: Stereochemistry has evinced the importance of many chiral drugs in aspects of drug designing and development. A literature review was conducted for several chiral drugs involving pharmacokinetic and pharmacodynamic parameters of their enantiomers along with their uses in certain diseased conditions. This article generally includes the pharmacological profile review of some chiral drugs and the aspects by which the single enantiomer can be of significant importance as compared to the racemic mixture of the drug. This can be achieved either by assuaging the side effects or toxic effects; or by the potentiated activity of the single enantiomer. Resolution deals with the separation of racemic compounds which shows up the credibility to obtain the desired enantiomeric properties. As isomers vary in their pharmacokinetic and pharmacodynamic profiles, chiral drugs have showcased considerable importance in the drug development process. Both enantiomers have a different pharmacological profile in the treatment of a disease, which differentiates them from drug racemates.
The G6PD deficiency increases hemoglobin vulnerability to oxidative damage, leading to hemoglobin instability and precipitation of Heinz bodies. [1] G6PD deficiency is the most common red cell enzyme abnormality associated with hemolysis. It is also known to be associated with neonatal jaundice, kernicterus, and even death. The marked elevation of bilirubin levels that sometimes occurs in the neonatal period raises the risk of kernicterus. Neonatal hyperbilirubinemia often arises in association with Gilbert's syndrome. [2,3] It affects over 400 million people worldwide. [4] G6PD deficiency occurs with increased frequency throughout Africa, Asia, the Mediterranean, and the Middle East. In the United States, black males are most commonly affected, with a prevalence of approximately 10%. [5] The global distribution and health burden of G6PD deficiency has Background: Glucose-6-phosphate dehydrogenase (G6PD) is an enzyme essential for basic cellular functions, including protection of red cell proteins from oxidative damage. G6PD deficiency is the most common red cell enzyme abnormality associated with hemolysis as well as with neonatal jaundice, kernicterus, and even death. It plays a protective role against malaria. It is a genetically inherited sex-linked abnormality. Objectives: To determine the age, sex, and different community-wise incidence of G6PD deficiency in neonatal subjects having neonatal hyperbilirubinemia.
: World Health Organization categorized breast cancer as one of the leading cancer types in females worldwide, and its treatment remains challenging. Accumulated evidence suggested the role of estrogen and its metabolites in pre- and post-menopausal women. Upregulation of estrogen-dependent aromatase is significantly involved in the pathogenesis of breast cancer. Several aromatase inhibitors, such as exemestane, formestane, and letrozole, are being used clinically, owing to their estrogen suppression role. Apart from these drugs, several other molecules, such as natural and synthetic flavonoids, have been reported widely for a similar biological activity. However, some reasonable modifications are required for these structures to achieve desired efficacy and to alleviate toxicity. Designing a novel aromatase inhibitor will be possible if we can establish a rational correlation between the chemistry and biological features of the existing molecules. The benzopyranone-ring system, present in the flavonoid molecules, has been reported as a pharmacophore due to its inhibitory activity on aromatase, which helps repress breast cancer progression. This essential feature has been utilized to modify several natural flavonoids into 5 and 7 hydroxy/methoxy flavone, 4-imidazolyl/triazolyl flavone, 5,4’- diamino flavone, 7,8- benzo-4-imidazolyl flavone, α-naphthoflavone, and 2-azole/thiazolyl isoflavone derivatives. These scaffolds have been considered in this review for meticulous study in aspects of the structure-activity relationship for aromatase inhibitory activity, and it would likely pave the way for designing a potential lead candidate in the future.
Objective: Recent scientific advances have expanded insight into the immune system and its response to malignant cells. In the past few years, immunotherapy has attained a hallmark for cancer treatment, especially for patients suffering from the advanced-stage disease. Modulating the immune system by blocking various immune checkpoint receptor proteins through monoclonal antibodies has improved cancer patients' survival rates. Methods: The scope of this review spans from 1985 to the present day. Many journals, books, and theses have been used to gather data, as well as Internet-based information such as Wiley, PubMed, Google Scholar, ScienceDirect, EBSCO, SpringerLink, and Online electronic journals. Key findings: Current review elaborates on the potential inhibitory and stimulatory checkpoint pathways which are emerged and have been tested in various preclinical models, clinical trials, and practices. Twenty-odd such significant checkpoints are identified and discussed in the present work. Conclusion: A large number of ongoing studies reveal that combination therapies that target more than one signaling pathway may become effective in order to maximize efficacy and minimize toxicity. Moreover, these immunotherapy targets can be a part of integrated therapeutic strategies in addition to classical approaches. It may become a paradigm shift as a promising strategy for cancer treatment.
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