785 Benserazide is a novel inhibitor targeting PKM2 in melanoma treatment

The TWEAK Receptor Fn14 is a Novel Therapeutic Target in Melanoma: Immunotoxins Targeting Fn14 Receptor for Malignant Melanoma Treatment

Fibroblast growth factor-inducible protein 14 (Fn14), the cell surface receptor for tumor necrosis factor-like weak inducer of apoptosis (TWEAK), is overexpressed in various human solid tumor types and can be a negative prognostic indicator. We detected Fn14 expression in ∼60% of the melanoma cell lines we tested, including both B-Raf WT and B-Raf(V600E) lines. Tumor tissue microarray analysis ...

Benserazide, a dopadecarboxylase inhibitor, suppresses tumor growth by targeting hexokinase 2

BACKGROUND Hexokinase (HK) is the rate-limiting enzyme in the first reaction of glycolysis. And Hexokinase 2 (HK2) is most closely related to malignant tumor which expresses at higher level compared with normal cells. HK2 plays a pivotal role in tumor initiation and maintenance, which provides a new target for cancer therapy. METHODS Structure-based virtual ligand screening was used in hit id...

A Novel Small-molecule Inhibitor Targeting

In Silico Screening Identifies a Novel Potential PARP1 Inhibitor Targeting Synthetic Lethality in Cancer Treatment.

Synthetic lethality describes situations in which defects in two different genes or pathways together result in cell death. This concept has been applied to drug development for cancer treatment, as represented by Poly (ADP-ribose) polymerase (PARPs) inhibitors. In the current study, we performed a computational screening to discover new PARP inhibitors. Among the 11,247 compounds analyzed, one...

Targeting KIT for Treatment Of Advanced Melanoma

This is a remarkable time for melanoma research and treatment. Before this year, approved agents available for the treatment of metastatic melanoma were limited to dacarbazine (DTIC) and interleukin-2 (IL-2), with benefits achieved in only a small minority of patients treated with either drug. In 2011, however, two new agents, ipilimumab (YervoyTM) and vemurafenib (ZelborafTM), were approved, w...