Epigenetics—an emerging and highly promising source of new drug targets

MedChemComm ◽  
2012 ◽  
Vol 3 (2) ◽  
pp. 162-166 ◽  
Author(s):  
Nessa Carey
Keyword(s):  
Gene Expression ◽  
Drug Discovery ◽  
Drug Targets ◽  
Epigenetic Modifications ◽  
Regulatory Process ◽  
Human Diseases ◽  
Histone Proteins ◽  
New Drug ◽  
Promising Source

Epigenetic modifications to DNA and its associated histone proteins are major influences on gene expression. This regulatory process is disrupted in cancer and a range of chronic human diseases, and provides attractive new intervention points and targets for drug discovery.

Drug discovery in tuberculosis. New drug targets and antimycobacterial agents

2018 ◽  
Vol 150 ◽  
pp. 525-545 ◽  
Author(s):  
André Campaniço ◽  
Rui Moreira ◽  
Francisca Lopes
Keyword(s):  
Drug Discovery ◽  
Drug Targets ◽  
New Drug ◽  
Antimycobacterial Agents

The impact of molecular biology on drug discovery

2006 ◽  
Vol 34 (2) ◽  
pp. 313-316 ◽  
Author(s):  
G.P. Belfield ◽  
S.J. Delaney
Keyword(s):  
Drug Discovery ◽  
Molecular Biology ◽  
Clinical Efficacy ◽  
Drug Targets ◽  
Safety Data ◽  
Vital Role ◽  
Drug Discovery And Development ◽  
New Drug ◽  
Whole Process ◽  
The Impact

The discipline of molecular biology has become increasingly important in recent times for the process of drug discovery. We describe the impact of molecular biology across the whole process of drug discovery and development, including (i) the identification and validation of new drug targets, (ii) the development of molecular screens to find new candidate drugs, and (iii) the generation of safety data and competences leading to enhanced clinical efficacy. We also speculate on emerging developments in drug discovery where it seems likely that molecular biology will play an even more vital role in the generation of future therapies.

scholarly journals Role of Tet2 in Regulating Adaptive and Innate Immunity

2021 ◽  
Vol 9 ◽  
Author(s):  
Jiaqi Li ◽  
Lifang Li ◽  
Xiaoxiao Sun ◽  
Tuo Deng ◽  
Gan Huang ◽  
...  
Keyword(s):  
Gene Expression ◽  
Drug Targets ◽  
Gene Expression Regulation ◽  
Epigenetic Modification ◽  
Epigenetic Modifications ◽  
Cellular Factors ◽  
Tet Enzymes ◽  
And Function ◽  
Opposing Effects ◽  
Tet Protein

Accumulated evidence indicates that epigenetic modifications play central roles in gene expression regulation and participate in developing many autoimmune and autoinflammatory diseases. Mechanistically, epigenetic modifications act as a bridge between environmental and cellular factors and susceptibility genes. DNA methylation is a critical epigenetic modification that is regulated by ten-eleven translocation (TET) enzymes. Accumulating evidence has revealed that TET family proteins function as gene regulators and antitumor drug targets mainly because of their ability to oxidize 5-methylcytosine (5mC) to 5-hydroxymethylcytosine (5hmC). Recently, the effect of Tet2, an essential TET protein, on the development of autoimmune diseases has been explored. In this review, we summarize the current understanding of Tet2 in immune response regulation, clarify the mechanisms of Tet2 in B and T cell differentiation and function, and discuss the opposing effects of Tet2 on inflammatory gene expression in the immune system to provide new potential therapeutic targets for related diseases.

scholarly journals Current advances of carbene-mediated photoaffinity labeling in medicinal chemistry

RSC Advances ◽  
2018 ◽  
Vol 8 (51) ◽  
pp. 29428-29454 ◽  
Author(s):  
Sha-Sha Ge ◽  
Biao Chen ◽  
Yuan-Yuan Wu ◽  
Qing-Su Long ◽  
Yong-Liang Zhao ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Uv Irradiation ◽  
Binding Sites ◽  
Drug Targets ◽  
Medicinal Chemistry ◽  
Photoaffinity Labeling ◽  
Chemical Probe ◽  
New Drug ◽  
Considerable Promise

Photoaffinity labeling (PAL) in combination with a chemical probe to covalently bind its target upon UV irradiation has demonstrated considerable promise in drug discovery for identifying new drug targets and binding sites.

Drug Discovery: Methods for Identifying New Drug Targets

2005 ◽  
Vol 2 (1) ◽  
pp. 35-46
Author(s):  
Murty V. Chengalvala ◽  
Joshua E. Cottom ◽  
Linda K. Shanno ◽  
Gregory S. Kopf
Keyword(s):  
Drug Discovery ◽  
Drug Targets ◽  
New Drug

scholarly journals Insights on recent approaches in drug discovery strategies and untapped drug targets against drug resistance

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Ramalingam Peraman ◽  
Sathish Kumar Sure ◽  
V. N. Azger Dusthackeer ◽  
Naresh Babu Chilamakuru ◽  
Padmanabha Reddy Yiragamreddy ◽  
...  
Keyword(s):  
Drug Resistance ◽  
Drug Discovery ◽  
Drug Targets ◽  
Genetic Research ◽  
Integrated Approach ◽  
Main Body ◽  
Chemical Structures ◽  
New Drug ◽  
Discovery Research ◽  
Drug Discovery Research

Abstract Background Despite the various strategies undertaken in the clinical practice, the mortality rate due to antibiotic-resistant microbes has been markedly increasing worldwide. In addition to multidrug-resistant (MDR) microbes, the “ESKAPE” bacteria are also emerging. Of course, the infection caused by ESKAPE cannot be treated even with lethal doses of antibiotics. Now, the drug resistance is also more prevalent in antiviral, anticancer, antimalarial and antifungal chemotherapies. Main body To date, in the literature, the quantum of research reported on the discovery strategies for new antibiotics is remarkable but the milestone is still far away. Considering the need of the updated strategies and drug discovery approaches in the area of drug resistance among researchers, in this communication, we consolidated the insights pertaining to new drug development against drug-resistant microbes. It includes drug discovery void, gene paradox, transposon mutagenesis, vitamin biosynthesis inhibition, use of non-conventional media, host model, target through quorum sensing, genomic-chemical network, synthetic viability to targets, chemical versus biological space, combinational approach, photosensitization, antimicrobial peptides and transcriptome profiling. Furthermore, we optimally briefed about antievolution drugs, nanotheranostics and antimicrobial adjuvants and then followed by twelve selected new feasible drug targets for new drug design against drug resistance. Finally, we have also tabulated the chemical structures of potent molecules against antimicrobial resistance. Conclusion It is highly recommended to execute the anti-drug resistance research as integrated approach where both molecular and genetic research needs to be as integrative objective of drug discovery. This is time to accelerate new drug discovery research with advanced genetic approaches instead of conventional blind screening.

scholarly journals Evaluation of Gene Expression and Phenotypic Profiling Data as Quantitative Descriptors for Predicting Drug Targets and Mechanisms of Action

2019 ◽  
Author(s):  
Maris Lapins ◽  
Ola Spjuth
Keyword(s):  
Gene Expression ◽  
Drug Discovery ◽  
Drug Targets ◽  
Chemical Structure ◽  
Predictive Accuracy ◽  
Mechanisms Of Action ◽  
In Vitro Assays ◽  
Using Data ◽  
Drug Leads

AbstractProfiling drug leads by means of in silico and in vitro assays as well as omics is widely used in drug discovery for safety and efficacy predictions. In this study, we evaluate the performance of machine learning models trained on data from gene expression and phenotypic profiling assays, with models trained on chemical structure descriptors, for prediction of various drug mechanisms of action and target proteins. Models for several hundred mechanisms of actions and targets were trained using data on 1484 compounds characterized in both gene expression using L1000 profiles, and phenotypic profiling with cell painting assay. The results indicate that the accuracy of the three profiling technologies varies for different endpoints, and indicate a clear potential synergistic effect if these methods are combined. We also study the effect of predictive accuracy of data from different cell lines for L1000 profiles, showing that the choice of cell line has a non-negligible effect on the predictive accuracy. The results strengthen the idea of integrated approaches for predicting drug targets and mechanisms of action in preclinical drug discovery.

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