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 ◽  
...  

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.

2018 ◽  
Vol 150 ◽  
pp. 525-545 ◽  
Author(s):  
André Campaniço ◽  
Rui Moreira ◽  
Francisca Lopes

MedChemComm ◽  
2012 ◽  
Vol 3 (2) ◽  
pp. 162-166 ◽  
Author(s):  
Nessa Carey

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.


2006 ◽  
Vol 34 (2) ◽  
pp. 313-316 ◽  
Author(s):  
G.P. Belfield ◽  
S.J. Delaney

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.


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

2021 ◽  
Vol 7 (1) ◽  
Author(s):  
Ramalingam Peraman ◽  
Sathish Kumar Sure ◽  
V. N. Azger Dusthackeer ◽  
Naresh Babu Chilamakuru ◽  
Padmanabha Reddy Yiragamreddy ◽  
...  

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.


2017 ◽  
Vol 39 (4) ◽  

AbstractIUPAC and Gedeon Richter, Plc. are pleased to announce the 2018 IUPAC-Richter Prize in Medicinal Chemistry. The prize was established in 2006 by a generous gift from the Chemical Works of Gedeon Richter, Plc. (Budapest, Hungary) to acknowledge the key role that medicinal chemistry plays toward improving human health. The prize—USD 10 000—is to be awarded to an internationally recognized scientist, preferably a medicinal chemist, whose activities or published accounts have made an outstanding contribution to the practice of medicinal chemistry or to an outstanding example of new drug discovery.


2016 ◽  
Vol 38 (1) ◽  

IUPAC and Gedeon Richter, Plc. are pleased to announce the 2016 IUPAC-Richter Prize in Medicinal Chemistry. The Prize was established in 2006 by a generous gift from the Chemical Works of Gedeon Richter, Plc. (Budapest, Hungary) to acknowledge the key role that medicinal chemistry plays in improving human health. The prize—USD 10000—is awarded to an internationally recognized scientist, preferably a medicinal chemist, whose activities or published accounts have made an outstanding contribution to the practice of medicinal chemistry, or to an outstanding example of new drug discovery. Previous IUPAC-Richter Prizes were awarded to Malcolm F.G. Stevens in 2006, Jan Heeres in 2008, Arun K. Ghosh in 2010, Stephen Hanessian in 2012, and Helmut Buschmann in 2014.


2019 ◽  
Vol 18 (31) ◽  
pp. 2681-2701
Author(s):  
Meghna Manjunath ◽  
Sinosh Skariyachan

Cryptococcosis is one of the major invasive fungal infections distributed worldwide with high mortality rate. C. neoformans and C. gattii are the major organisms that cause various types of infections. Anti-fungal resistances exhibited by the mentioned species of Cryptococcus threaten their effective prevention and treatment. There is limited information available on human to human transmission of the pathogen and virulent factors that are responsible for Cryptococcus mediated infections. Hence, there is high scope for understanding the mechanism, probable drug targets and scope of developing natural therapeutic agents that possess high relevance to pharmaceutical biotechnology and medicinal chemistry. The proposed review illustrates the role of computer-aided virtual screening for the screening of probable drug targets and identification of natural lead candidates as therapeutic remedies. The review initially focuses on the current perspectives on cryptococcosis, major metabolic pathways responsible for the pathogenesis, conventional therapies and associated drug resistance, challenges and scope of structure-based drug discovery. The review further illustrates various approaches for the prediction of unknown drug targets, molecular modeling works, screening of natural compounds by computational virtual screening with ideal drug likeliness and pharmacokinetic features, application of molecular docking studies and simulation. Thus, the present review probably provides AN insight into the role of medicinal chemistry and computational drug discovery to combat Cryptococcus infections and thereby open a new paradigm for the development of novel natural therapeutic against various drug targets for cryptococcal infections.


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