poster session 1: new drug targets, drug design and drug discovery

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.

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The impact of molecular biology on drug discovery

Biochemical Society Transactions ◽

10.1042/bst0340313 ◽

2006 ◽

Vol 34 (2) ◽

pp. 313-316 ◽

Cited By ~ 4

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.

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Advances toward structure-based drug discovery for inflammasome targets

Journal of Experimental Medicine ◽

10.1084/jem.20211147 ◽

2021 ◽

Vol 219 (1) ◽

Author(s):

Li Wang ◽

Michael A. Crackower ◽

Hao Wu

Keyword(s):

Drug Discovery ◽

High Resolution ◽

Drug Design ◽

Structural Biology ◽

Drug Targets ◽

Unmet Need ◽

Structure Based Drug Design ◽

Important Family ◽

Recent Advances

Inflammasome proteins play an important role in many diseases of high unmet need, making them attractive drug targets. However, drug discovery for inflammasome proteins has been challenging in part due to the difficulty in solving high-resolution structures using cryo-EM or crystallography. Recent advances in the structural biology of NLRP3 and NLRP1 have provided the first set of data that proves a promise for structure-based drug design for this important family of targets.

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Drugging Fuzzy Complexes in Transcription

Frontiers in Molecular Biosciences ◽

10.3389/fmolb.2021.795743 ◽

2021 ◽

Vol 8 ◽

Author(s):

Bonnie G. Su ◽

Matthew J. Henley

Keyword(s):

Transcription Factor ◽

Transcription Factors ◽

Drug Discovery ◽

Drug Design ◽

Drug Targets ◽

Chemical Biology ◽

Intrinsic Disorder ◽

High Degree ◽

Screening Approaches

Transcription factors (TFs) are one of the most promising but underutilized classes of drug targets. The high degree of intrinsic disorder in both the structure and the interactions (i.e., “fuzziness”) of TFs is one of the most important challenges to be addressed in this context. Here, we discuss the impacts of fuzziness on transcription factor drug discovery, describing how disorder poses fundamental problems to the typical drug design, and screening approaches used for other classes of proteins such as receptors or enzymes. We then speculate on ways modern biophysical and chemical biology approaches could synergize to overcome many of these challenges by directly addressing the challenges imposed by TF disorder and fuzziness.

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Zika virus drug targets: a missing link in drug design and discovery – a route map to fill the gap

RSC Advances ◽

10.1039/c6ra12142j ◽

2016 ◽

Vol 6 (73) ◽

pp. 68719-68731 ◽

Cited By ~ 18

Author(s):

Pritika Ramharack ◽

Mahmoud E. S. Soliman

Keyword(s):

Drug Discovery ◽

Drug Design ◽

Viral Replication ◽

Zika Virus ◽

In Silico ◽

Drug Targets ◽

Missing Link ◽

Potential Inhibitors

This review depicts anin silicoroute map for ZIKV drug discovery, thus revealing novel potential inhibitors of viral replication.

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Poster session 2: New drug targets

Annals of Oncology ◽

10.1093/annonc/mdi611 ◽

2005 ◽

Vol 16 ◽

pp. iii35-iii36

Keyword(s):

Drug Targets ◽

Poster Session ◽

New Drug

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Current advances of carbene-mediated photoaffinity labeling in medicinal chemistry

RSC Advances ◽

10.1039/c8ra03538e ◽

2018 ◽

Vol 8 (51) ◽

pp. 29428-29454 ◽

Cited By ~ 15

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.

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Drug Discovery: Methods for Identifying New Drug Targets

Drug Design Reviews - Online ◽

10.2174/1567269053390301 ◽

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

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

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-021-00196-5 ◽

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.

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