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Raj Kumar
Gyeongsang National University
12Publications
5H-index
61Citations
Publications 12
Newest
#1Shailima Rampogu (Gyeongsang National University)H-Index: 7
#2Ayoung Baek (Gyeongsang National University)H-Index: 7
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 11 authors...
Aromatase inhibitors with an \mathrm{IC}_{50}IC 50 value ranging from 1.4 to 49.7 µM are known to act as antiepileptic drugs besides being potential breast cancer inhibitors. The aim of the present study is to identify novel antiepileptic aromatase inhibitors with higher activity exploiting the ligand-based pharmacophore approach utilizing the experimentally known inhibitors. The resultant Hypo1 consists of four features and was further validated by using three different strategies. Hypo1 was...
Source
#1Amir ZebH-Index: 5
#2Donghwan KimH-Index: 1
Last.Keun Woo LeeH-Index: 30
view all 12 authors...
Mechanistically, neurotoxic insults provoke Ca2+-mediated calpain activation, which cleaves the cytoplasmic region of membrane-embedded p35 and produces its truncated form p25. Upon physical interaction, cyclin-dependent kinase 5 (Cdk5) and p25 forms hyperactivated Cdk5/p25 complex and causes severe neuropathological aberrations including hyperphosphorylated tau-mediated neurofibrillary tangles formation, Alzheimer’s symptoms, and neuronal death. Therefore, the inhibition of Cdk5/p25 complex may...
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#1Raj Kumar (Gyeongsang National University)H-Index: 5
#2Saravanan Parameswaran (Gyeongsang National University)H-Index: 1
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 12 authors...
Abstract Prolyl oligopeptidase (POP) is a potential therapeutic target for treatment of several neurological disorders and α-synucleinopathies including Parkinson's disease. Most of the known POP inhibitors failed in the clinical trials due to poor pharmacokinetic properties and blood-brain impermeability. Therefore, a training set of 30 structurally diverse compounds with a wide range of inhibitory activity against POP was used to generate a quantitative pharmacophore model, Hypo 3, to identify...
1 CitationsSource
#1Shailima Rampogu (Gyeongsang National University)H-Index: 7
#2Chanin Park (Gyeongsang National University)H-Index: 8
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 14 authors...
Breast cancer (BC) is the leading cause of death among women worldwide devoid of effective treatment. It is therefore important to develop agents that can reverse, reduce, or slow the growth of BC. The use of natural products as chemopreventive agents provides enormous advantages. The aim of the current investigation is to determine the efficacy of the phytochemicals against BC along with the approved drugs to screen the most desirable and effective phytocompound. In the current study, 36 phytoc...
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#1Shailima Rampogu (Gyeongsang National University)H-Index: 7
#2Ayoung Baek (Gyeongsang National University)H-Index: 7
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 9 authors...
Background Antibiotic resistance is a defense mechanism, harbored by pathogens to survive under unfavorable conditions. Among several antibiotic resistant microbial consortium, Staphylococcus aureus is one of the most havoc microorganisms. Staphylococcus aureus encodes a unique enzyme 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase (SaHPPK), against which, none of existing antibiotics have been reported.
3 CitationsSource
#1Raj Kumar (Gyeongsang National University)H-Index: 5
#2Rohit Bavi (Gyeongsang National University)H-Index: 4
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 8 authors...
Prolyl oligopeptidase (POP) is a serine protease that is responsible for the maturation and degradation of short neuropeptides and peptide hormones. The inhibition of POP has been demonstrated in the treatment of α-synucleinopathies and several neurological conditions. Therefore, ligand-based and structure-based pharmacophore models were generated and validated in order to identify potent POP inhibitors. Pharmacophore-based and docking-based virtual screening of a drug-like database resulted in ...
7 CitationsSource
#1Rohit Bavi (Gyeongsang National University)H-Index: 4
#2Raj Kumar (Gyeongsang National University)H-Index: 5
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 7 authors...
AbstractHigh level of hematopoietic cell kinase (Hck) is associated with drug resistance in chronic myeloid leukemia. Additionally, Hck activity has also been connected with the pathogenesis of HIV-1 and chronic obstructive pulmonary disease. In this study, three-dimensional (3D) QSAR pharmacophore models were generated for Hck based on experimentally known inhibitors. A best pharmacophore model, Hypo1, was developed with high correlation coefficient (0.975), Low RMS deviation (0.60) and large c...
4 CitationsSource
#1Shailima Rampogu (Gyeongsang National University)H-Index: 7
#2Ayoung Baek (Gyeongsang National University)H-Index: 7
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 13 authors...
Progeria is a rare genetic disorder characterized by premature aging that eventually leads to death and is noticed globally. Despite alarming conditions, this disease lacks effective medications; however, the farnesyltransferase inhibitors (FTIs) are a hope in the dark. Therefore, the objective of the present article is to identify new compounds from the databases employing pharmacophore based virtual screening. Utilizing nine training set compounds along with lonafarnib, a common feature pharma...
9 CitationsSource
#1Guang Ping Cao (Gyeongsang National University)H-Index: 6
#2Sundarapandian Thangapandian (Gyeongsang National University)H-Index: 17
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 10 authors...
HDAC8 inhibitors have become an attractive treatment for cancer. This study aimed to facilitate the identification of potential chemical scaffolds for the selective inhibition of histone deacetylase 8 (HDAC8) using in silico approaches. Non-linear QSAR classification and regression models of HDAC8 inhibitors were developed with support vector machine. Mean impact value-based sequential forward feature selection and grid search strategy were used for molecular descriptor selection and parameter o...
4 CitationsSource
#1Rohit Bavi (Gyeongsang National University)H-Index: 4
#2Raj Kumar (Gyeongsang National University)H-Index: 5
Last.Keun Woo Lee (Gyeongsang National University)H-Index: 30
view all 10 authors...
Abstract Helicobacter pylori ( H. pylori ) persevere in the human stomach, an environment in which they encounter many DNA-damaging conditions, including gastric acidity. The pathogenicity of H. pylori is enhanced by its well-developed DNA repair mechanism, thought of as ‘machinery,’ such as nucleotide excision repair (NER). NER involves multi-enzymatic excinuclease proteins (UvrABC endonuclease), which repair damaged DNA in a sequential manner. UvrB is the central component in prokaryotic NER, ...
7 CitationsSource
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