Glutamic acid and its derivatives: candidates for rational design of anticancer drugs

2013 ◽  
Vol 5 (8) ◽  
pp. 961-978 ◽  
Author(s):  
Imran Ali ◽  
Waseem A Wani ◽  
Ashanul Haque ◽  
Kishwar Saleem
Keyword(s):  
Glutamic Acid ◽  
Anticancer Drugs ◽  
Rational Design

scholarly journals How Computational Chemistry and Drug Delivery Techniques Can Support the Development of New Anticancer Drugs

Molecules ◽  
2020 ◽  
Vol 25 (7) ◽  
pp. 1756 ◽  
Author(s):  
Mariangela Garofalo ◽  
Giovanni Grazioso ◽  
Andrea Cavalli ◽  
Jacopo Sgrignani
Keyword(s):  
Drug Delivery ◽  
Anticancer Drugs ◽  
Rational Design ◽  
Significant Contribution ◽  
Research Experience ◽  
Computer Aided Drug Design ◽  
Target Drug Delivery ◽  
Research Fields ◽  
Target Drug ◽  
New Anticancer Drugs

The early and late development of new anticancer drugs, small molecules or peptides can be slowed down by some issues such as poor selectivity for the target or poor ADME properties. Computer-aided drug design (CADD) and target drug delivery (TDD) techniques, although apparently far from each other, are two research fields that can give a significant contribution to overcome these problems. Their combination may provide mechanistic understanding resulting in a synergy that makes possible the rational design of novel anticancer based therapies. Herein, we aim to discuss selected applications, some also from our research experience, in the fields of anticancer small organic drugs and peptides.

scholarly journals MN4-based G4-Ligands as Potential Antitumor Agents: A Review

2021 ◽  
Vol 12 (3) ◽  
pp. 3977-3988
Keyword(s):  
Metal Complexes ◽  
Anticancer Drugs ◽  
Anticancer Agents ◽  
Genomic Dna ◽  
Rational Design ◽  
Structural Engineering ◽  
Antitumor Agents ◽  
Medical Field ◽  
G Quadruplex ◽  
Potential Antitumor

Cisplatin-based metal drugs have been widely used clinically as anticancer agents. However, these drugs also harm ordinary tissues because cisplatin kills cancer cells by attacking genomic DNA. Therefore, it has been shown that cisplatin-based metal drugs have some serious side effects that cannot be avoided. In order to replace the target site of genomic DNA, G-quadruplex nucleic acid is considered to be an alternative and attractive target for anticancer agents because G-quadruplex always folds into a parallel topology and is, therefore, more important than DNA. This review discussed the recent advancements in the rational design and the development of metal complexes containing anticancer drugs to interact and stabilize or cleave the G4 structure selectively. Further, we also highlighted the G4-interacting transition metal complexes, interacting modes, and their potentials to serve as anticancer drugs in the medical field. The significance of this survey lies in designing the metallodrugs from the most fundamental characteristic of electronic structural engineering to an increasingly reasonable dimension of bio-science.

Rational design and synthesis of potent and long-lasting glutamic acid-based dipeptidyl peptidase IV inhibitors

2009 ◽  
Vol 19 (7) ◽  
pp. 1908-1912 ◽  
Author(s):  
Ting-Yueh Tsai ◽  
Tsu Hsu ◽  
Chiung-Tong Chen ◽  
Jai-Hong Cheng ◽  
Mei-Chun Chiou ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Rational Design ◽  
Dipeptidyl Peptidase ◽  
Dipeptidyl Peptidase Iv ◽  
Design And Synthesis ◽  
Dipeptidyl Peptidase Iv Inhibitors

The rational design of NAMI-A-loaded mesoporous silica nanoparticles as antiangiogenic nanosystems

2015 ◽  
Vol 3 (30) ◽  
pp. 6338-6346 ◽  
Author(s):  
Hao Hu ◽  
Yuanyuan You ◽  
Lizhen He ◽  
Tianfeng Chen
Keyword(s):  
Mesoporous Silica ◽  
Silica Nanoparticles ◽  
Anticancer Drugs ◽  
Rational Design ◽  
Mesoporous Silica Nanoparticles ◽  
Antiangiogenic Activity

Herein we demonstrate the use of RGD-modified MSNs as a vehicle for anticancer drugs to achieve enhanced antiangiogenic activity.

scholarly journals Rational design of novel, fluorescent, tagged glutamic acid dendrimers with different terminal groups and in silico analysis of their properties

2017 ◽  
Vol Volume 12 ◽  
pp. 7053-7073 ◽  
Author(s):  
Nuno Martinho ◽  
Liana Silva ◽  
Helena Florindo ◽  
Steve Brocchini ◽  
Mire Zloh ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
In Silico ◽  
Rational Design ◽  
In Silico Analysis ◽  
Silico Analysis

scholarly journals Unravelling the Allosteric Targeting of PHGDH at the ACT-Binding Domain with a Photoactivatable Diazirine Probe and Mass Spectrometry Experiments

Molecules ◽  
2021 ◽  
Vol 26 (2) ◽  
pp. 477
Author(s):  
Quentin Spillier ◽  
Séverine Ravez ◽  
Simon Dochain ◽  
Didier Vertommen ◽  
Léopold Thabault ◽  
...  
Keyword(s):  
Mass Spectrometry ◽  
Anticancer Drugs ◽  
Mechanism Of Action ◽  
Rational Design ◽  
Biosynthetic Pathway ◽  
Allosteric Site ◽  
Site Of Action ◽  
Phosphoglycerate Dehydrogenase ◽  
New Anticancer Drugs

The serine biosynthetic pathway is a key element contributing to tumor proliferation. In recent years, targeting of phosphoglycerate dehydrogenase (PHGDH), the first enzyme of this pathway, intensified and revealed to be a promising strategy to develop new anticancer drugs. Among attractive PHGDH inhibitors are the α-ketothioamides. In previous work, we have demonstrated their efficacy in the inhibition of PHGDH in vitro and in cellulo. However, the precise site of action of this series, which would help the rational design of new inhibitors, remained undefined. In the present study, the detailed mechanism-of-action of a representative α-ketothioamide inhibitor is reported using several complementary experimental techniques. Strikingly, our work led to the identification of an allosteric site on PHGDH that can be targeted for drug development. Using mass spectrometry experiments and an original α-ketothioamide diazirine-based photoaffinity probe, we identified the 523Q-533F sequence on the ACT regulatory domain of PHGDH as the binding site of α-ketothioamides. Mutagenesis experiments further documented the specificity of our compound at this allosteric site. Our results thus pave the way for the development of new anticancer drugs using a completely novel mechanism-of-action.

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