of RP-1 peptide conjugate with ferrocene group by Natalia C. S. Costa (8626206)

“…The Fc-RP1 presented anti-amastigote activity against <i>Leishmania amazonensis</i> (IC₅₀ = 0.25 μmol L^–1). In comparison with amphotericin B, a second-line drug approved for leishmaniasis treatment, (IC₅₀ = 0.63 μmol L^-1), Fc-RP1 was more active and showed a 2.5-fold higher selectivity index. …”

Synthesis and Biological Evaluation of New Chalcogen Semicarbazone (<i>S</i>, <i>Se</i>) and Their Azole Derivatives against Chagas Disease by Mercedes Rubio-Hernández (20036142)

“…Three compounds were selected, based on their activity against the intracellular amastigotes (EC₅₀ < 1 μM, SI > 10) and cruzain (IC₅₀ < 100 nM, SI > 5.55) which compared favorably with the approved drug, Benznidazole, and the well-established cruzain inhibitor K777. …”

Synthesis and Biological Evaluation of New Chalcogen Semicarbazone (<i>S</i>, <i>Se</i>) and Their Azole Derivatives against Chagas Disease by Mercedes Rubio-Hernández (20036142)

“…Three compounds were selected, based on their activity against the intracellular amastigotes (EC₅₀ < 1 μM, SI > 10) and cruzain (IC₅₀ < 100 nM, SI > 5.55) which compared favorably with the approved drug, Benznidazole, and the well-established cruzain inhibitor K777. …”

Potent 5‑Cyano-6-phenyl-pyrimidin-Based Derivatives Targeting DCN1–UBE2M Interaction by Wenjuan Zhou (115285)

“…After finding a novel inhibitor <b>DC-1</b> with IC₅₀ = 1.2 μM, we performed a series of chemical optimizations, which finally led to the discovery of a potent thiazole containing 5-cyano-6-phenylpyrimidin-based inhibitor <b>DC-2</b> (IC₅₀ = 15 nM). …”

Baseline clinical profile of hospitalized COVID-19 patients with low and high renalase. by Basmah Safdar (12213257)

Histology of the perfused intestinal tract at the end of the 3 hours of extracorporeal circulation (H&E stain, 100x, scale bar = 200 μm). by Matteo Dell’Anno (10724418)

Identification of druggable small molecule antagonists of the <i>Plasmodium falciparum</i> hexose transporter PfHT and assessment of ligand access to the glucose permeation pathway... by Monique R. Heitmeier (6686069)

“…WU-1 showed comparable potency in blocking 2-DG uptake in freed parasites and inhibiting parasite growth, with an IC₅₀ of 6.1 ± 0.8 μM and EC₅₀ of 5.5 ± 0.6 μM, respectively. …”

Cell invasiveness in metastatic cancer cells exposed to their IC₅₀ Aur for 24 h. by Sara Rodríguez-Enríquez (4373332)

Migratory capacity in metastatic cancer cells exposed to IC₅₀ Aur for 24 h. by Sara Rodríguez-Enríquez (4373332)

Proportional symbol map of arsenic (As) in micrograms per liter (μg/L) in Bangladesh’s drinking well water. by Seth H. Frisbie (7821866)

The first regression of log of confirmed cases vs consecutive days for 4 of the total of 50 countries is shown. by Adam Kaplin (10156481)

The aging-induced decrease in the number of dendritic branches in neurons of the hippocampus and cerebral cortex was attenuated by the administration of GTDE. by Hui-Chuan Kuo (12368492)

TTLL12 knockdown in HEp-2 and DU145 cells decreases cell survival in the presence of nitrotyrosine. by Amit Deshpande (255211)

Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor (LPA₂), UCM-14216, Ameliorates Spinal Cord Injury in Mice by Nora Khiar-Fernández (8130210)

“…Inhibition of the type 2 lysophosphatidic acid receptor (LPA₂) has recently emerged as a new potential pharmacological approach to decrease SCI-associated damage. Toward validating this receptor as a target in SCI, we have developed a new series of LPA₂ antagonists, among which compound <b>54</b> (UCM-14216) stands out as a potent and selective LPA₂ receptor antagonist (<i>E</i>_max = 90%, IC₅₀ = 1.9 μM, <i>K</i>_D = 1.3 nM; inactive at LPA_1,3–6 receptors). …”

Novel Antagonist of the Type 2 Lysophosphatidic Acid Receptor (LPA₂), UCM-14216, Ameliorates Spinal Cord Injury in Mice by Nora Khiar-Fernández (8130210)

“…Inhibition of the type 2 lysophosphatidic acid receptor (LPA₂) has recently emerged as a new potential pharmacological approach to decrease SCI-associated damage. Toward validating this receptor as a target in SCI, we have developed a new series of LPA₂ antagonists, among which compound <b>54</b> (UCM-14216) stands out as a potent and selective LPA₂ receptor antagonist (<i>E</i>_max = 90%, IC₅₀ = 1.9 μM, <i>K</i>_D = 1.3 nM; inactive at LPA_1,3–6 receptors). …”

Example of the process used to determine time dependence of <i>ε</i>_max and IC₅₀. by Hope Murphy (8843516)

Partial correlation of <i>ε</i>_max (left column) and IC₅₀ (right column) estimates at 10 days and 20 days (first and second bar of each color, respectively) o... by Hope Murphy (8843516)

Representative μCT image slice of the femoral cortical mid-diaphysis (thresholded). by Daksh Arora (16510065)

Jag2 knockdown ameliorates mitochondrial dysfunction induced by hypoxia. by Hanhan Liu (568151)

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