Novel cruzain inhibitors for the treatment of Chagas' disease. [PDF]
The protozoan parasite Trypanosoma cruzi, the etiological agent of Chagas' disease, affects millions of individuals and continues to be an important global health concern.
Arkin, Michelle R+6 more
core +1 more source
This study demonstrates that the resveratrol analogue, trans‐4,4′‐dihydroxystilbene (DHS), exhibits synergistic anti‐tumor activity with the PARP inhibitor talazoparib, inducing significant ovarian cancer cell death. The synergistic effect of this combination arises from the concurrent downregulation of homologous recombination factors and the ...
Ganesh Pai Bellare+7 more
wiley +1 more source
Design of a folding inhibitor of the HIV-1 Protease [PDF]
Being HIV-1-PR an essential enzyme in the viral life cycle, its inhibition can control AIDS. Because the folding of single domain proteins, like HIV-1-PR is controlled by local elementary structures (LES, folding units stabilized by strongly interacting, highly conserved amino acids) which have evolved over myriads of generations to recognize and ...
arxiv
Unveiling the molecular mechanism of SARS-CoV-2 main protease inhibition from 92 crystal structures [PDF]
Currently, there is no effective antiviral drugs nor vaccine for coronavirus disease 2019 (COVID-19) caused by acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Due to its high conservativeness and low similarity with human genes, SARS-CoV-2 main protease (M$^{\text{pro}}$) is one of the most favorable drug targets.
arxiv
Staurosporine induces necroptotic cell death under caspase-compromised conditions in U937 cells [PDF]
For a long time necrosis was thought to be an uncontrolled process but evidences recently have revealed that necrosis can also occur in a regulated manner.
Barna, Gabor+6 more
core +3 more sources
HNF3α Targets Nckap1l and Promotes Renal Fibrosis Following Ischemia‐Reperfusion Injury
Hepatocyte Nuclear Factor 3 alpha (HNF3α) is significantly upregulated in renal tubular epithelial cells of CKD patients and fibrotic mice. Deletion of HNF3α mitigates IRI‐induced renal fibrosis, while overexpression worsens it. HNF3α directly regulates NCK‐associated protein 1‐like (Nckap1l), whose overexpression exacerbates fibrosis.
Ling Hou+7 more
wiley +1 more source
Drug Repurposing to find Inhibitors of SARS-CoV-2 Main Protease [PDF]
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is the strain of coronavirus that causes coronavirus disease 2019 (COVID-19), the respiratory illness responsible for the COVID-19 pandemic. Currently there is no known vaccine or specific antiviral treatment for COVID-19 and so, there is an urgent need for expedite discovery of new ...
arxiv
A neutrophil-dependent pathway for the generation of a neutral peptide mediator: partial characterization of components and control by alpha-1-antitrypsin. [PDF]
A biologically active neutral peptide mediator is cleaved from a plasma protein substrate by an alpha-1-antitrypsin-inhibitable serine protease apparently residing on the membrane of the human neutrophil. The peptide mediator has an approximate mol wt of
Austen, KF, Goetzl, EJ, Wintroub, BU
core
Method to Predict Crowding Effects by Postprocessing Molecular Dynamics Trajectories: Application to the Flap Dynamics of HIV-1 Protease. [PDF]
The internal dynamics of proteins inside of cells may be affected by the crowded intracellular environments. Here, we test a novel approach to simulations of crowding, in which simulations in the absence of crowders are postprocessed to predict crowding ...
McCammon, J Andrew+3 more
core +2 more sources
In mice challenged with lipopolysaccharide/D‐galactosamine (L/G), Mas signaling increased SHP2 in hepatic Col4a1+ endothelial cells, inhibiting farnesoid X receptor (FXR), potentially due to enterogenic deoxycholic acid. This inhibition activates sphingosine‐1‐phosphate‐induced Raf/MEK/ERK signaling in Cldn1+CD177+ neutrophils, causing neutrophil ...
Bo Yang+11 more
wiley +1 more source