scholarly journals Advanced Models for Target Validation & Drug Discovery in Prostate Cancer

10.5772/25629 ◽  
2011 ◽  
Author(s):  
Malin Akerfelt ◽  
Ville Harma ◽  
Matthias Nees
Keyword(s):  
Prostate Cancer ◽  
Drug Discovery ◽  
Target Validation

Role of Cytochrome P450 in Prostate Cancer and its Therapy

2020 ◽  
Vol 16 (1) ◽  
pp. 63-73 ◽  
Author(s):  
Rishabh Kaushik ◽  
Sheeza Khan ◽  
Meesha Sharma ◽  
Srinivasan Hemalatha ◽  
Zeba Mueed ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cytochrome P450 ◽  
Drug Discovery ◽  
Cholesterol Metabolism ◽  
Molecular Targets ◽  
Health Concern ◽  
Metabolic Functions ◽  
Novel Drugs ◽  
Genes Encoding ◽  
Causes Of Mortality

Prostate cancer has become a global health concern as it is one of the leading causes of mortality in males. With the emerging drug resistance to conventional therapies, it is imperative to unravel new molecular targets for disease prevention. Cytochrome P450 (P450s or CYPs) represents a unique class of mixed-function oxidases which catalyses a wide array of biosynthetic and metabolic functions including steroidogenesis and cholesterol metabolism. Several studies have reported the overexpression of the genes encoding CYPs in prostate cancer cells and how they can be used as molecular targets for drug discovery. But due to functional redundancy and overlapping expression of CYPs in several other metabolic pathways there are several impediments in the clinical efficacy of the novel drugs reported till now. Here we review the most crucial P450 enzymes which are involved in prostate cancer and how they can be used as molecular targets for drug discovery along with the clinical limitations of the currently existing CYP inhibitors.

Screening the receptorome: an efficient approach for drug discovery and target validation

2006 ◽  
Vol 11 (15-16) ◽  
pp. 708-716 ◽  
Author(s):  
Ryan T. Strachan ◽  
Gina Ferrara ◽  
Bryan L. Roth
Keyword(s):  
Drug Discovery ◽  
Target Validation ◽  
Efficient Approach

scholarly journals Computer-aided drug discovery of Myc-Max inhibitors as potential therapeutics for prostate cancer

2018 ◽  
Vol 160 ◽  
pp. 108-119 ◽  
Author(s):  
Lavinia A. Carabet ◽  
Nada Lallous ◽  
Eric Leblanc ◽  
Fuqiang Ban ◽  
Helene Morin ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Drug Discovery ◽  
Computer Aided ◽  
Potential Therapeutics

scholarly journals Three-Dimensional Cell Cultures as an In Vitro Tool for Prostate Cancer Modeling and Drug Discovery

2020 ◽  
Vol 21 (18) ◽  
pp. 6806 ◽  
Author(s):  
Fabrizio Fontana ◽  
Michela Raimondi ◽  
Monica Marzagalli ◽  
Michele Sommariva ◽  
Nicoletta Gagliano ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cell Culture ◽  
Drug Discovery ◽  
Cancer Cells ◽  
Cell Cultures ◽  
Antitumor Agents ◽  
Three Dimensional ◽  
3D Cell Culture ◽  
Cancer Modeling

In the last decade, three-dimensional (3D) cell culture technology has gained a lot of interest due to its ability to better recapitulate the in vivo organization and microenvironment of in vitro cultured cancer cells. In particular, 3D tumor models have demonstrated several different characteristics compared with traditional two-dimensional (2D) cultures and have provided an interesting link between the latter and animal experiments. Indeed, 3D cell cultures represent a useful platform for the identification of the biological features of cancer cells as well as for the screening of novel antitumor agents. The present review is aimed at summarizing the most common 3D cell culture methods and applications, with a focus on prostate cancer modeling and drug discovery.

scholarly journals Encoded Library Technologies as Integrated Lead Finding Platforms for Drug Discovery

Molecules ◽  
2019 ◽  
Vol 24 (8) ◽  
pp. 1629 ◽  
Author(s):  
Johannes Ottl ◽  
Lukas Leder ◽  
Jonas V. Schaefer ◽  
Christoph E. Dumelin
Keyword(s):  
Drug Discovery ◽  
Cyclic Peptides ◽  
Chemical Space ◽  
Pharmaceutical Research ◽  
Peptide Libraries ◽  
Assay Development ◽  
Low Molecular Weight ◽  
Target Validation ◽  
Lead Finding ◽  
Chemical Matter

The scope of targets investigated in pharmaceutical research is continuously moving into uncharted territory. Consequently, finding suitable chemical matter with current compound collections is proving increasingly difficult. Encoded library technologies enable the rapid exploration of large chemical space for the identification of ligands for such targets. These binders facilitate drug discovery projects both as tools for target validation, structural elucidation and assay development as well as starting points for medicinal chemistry. Novartis internalized two complementing encoded library platforms to accelerate the initiation of its drug discovery programs. For the identification of low-molecular weight ligands, we apply DNA-encoded libraries. In addition, encoded peptide libraries are employed to identify cyclic peptides. This review discusses how we apply these two platforms in our research and why we consider it beneficial to run both pipelines in-house.

Kinase Chemogenomics: Targeting the Human Kinome for Target Validation and Drug Discovery

2004 ◽  
Vol 4 (3) ◽  
pp. 235-253 ◽  
Author(s):  
E. Haar ◽  
W. Walters ◽  
S. Pazhanisamy ◽  
P. Taslimi ◽  
A. Pierce ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Target Validation ◽  
Human Kinome
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