A simple yeast-based system for analyzing inhibitor resistance in the human cancer drug targets Hsp90α/β

2010 ◽  
Vol 79 (11) ◽  
pp. 1581-1588 ◽  
Author(s):  
Stefan H. Millson ◽  
Chrisostomos Prodromou ◽  
Peter W. Piper
Keyword(s):  
Drug Targets ◽  
Human Cancer ◽  
Cancer Drug ◽  
Inhibitor Resistance

scholarly journals Cellular Fitness Phenotypes of Cancer Target Genes from Oncobiology to Cancer Therapeutics

Cells ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 433
Author(s):  
Bijesh George ◽  
P. Mukundan Pillai ◽  
Aswathy Mary Paul ◽  
Revikumar Amjesh ◽  
Kim Leitzel ◽  
...  
Keyword(s):  
Drug Targets ◽  
Target Genes ◽  
Human Cancer ◽  
Cancer Therapeutics ◽  
Survival Duration ◽  
Cancer Drug ◽  
Targeted Therapeutics ◽  
Cellular Targets ◽  
Human Cancer Cells ◽  
Cancer Types

To define the growing significance of cellular targets and/or effectors of cancer drugs, we examined the fitness dependency of cellular targets and effectors of cancer drug targets across human cancer cells from 19 cancer types. We observed that the deletion of 35 out of 47 cellular effectors and/or targets of oncology drugs did not result in the expected loss of cell fitness in appropriate cancer types for which drugs targeting or utilizing these molecules for their actions were approved. Additionally, our analysis recognized 43 cellular molecules as fitness genes in several cancer types in which these drugs were not approved, and thus, providing clues for repurposing certain approved oncology drugs in such cancer types. For example, we found a widespread upregulation and fitness dependency of several components of the mevalonate and purine biosynthesis pathways (currently targeted by bisphosphonates, statins, and pemetrexed in certain cancers) and an association between the overexpression of these molecules and reduction in the overall survival duration of patients with breast and other hard-to-treat cancers, for which such drugs are not approved. In brief, the present analysis raised cautions about off-target and undesirable effects of certain oncology drugs in a subset of cancers where the intended cellular effectors of drug might not be good fitness genes and that this study offers a potential rationale for repurposing certain approved oncology drugs for targeted therapeutics in additional cancer types.

scholarly journals Cellular Fitness Phenotypes of Cancer Target Genes in Cancer Therapeutics

2019 ◽  
Author(s):  
Bijesh George ◽  
P. Mukundan Pillai ◽  
Aswathy Mary Paul ◽  
Kim Leitzel ◽  
Suhail M. Ali ◽  
...  
Keyword(s):  
Drug Targets ◽  
Target Genes ◽  
Human Cancer ◽  
Cancer Therapeutics ◽  
Survival Duration ◽  
Cancer Drug ◽  
Cellular Targets ◽  
Human Cancer Cells ◽  
Cancer Types ◽  
Approved Drugs

AbstractTo define the growing significance of cellular targets of targeted cancer drugs, we examined the fitness dependency of cancer drug targets across human cancer cells in a CRISPR-Cas9 fitness screening dataset wherein cellular genes were selectively knocked out before assaying for their fitness dependency in cancer cell lines representing 19 cancer types. We observed that the deletion of 35 out of 47 fitness targets of oncology drugs did not result in the expected loss of cell fitness in appropriate cancer types for which drugs targeting these molecules were approved. This raised the possibility of undesirable off-target effects of these drugs in such cancers. Additionally, our analysis recognized 43 drug targets which were fitness genes observed in several cancer types as candidate targets for repurposing approved oncology drugs in cancer types in which these drugs were not approved. For example, we found the widespread upregulation and fitness dependency of the components of the mevalonate and purine biosynthesis pathways (currently targeted by bisphosphonates, statins, and pemetrexed in certain cancers) and an association between the overexpression of these targets and reduction in the overall survival duration of patients with breast and other hard-to-treat cancers, for which these drugs are not approved. In brief, the present analysis raised cautions about off-target and undesirable effects of certain oncology drugs in a subset of cancers where the intended drug targets are not fitness genes. The study also offers a rationale for repurposing approved oncology drugs for cancer types that have significant fitness dependency on cellular targets of such approved drugs.

New cancer drug targets identified in adrenocortical carcinoma through gene expression profiling

2018 ◽  
Author(s):  
Raimunde Liang ◽  
Isabel Weigand ◽  
Barbara Altieri ◽  
Stefan Kircher ◽  
Sonja Steinhauer ◽  
...  
Keyword(s):  
Gene Expression ◽  
Gene Expression Profiling ◽  
Adrenocortical Carcinoma ◽  
Expression Profiling ◽  
Drug Targets ◽  
Cancer Drug

scholarly journals Validating cancer drug targets through chemical genetics

2010 ◽  
Vol 1806 (2) ◽  
pp. 251-257
Author(s):  
Mark E. Burkard ◽  
Prasad V. Jallepalli
Keyword(s):  
Drug Targets ◽  
Chemical Genetics ◽  
Cancer Drug

Synthesis, Spectral, Bio Assay, Chromatographic - Studying of New Imidazole Reagents Via Three Components Reaction

2021 ◽  
Vol 19 (7) ◽  
pp. 115-122
Author(s):  
Mohammed Nawfal Abdul Maged Alkhafaji ◽  
Hutham Abd Ali Abd Al Hussain ◽  
Dr. Nagham Mahmood Aljamali
Keyword(s):  
Nervous System ◽  
Drug Targets ◽  
Biological Activities ◽  
Drug Carrier ◽  
Chemical Properties ◽  
Cancer Drug ◽  
Condensation Process ◽  
Chromatographic Study ◽  
The Central Nervous System ◽  
Physical And Chemical

Imidazoles are part of the theophylline Reagent, found in tea leaves and coffee beans, which stimulates the central nervous system. It is found in the anti-cancer drug mercaptopurine, which fights leukemia by interfering with DNA systems. A number of prepared imidazoles, including clotrimazole, are selective inhibitors of nitric oxide synthase, which makes them interesting drug targets in inflammation, respiratory diseases and tumors of the nervous system. Other biological activities of the drug carrier imidazole relate to deregulation of the intracellular fluxes of (Ca and K) ions. Novel imidazole –heterocyclic reagents were created via cyclization process then condensation process., followed by investigation of all created new reagents via a number of spectral performances (FT.IR, H.NMR)–spectrophotometric, other physical and chemical properties, and chromatographic study with microbial studying for all new created imidazole reagents.

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