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dIdentification of Inhibitors of SARS-CoV-2 3CL-Pro Enzymatic Activity Using a Small Molecule in Vitro Repurposing Screen

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (3)

Compound repurposing is an important strategy for the identification of effective treatment options against SARS-CoV-2 infection and COVID-19 disease.......

Treatment with an Anti-CK2 Synthetic Peptide Improves Clinical Response in COVID-19 Patients with Pneumonia. A Randomized and Controlled Clinical Trial

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (1)

The instrumental role of CK2 in the SARS-CoV-2 infection has pointed out this protein kinase as promising therapeutic target in COVID-19. Anti-SARS-Co......

Biosimilar or Not: Physicochemical and Biological Characterization of MabThera and Its Two Biosimilar Candidates

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (2)

The development of therapeutic biosimilar antibodies has become an important driving force of the modern biopharmaceutical industry. In this study, ph......

Design, Synthesis, Pharmacokinetics, and Biodistribution of a Series of Bone-Targeting EP4 Receptor Agonist Prodrugs for Treatment of Osteoporosis and Other Bone Conditions

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (2)

A series of bone-targeting EP4 receptor agonist conjugate prodrugs were prepared wherein a potent EP4 receptor agonist was bound to a biologically ina......

Potential Role of Lycopene in the Inhibition of Di(2-ethylhexyl) Phthalate-Induced Ferroptosis in Spleen Via Modulation of Iron Ion Homeostasis

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (1)

Di(2-ethylhexyl) phthalate (DEHP) is a synthetic chemical and widely used as a plasticizer. Humans can be exposed to DEHP through direct contact or en......

Selective Targeting of Vascular Endothelial YAP Activity Blocks EndMT and Ameliorates Unilateral Ureteral Obstruction-Induced Kidney Fibrosis

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (3)

Kidney fibrosis is accompanied by vascular dysfunction. Discovering new ways to ameliorate dysfunctional angiogenesis may bypass kidney fibrosis. YAP ......

Highly Efficient Water-Soluble Photosensitizer Based on Chlorin: Synthesis, Characterization, and Evaluation for Photodynamic Therapy

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (2)

The clinical applications of many photosensitizers (PSs) are limited because of their poor water solubility, weak tissue penetration, low chemical pur......

Compensatory Transition of Bile Acid Metabolism from Fecal Disposition of Secondary Bile Acids to Urinary Excretion of Primary Bile Acids Underlies Rifampicin-Induced Cholestasis in Beagle Dogs

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (2)

Drug induced cholestasis (DIC) is complexly associated with dysbiosis of the host-gut microbial cometabolism of bile acids (BAs). Murine animals are n......

Rational Design of Hybrid SARS-CoV-2 Main Protease Inhibitors Guided by the Superimposed Cocrystal Structures with the Peptidomimetic Inhibitors GC-376, Telaprevir, and Boceprevir

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (4)

SARS-CoV-2 main protease (M-Pro) is a cysteine protease that mediates the cleavage of viral polyproteins and is a validated antiviral drug target. M-P......

Inhibition of Histone Deacetylases 1, 2, and 3 Enhances Clearance of Cholesterol Accumulation in Niemann-Pick C1 Fibroblasts

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (3)

Niemann-Pick disease type C1 (NPC1) is a rare genetic cholesterol storage disorder caused by mutations in the NPC1 gene. Mutations in this transmembra......

Simultaneous Determination of Six Alkaloids in Rat Plasma by SPE-HPLC-MS/MS and Their Pharmacokinetics after Oral Administration of Radix aconiti Preparata Extract

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2021; 4 (1)

Simultaneous determination of the content of six alkaloids (aconitine, hypoaconitine, mesaconitine, benzoylaconine, benzoylhypaconine, and benzoylmesa......

Identification of PDCD2 as a Candidate Target of Andrographolide That Arrests the Tumor Cell Cycle by Human Proteome-Scale Screening

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2022; 5 (7)

Andrographolide (andro) and its derivatives have been reported to have antitumor activity by arresting the cell cycle. However, the more precise mecha......

Evaluating a Specific Dual ROCK Inhibitor against Bleomycin-Induced Idiopathic Pulmonary Fibrosis in Rats

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2022; 5 (9)

Idiopathic pulmonary fibrosis (IPF) is a chronic, progressive, and fatal lung disease. Rho-associated protein kinases (ROCK) 1/2 are promising therape......

NFL-TBS.40-63 Peptide Gold Complex Nanovector: A Novel Therapeutic Approach to Increase Anticancer Activity by Breakdown of Microtubules in Pancreatic Adenocarcinoma (PDAC)

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2022; 5 (12)

The role of the NFL-TBS.40-63 peptide is to destroy the microtubule network of target glioma cancer cells. Recently, we have conceived a gold-complex ......

Monomerization of Homodimeric Trefoil Factor 3 (TFF3) by an Aminonitrile Compound Inhibits TFF3-Dependent Cancer Cell Survival

期刊: ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE, 2022; 5 (9)

Trefoil factor 3 (TFF3) is a secreted protein with an established oncogenic function and a highly significant association with clinical progression of......

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