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Metalloproteases and inhibitors in arthritic diseases.
TLDR
This chapter addresses the different metalloprotease enzymes and sub-families and their implication in arthritic diseases, and assess physiological and chemical metalliprotease inhibitors, and for the latter, the current inhibitory classes of compounds being studied. Expand
Real-time Genomic Characterization of Advanced Pancreatic Cancer to Enable Precision Medicine.
TLDR
Using an integrated multidisciplinary biopsy program, it is demonstrated that real-time genomic characterization of advanced PDAC can identify clinically relevant alterations that inform management of this difficult disease. Expand
First-in-Class ERK1/2 Inhibitor Ulixertinib (BVD-523) in Patients with MAPK Mutant Advanced Solid Tumors: Results of a Phase I Dose-Escalation and Expansion Study.
TLDR
The first-in-human dose-escalation study of an ERK1/2 inhibitor for the treatment of patients with advanced solid tumors is described, which has an acceptable safety profile with favorable pharmacokinetics and has shown early evidence of clinical activity in NRAS- and BRAF V600- and non-V600-mutant solid-tumor malignancies. Expand
The ligand-dependent interaction of mineralocorticoid receptor with coactivator and corepressor peptides suggests multiple activation mechanisms.
TLDR
The coregulator and corepressor interactions with the mineralocorticoid receptor (MR) indicate that MR ligand binding domain (LBD) interacts strongly with only a few specific coactivator peptides in the presence of the agonist aldosterone and that these interactions are blocked by the antagonist eplerenone. Expand
Targeting the MAPK Signaling Pathway in Cancer: Promising Preclinical Activity with the Novel Selective ERK1/2 Inhibitor BVD-523 (Ulixertinib)
TLDR
It is demonstrated BVD-523 holds promise as a treatment for ERK-dependent cancers, including those whose tumors have acquired resistance to other treatments targeting upstream nodes of the MAPK pathway. Expand
Eradication of Tumors through Simultaneous Ablation of CD276/B7-H3-Positive Tumor Cells and Tumor Vasculature.
TLDR
It is demonstrated that the cell-surface protein CD276/B7-H3 is broadly overexpressed by multiple tumor types on both cancer cells and tumor-infiltrating blood vessels, making it a potentially ideal dual-compartment therapeutic target. Expand
Novel, selective Δ6 or Δ5 fatty acid desaturase inhibitors as antiinflammatory agents in mice
TLDR
The Delta6 desaturase may be a target for development of antiinflammatory drugs whose mechanism of action is unique because of its correlation existed between inhibition of liver Delta6 Desaturase activity and decreases in edema. Expand
Novel, selective delta6 or delta5 fatty acid desaturase inhibitors as antiinflammatory agents in mice.
TLDR
The Delta6 desaturase may be a target for development of antiinflammatory drugs whose mechanism of action is unique because of its correlation existed between inhibition of liver Delta6 Desaturase activity and decreases in edema. Expand
Molecular cloning and expression of human leukotriene C4 synthase.
TLDR
The cloning and expression of human LTC4S provide the basis for a better understanding of this key enzyme in leukotriene biosynthesis, which shows no homology to other glutathione S-transferases. Expand
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