Abstract C159: Identification of potential cancer drug targets using HT RNAi screening with pooled shRNA libraries.

Author(s):  
Donato Tedesco ◽  
Kyle Bonneau ◽  
Mikhail Makhanov ◽  
Costas G. Frangou ◽  
Alex Chenchik
2015 ◽  
Vol 9 (1) ◽  
pp. 141-149
Author(s):  
Amitha Joy ◽  
S. Balaji

Inositol hexakisphosphate is known to be the phosphorous reserve in plants particularly in the seeds. Though it has been known for its antinutrient properties for many years, recent research shed light to reveal it as a novel anticancer agent. Hence the present study investigates the drug-likeness of phytic acid and its analogues through bioinformatics methods. Two potential cancer drug targets such as mitogen activated kinase and inositol 1,4,5-triphosphate receptor are included in the study. Out of 50 selected analogues of phytic acid, 42 structures interact well with the chosen drug targets. The best interacting structures are 1-diphosinositol pentakisphosphate and 2,3,4,5,6-pentaphosphonooxycyclohexyl dihydrogen phosphate. For both of these structures, the negative binding energy obtained was -49.5 KJ/mol; this affirms the stability of the complex. ADME properties are also predicted to assess the drug-like properties of the compounds. The structure activity relationship model is generated for 12 compounds with experimental IC50 values.


2013 ◽  
Vol 12 (6) ◽  
pp. 2354-2364 ◽  
Author(s):  
Jingqi Chen ◽  
Ming Ma ◽  
Ning Shen ◽  
Jianzhong Jeff Xi ◽  
Weidong Tian

2018 ◽  
Author(s):  
Raimunde Liang ◽  
Isabel Weigand ◽  
Barbara Altieri ◽  
Stefan Kircher ◽  
Sonja Steinhauer ◽  
...  

Cells ◽  
2021 ◽  
Vol 10 (2) ◽  
pp. 433
Author(s):  
Bijesh George ◽  
P. Mukundan Pillai ◽  
Aswathy Mary Paul ◽  
Revikumar Amjesh ◽  
Kim Leitzel ◽  
...  

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.


2010 ◽  
Vol 1806 (2) ◽  
pp. 251-257
Author(s):  
Mark E. Burkard ◽  
Prasad V. Jallepalli

2020 ◽  
Vol 66 (3) ◽  
pp. 56-65
Author(s):  
Filip Przerwa ◽  
Arnold Kukowka ◽  
Izabela Uzar

Abstract Ballota nigra, also known as black horehound is a common medical herb used in folk medicine around the world. First reported mentions of its medical properties and use goes as far as the 13th century. The use of black horehound depends on regions and countries. It is used mostly to treat e.g. mild sleep disorders, nervousness, upset stomach, wound healing. It can be used as an anti-inflammatory, antibacterial, antiprotozoal, antifungal drug. Moreover, it has been reported as a potential cancer drug. This extensive usage is particularly interesting for us. The aim of this review is to present available data on B. nigra pharmacological effects and known traditional uses gathered from a wide range of scientific articles published in 1997–2020.


2021 ◽  
Vol 19 (7) ◽  
pp. 115-122
Author(s):  
Mohammed Nawfal Abdul Maged Alkhafaji ◽  
Hutham Abd Ali Abd Al Hussain ◽  
Dr. Nagham Mahmood Aljamali

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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