At the Crossroads Between Mitochondrial Metabolite Transport and Apoptosis: VDAC1 as an Emerging Cancer Drug Target

2014 ◽  
pp. 345-373
Author(s):  
Varda Shoshan-Barmatz ◽  
Anna Shteinfer ◽  
Danya Ben-Hail ◽  
Tasleem Arif ◽  
Dario Mizrachi
Keyword(s):  
Drug Target ◽  
Cancer Drug ◽  
Metabolite Transport

Computational drug analysis of APOBEC3B enzyme: Promising cancer drug target

2020 ◽  
Author(s):  
Zachary Daniel Smith ◽  
Bill R Miller III
Keyword(s):  
Drug Target ◽  
Drug Analysis ◽  
Cancer Drug

Inhibitor Binding Sites in the Protein Tyrosine Phosphatase SHP-2

2020 ◽  
Vol 20 (11) ◽  
pp. 1017-1030
Author(s):  
Haonan Zhang ◽  
Zhengquan Gao ◽  
Chunxiao Meng ◽  
Xiangqian Li ◽  
Dayong Shi
Keyword(s):  
Small Molecule ◽  
Protein Tyrosine Phosphatase ◽  
Binding Sites ◽  
Drug Target ◽  
Tyrosine Phosphatase ◽  
Cancer Drug ◽  
Cellular Activity ◽  
Binding Modes ◽  
Inhibitor Binding ◽  
Protein Tyrosine

Protein tyrosine phosphatase 2 (SHP-2) has long been proposed as a cancer drug target. Several small-molecule compounds with different mechanisms of SHP-2 inhibition have been reported, but none are commercially available. Pool selectivity over protein tyrosine phosphatase 1 (SHP-1) and a lack of cellular activity have hindered the development of selective SHP-2 inhibitors. In this review, we describe the binding modes of existing inhibitors and SHP-2 binding sites, summarize the characteristics of the sites involved in selectivity, and identify the suitable groups for interaction with the binding sites.

The Protein Acetyltransferase ARD1: A Novel Cancer Drug Target?

2008 ◽  
Vol 8 (7) ◽  
pp. 545-553 ◽  
Author(s):  
Thomas Arnesen ◽  
Paul Thompson ◽  
Jan Varhaug ◽  
Johan Lillehaug
Keyword(s):  
Drug Target ◽  
Cancer Drug ◽  
Protein Acetyltransferase

Abstract 2139: Enabling cancer drug target discovery through genome-scale identification of synthetic lethal paralog pairs

2021 ◽  
Author(s):  
Phoebe C. Parrish ◽  
James D. Thomas ◽  
Shriya Kamlapurkar ◽  
Robert K. Bradley ◽  
Alice H. Berger
Keyword(s):  
Drug Target ◽  
Cancer Drug ◽  
Drug Target Discovery ◽  
Target Discovery ◽  
Synthetic Lethal ◽  
Genome Scale

scholarly journals Dysregulated Pyrimidine Biosynthesis Contributes to 5-FU Resistance in SCLC Patient-Derived Organoids but Response to a Novel Polymeric Fluoropyrimidine, CF10

Cancers ◽  
2020 ◽  
Vol 12 (4) ◽  
pp. 788 ◽  
Author(s):  
William H. Gmeiner ◽  
Lance D. Miller ◽  
Jeff W. Chou ◽  
Anthony Dominijanni ◽  
Lysette Mutkus ◽  
...  
Keyword(s):  
Drug Target ◽  
Pyrimidine Biosynthesis ◽  
Cancer Drug ◽  
Rna Seq ◽  
Novel Approach ◽  
Anti Cancer ◽  
New Treatments ◽  
Insight Into ◽  
Sclc Patient ◽  
Identify Gene Expression

Chemo-immunotherapy is central to the treatment of small cell lung cancer (SCLC). Despite modest progress made with the addition of immunotherapy, current cytotoxic regimens display minimal survival benefit and new treatments are needed. Thymidylate synthase (TS) is a well-validated anti-cancer drug target, but conventional TS inhibitors display limited clinical efficacy in refractory or recurrent SCLC. We performed RNA-Seq analysis to identify gene expression changes in SCLC biopsy samples to provide mechanistic insight into the potential utility of targeting pyrimidine biosynthesis to treat SCLC. We identified systematic dysregulation of pyrimidine biosynthesis, including elevated TYMS expression that likely contributes to the lack of efficacy for current TS inhibitors in SCLC. We also identified E2F1-3 upregulation in SCLC as a potential driver of TYMS expression that may contribute to tumor aggressiveness. To test if TS inhibition could be a viable strategy for SCLC treatment, we developed patient-derived organoids (PDOs) from human SCLC biopsy samples and used these to evaluate both conventional fluoropyrimidine drugs (e.g., 5-fluorouracil), platinum-based drugs, and CF10, a novel fluoropyrimidine polymer with enhanced TS inhibition activity. PDOs were relatively resistant to 5-FU and while moderately sensitive to the front-line agent cisplatin, were relatively more sensitive to CF10. Our studies demonstrate dysregulated pyrimidine biosynthesis contributes to drug resistance in SCLC and indicate that a novel approach to target these pathways may improve outcomes.

scholarly journals Pim-1 kinase as cancer drug target: An update

2015 ◽  
Vol 4 (2) ◽  
pp. 140-146 ◽  
Author(s):  
YERNAR TURSYNBAY ◽  
JINFU ZHANG ◽  
ZHI LI ◽  
TURSONJAN TOKAY ◽  
ZHAXYBAY ZHUMADILOV ◽  
...  
Keyword(s):  
Drug Target ◽  
Cancer Drug

The Ubiquitin-Proteasome System (UPS) as a Cancer Drug Target: Emerging Mechanisms and Therapeutics

2014 ◽  
pp. 225-264 ◽  
Author(s):  
Lydia Mata-Cantero ◽  
Sofía Lobato-Gil ◽  
Fabienne Aillet ◽  
Valérie Lang ◽  
Manuel S. Rodriguez
Keyword(s):  
Drug Target ◽  
Ubiquitin Proteasome System ◽  
Cancer Drug ◽  
Ubiquitin Proteasome
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