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Article ; Online: Raltegravir

Kavya Ramkumar / Nouri Neamati

Core Evidence, Vol 2009, Iss default, Pp 131-

The evidence of its therapeutic value in HIV-1 infection

2009 Volume 147

Abstract: Kavya Ramkumar, Nouri NeamatiDepartment of Pharmacology and Pharmaceutical Sciences ...

Abstract	Kavya Ramkumar, Nouri NeamatiDepartment of Pharmacology and Pharmaceutical Sciences, School of Pharmacy, University of Southern California, Los Angeles, CA, USAIntroduction: The antiretroviral treatment paradigm for human immunodeficiency virus-1 (HIV-1) infection has undergone a significant change with the addition of a new class of therapeutic agents targeting HIV-1 integrase (IN). IN inhibitors prevent the integration of viral DNA into the human genome and terminate the viral life cycle. As the first member of this new class of anti-HIV drugs, raltegravir has shown promising results in the clinic. Aims: To review the emerging evidence for the use of the IN inhibitor raltegravir in the treatment of HIV-1 infection.Evidence review: Strong evidence shows that raltegravir is effective in reducing the viral load to less than 50 copies/mL and increasing CD4 cell count in treatment-experienced patients with triple-drug class-resistant HIV-1 infection. Substantial evidence also indicates that while raltegravir is able to achieve treatment response in patients with drug-resistant HIV-1, it is susceptible to development of resistance. Raltegravir should be used with at least one other active drug. In addition to its use in salvage therapy upon failure of first-line antiretroviral treatment, a raltegravir-based treatment regimen may also be effective as initial therapy. Substantial evidence also shows that raltegravir-based treatment regimen is well tolerated with minimal clinically severe adverse events and toxicities. Modeling studies suggest a cost-effectiveness of US$21,339 per quality-adjusted life year gained with raltegravir use, though further direct evidence on quality of life and cost-effectiveness is needed. Place in therapy: Raltegravir shows significant and sustained virologic and immunologic response in combination with other antiretrovirals in treatment-experienced HIV-1 infected patients who show evidence of viral replication or multidrug-resistant HIV-1 strains, without any significant tolerability issues.Keywords: raltegravir, isentress, MK-0518, integrase inhibitor, HIV-1, clinical evidence
Keywords	Medicine (General) ; R5-920 ; Medicine ; R ; DOAJ:Medicine (General) ; DOAJ:Health Sciences ; Therapeutics. Pharmacology ; RM1-950 ; DOAJ:Therapeutics
Subject code	616
Language	English
Publishing date	2009-07-01T00:00:00Z
Publisher	Dove Medical Press
Document type	Article ; Online
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Article ; Online: Triple blockade of Ido-1, PD-L1 and MEK as a potential therapeutic strategy in NSCLC

Journal of Translational Medicine, Vol 20, Iss 1, Pp 1-

2022 Volume 12

Abstract: Abstract Background Despite the recent progress in the treatment and outcome of Non Small Cell Lung Cancer (NSCLC), immunotherapy has still significant limitations reporting a significant proportion of patients not benefiting from therapy, even in ... ...

Abstract	Abstract Background Despite the recent progress in the treatment and outcome of Non Small Cell Lung Cancer (NSCLC), immunotherapy has still significant limitations reporting a significant proportion of patients not benefiting from therapy, even in patients with high PD-L1 expression. We have previously demonstrated that the combined inhibition of MEK and PD-L1 in NSCLC patients derived three dimensional cultures exerted significant synergistic effect in terms of immune-dependent cancer cell death. However, subsequent experiments analyzing the expression of Indoleamine 2,3-dioxygenase-1 (Ido-1) gene expression demonstrated that Ido-1 resulted unaffected by the MEK inhibition and even increased after the combined inhibition of MEK and PD-L1 thus representing a potential escape mechanism to this combination. Methods We analyzed transcriptomic profile of NSCLC lung adenocarcinoma cohort of TCGA (The Cancer Genome Atlas), stratifying tumors based on EMT (Epithelial mesenchymal Transition) score; in parallel, we investigated the activation of Ido-1 pathway and modulation of immune cytokines productions both in NSCLC cells lines, in peripheral blood mononuclear cells (PBMCs) and in ex-vivo NSCLC spheroids induced by triple inhibition with an anti-PD-L1 monoclonal antibody, the MEK inhibitor and the Ido-1 inhibitor. Results In NSCLC lung adenocarcinoma patient cohort (from TCGA) Ido-1 gene expression was significantly higher in samples classified as mesenchymal according EMT score. Similarly, on a selected panel of NSCLC cell lines higher expression of MEK and Ido-1 related genes was detected in cells with mesenchymal phenotype according EMT score, thus suggesting a potential correlation of co-activation of these two pathways in the context of EMT, with cancer cells sustaining an immune-suppressive microenvironment. While exerting an antitumor activity, the dual blockade of MEK and PD-L1 enhances the secretion of pro-inflammatory cytokines (IFNγ, TNFα, IL-12 and IL-6) and, consequently, the expression of new immune ...
Keywords	Ido-1 ; Checkpoint inhibitor ; Resistance ; EMT ; Medicine ; R
Subject code	570
Language	English
Publishing date	2022-11-01T00:00:00Z
Publisher	BMC
Document type	Article ; Online
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Article: Nitric oxide synthase regulation and diversity: implications in Parkinson's disease.

Kavya, Ramkumar / Saluja, Rohit / Singh, Sarika / Dikshit, Madhu

Nitric oxide : biology and chemistry

2006 Volume 15, Issue 4, Page(s) 280–294

Abstract: Nitric oxide (NO) is a janus faced chemical messenger, which, in the recent years, has been the focus of neurobiologists for its involvement in neurodegenerative disorders in particular, Parkinson's disease (PD). Nitric oxide synthase, the key enzyme ... ...

Abstract	Nitric oxide (NO) is a janus faced chemical messenger, which, in the recent years, has been the focus of neurobiologists for its involvement in neurodegenerative disorders in particular, Parkinson's disease (PD). Nitric oxide synthase, the key enzyme involved in NO production exists in three known isoforms. The neuronal and inducible isoforms have been implicated in the pathogenesis of PD. These enzymes are subject to complex expressional and functional regulation involving mRNA diversity, phosphorylation and protein interaction. In the recent years, mRNA diversity and polymorphisms have been identified in the NOS isoforms. Some of these genetic variations have been associated with PD, indicating an etiological role for the NOS genes. This review mainly focuses on the NOS genes - their differential regulation and genetic heterogeneity, highlighting their significance in the pathobiology of PD.
MeSH term(s)	Gene Expression Regulation, Enzymologic ; Humans ; Nitric Oxide/physiology ; Nitric Oxide Synthase/genetics ; Nitric Oxide Synthase/metabolism ; Parkinson Disease/enzymology ; Parkinson Disease/physiopathology ; RNA, Messenger/genetics
Chemical Substances	RNA, Messenger ; Nitric Oxide (31C4KY9ESH) ; Nitric Oxide Synthase (EC 1.14.13.39)
Language	English
Publishing date	2006-12
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	1362794-6
ISSN	1089-8611 ; 1089-8603
ISSN (online)	1089-8611
ISSN	1089-8603
DOI	10.1016/j.niox.2006.07.003
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Article: Synthesis and in-vitro cytotoxicity evaluation of gatifloxacin Mannich bases.

Yogeeswari, Perumal / Sriram, Dharmarajan / Kavya, Ramkumar / Tiwari, Sonali

Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie

2005 Volume 59, Issue 9, Page(s) 501–510

Abstract: Mannich bases of gatifloxacin were synthesized by reacting them with formaldehyde and several isatin derivatives. Their chemical structures have been confirmed by means of their IR, 1H-NMR data and by elemental analysis. The compounds were tested in- ... ...

Abstract	Mannich bases of gatifloxacin were synthesized by reacting them with formaldehyde and several isatin derivatives. Their chemical structures have been confirmed by means of their IR, 1H-NMR data and by elemental analysis. The compounds were tested in-vitro against a panel of 58 human tumour cell lines derived from nine neoplastic diseases. Among them compound 1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-7[[N4-(3'-sulphadoximino)-1'-(5-bromoisatinyl) methyl]-3-methyl N1-piperazinyl]-3-quinoline carboxylic acid (6) emerged as a potent anticancer agent being more active than standard DNA topoisomerase II inhibitor, etoposide against 30 cancer cell lines.
MeSH term(s)	Antineoplastic Agents/chemical synthesis ; Antineoplastic Agents/toxicity ; Cell Line, Tumor ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical ; Drug Screening Assays, Antitumor ; Etoposide/pharmacology ; Female ; Fluoroquinolones/chemical synthesis ; Fluoroquinolones/toxicity ; Formaldehyde/chemistry ; Humans ; Inhibitory Concentration 50 ; Isatin/analogs & derivatives ; Isatin/chemistry ; Magnetic Resonance Spectroscopy ; Male ; Mannich Bases/chemical synthesis ; Mannich Bases/chemistry ; Molecular Structure ; Reference Standards ; Spectrophotometry, Infrared
Chemical Substances	Antineoplastic Agents ; Fluoroquinolones ; Mannich Bases ; Formaldehyde (1HG84L3525) ; Etoposide (6PLQ3CP4P3) ; Isatin (82X95S7M06) ; gatifloxacin (L4618BD7KJ)
Language	English
Publishing date	2005-10
Publishing country	France
Document type	Comparative Study ; Evaluation Studies ; Journal Article
ZDB-ID	392415-4
ISSN	1950-6007 ; 0753-3322 ; 0300-0893
ISSN (online)	1950-6007
ISSN	0753-3322 ; 0300-0893
DOI	10.1016/j.biopha.2005.06.006
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Article ; Online: Mechanistic evaluation and transcriptional signature of a glutathione S-transferase omega 1 inhibitor

Kavya Ramkumar / Soma Samanta / Anahita Kyani / Suhui Yang / Shuzo Tamura / Elizabeth Ziemke / Jeanne A. Stuckey / Si Li / Krishnapriya Chinnaswamy / Hiroyuki Otake / Bikash Debnath / Vladimir Yarovenko / Judith S. Sebolt-Leopold / Mats Ljungman / Nouri Neamati

Nature Communications, Vol 7, Iss 1, Pp 1-

2016 Volume 13

Abstract: Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform overexpressed in several cancers that has been implicated in drug resistance. Here the authors identify a small molecule inhibitor of GSTO1 that effectively inhibits tumor growth in ... ...

Abstract	Glutathione S-transferase omega 1 (GSTO1) is an atypical GST isoform overexpressed in several cancers that has been implicated in drug resistance. Here the authors identify a small molecule inhibitor of GSTO1 that effectively inhibits tumor growth in colon cancer models, and establish its mechanism of action.
Keywords	Science ; Q
Language	English
Publishing date	2016-10-01T00:00:00Z
Publisher	Nature Portfolio
Document type	Article ; Online
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Article ; Online: Newer N-phthaloyl GABA derivatives with antiallodynic and antihyperalgesic activities in both sciatic nerve and spinal nerve ligation models of neuropathic pain.

Yogeeswari, Perumal / Ragavendran, Jegadeesan Vaigunda / Sriram, Dharmarajan / Kavya, Ramkumar / Vanitha, Kaliappan / Neelakantan, Harshini

Pharmacology

2008 Volume 81, Issue 1, Page(s) 21–31

Abstract: Background: There is considerable research evidence supporting a palliative role for gamma-aminobutyric acid (GABA)-ergic neurotransmission and voltage-gated sodium channel blockade in neuropathic pain conditions. Hence, the present study was undertaken ...

Abstract	Background: There is considerable research evidence supporting a palliative role for gamma-aminobutyric acid (GABA)-ergic neurotransmission and voltage-gated sodium channel blockade in neuropathic pain conditions. Hence, the present study was undertaken to assess the peripheral analgesic, antiallodynic and antihyperalgesic activities of the synthesized structural analogues of GABA. Methods: The screening study included acute tissue injury, chronic constriction injury (CCI), and spinal nerve ligation (SNL) models of neuropathic pain. Results: All of the tested compounds sup-pressed the acetic acid-induced writhing response significantly in comparison to the control. In particular, compound JVP-8 was observed to be the most active compound with percent inhibition greater than that of the standard drug aspirin (97.8% inhibition of writhing response as against 97.0% shown by aspirin). In neuropathic pain studies, compound JVP-5 (100 mg/kg i.p.) emerged as the most active compound affording maximum protection against dynamic allodynia and mechanical hyperalgesia in the CCI model, and against spontaneous pain and mechanical hyperalgesia in SNL rats. Conclusion: In this study, we have demonstrated that combining phthalimide pharmacophore with GABA has evolved compounds effective for the treatment of neuropathic pain.
MeSH term(s)	Analgesics/chemistry ; Analgesics/therapeutic use ; Animals ; Disease Models, Animal ; Female ; Hyperalgesia/drug therapy ; Hyperalgesia/metabolism ; Male ; Mice ; Molecular Structure ; Neuralgia/drug therapy ; Neuralgia/metabolism ; Pain Measurement ; Phthalimides/chemistry ; Phthalimides/therapeutic use ; Rats ; Rats, Wistar ; Sciatic Nerve/injuries ; Spinal Nerves/injuries ; Structure-Activity Relationship ; gamma-Aminobutyric Acid/analogs & derivatives ; gamma-Aminobutyric Acid/therapeutic use
Chemical Substances	Analgesics ; Phthalimides ; gamma-Aminobutyric Acid (56-12-2)
Language	English
Publishing date	2008
Publishing country	Switzerland
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	206671-3
ISSN	1423-0313 ; 0031-7012
ISSN (online)	1423-0313
ISSN	0031-7012
DOI	10.1159/000107711
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Article: 3-Chloro-2-methylphenyl-substituted semicarbazones: synthesis and anticonvulsant activity.

Yogeeswari, Perumal / Thirumurugan, Rathinasabapathy / Kavya, Ramkumar / Samuel, Jayakar Selwyn / Stables, James / Sriram, Dharmarajan

European journal of medicinal chemistry

2004 Volume 39, Issue 8, Page(s) 729–734

Abstract: A series of 3-chloro-2-methylphenyl substituted semicarbazones (3-33) was synthesized and evaluated for anticonvulsant and CNS activities. After intraperitoneal injection to mice or rats, the semicarbazone derivatives were examined in the maximal ... ...

Abstract	A series of 3-chloro-2-methylphenyl substituted semicarbazones (3-33) was synthesized and evaluated for anticonvulsant and CNS activities. After intraperitoneal injection to mice or rats, the semicarbazone derivatives were examined in the maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ), and subcutaneous strychnine (scSTY)-induced seizure and neurotoxicity screens. The aryl urea (1) and the semicarbazide (2) showed anticonvulsant activity in the MES and scPTZ screens with acute neurotoxicity, whereas the semicarbazone derivatives showed good anticonvulsant potency in the scSTY screen with moderate activity against MES and scPTZ screens. Compound 21 exhibited anticonvulsant potency against all the three screens with lesser neurotoxicity. Some titled compounds exhibited lesser CNS depression and neurotoxicity compared to phenytoin or carbamazepine as was evident from the CNS studies.
MeSH term(s)	Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/therapeutic use ; Male ; Mice ; Rats ; Rats, Sprague-Dawley ; Rats, Wistar ; Seizures/prevention & control ; Semicarbazones/chemical synthesis ; Semicarbazones/therapeutic use
Chemical Substances	Anticonvulsants ; Semicarbazones
Language	English
Publishing date	2004-08
Publishing country	France
Document type	Comparative Study ; Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	188597-2
ISSN	1768-3254 ; 0223-5234 ; 0009-4374
ISSN (online)	1768-3254
ISSN	0223-5234 ; 0009-4374
DOI	10.1016/j.ejmech.2004.03.008
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Article ; Online: Design, Synthesis and Structure-activity Studies of Rhodanine Derivatives as HIV-1 Integrase Inhibitors

Kavya Ramkumar / Vladimir N. Yarovenko / Alexandra S. Nikitina / Igor V. Zavarzin / Mikhail M. Krayushkin / Leonid V. Kovalenko / Adrian Esqueda / Srinivas Odde / Nouri Neamati

Molecules, Vol 15, Iss 6, Pp 3958-

2010 Volume 3992

Abstract: Raltegravir was the first HIV-1 integrase inhibitor that gained FDA approval for use in the treatment of HIV-1 infection. Because of the emergence of IN inhibitor-resistant viral strains, there is a need to identify innovative second-generation IN ... ...

Abstract	Raltegravir was the first HIV-1 integrase inhibitor that gained FDA approval for use in the treatment of HIV-1 infection. Because of the emergence of IN inhibitor-resistant viral strains, there is a need to identify innovative second-generation IN inhibitors. Previously, we identified 2-thioxo-4-thiazolidinone (rhodanine)-containing compounds as IN inhibitors. Herein, we report the design, synthesis and docking studies of a series of novel rhodanine derivatives as IN inhibitors. All these compounds were further tested against human apurinic/apyrimidinic endonuclease 1 (APE1) to determine their selectivity. Two compounds showed significant cytotoxicity in a panel of human cancer cell lines. Taken together, our results show that rhodanines are a promising class of compounds for developing drugs with antiviral and anticancer properties.
Keywords	rhodanine ; HIV-1 ; integrase ; APE1 ; 2-thioxo-4-thiazolidinone ; docking ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2010-06-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
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Article: Discovery of 4-aminobutyric acid derivatives possessing anticonvulsant and antinociceptive activities: a hybrid pharmacophore approach.

Yogeeswari, Perumal / Ragavendran, Jegadeesan Vaigunda / Sriram, Dharmarajan / Nageswari, Yarravarapu / Kavya, Ramkumar / Sreevatsan, Narayanan / Vanitha, Kaliappan / Stables, James

Journal of medicinal chemistry

2007 Volume 50, Issue 10, Page(s) 2459–2467

Abstract: Antiepileptic drugs are often utilized in the treatment of neuropathic pain. The present study aims at the design and synthesis of newer gamma-aminobutyric acid (GABA) derivatives with the combination of aryl semicarbazone and the GABA pharmacophores in ... ...

Abstract	Antiepileptic drugs are often utilized in the treatment of neuropathic pain. The present study aims at the design and synthesis of newer gamma-aminobutyric acid (GABA) derivatives with the combination of aryl semicarbazone and the GABA pharmacophores in order to develop a multifunctional drug useful in the treatment of neurological disorders like epilepsy and neuropathic pain. Various GABA semicarbazones were synthesized and screened for anticonvulsant, peripheral analgesic, antiallodynic, and antihyperalgesic activities. The structures of the synthesized compounds were confirmed by the use of their spectral data in addition to elemental analysis. The synthesized derivatives of the inhibitory neurotransmitter GABA produced anticonvulsant and antinociceptive actions in the acetic acid induced writhing test and peripheral nerve injury (chronic constriction injury and L5 spinal nerve ligation) models of neuropathic pain. The underlying mechanisms are expected to be enhancement of peripheral GABAergic neurotransmission owing to their activity in the scPIC screen and due to various reports on the involvement of GABAergic pathway in peripheral models of neuropathic pain.
MeSH term(s)	Analgesics/chemical synthesis ; Analgesics/pharmacology ; Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/pharmacology ; Disease Models, Animal ; Hyperalgesia/drug therapy ; Mice ; Pain/drug therapy ; Pain Measurement ; Peripheral Nerve Injuries ; Peripheral Nervous System Diseases/drug therapy ; Rats ; Semicarbazones/chemical synthesis ; Semicarbazones/pharmacology ; Structure-Activity Relationship ; Touch ; gamma-Aminobutyric Acid/analogs & derivatives ; gamma-Aminobutyric Acid/chemical synthesis ; gamma-Aminobutyric Acid/pharmacology
Chemical Substances	Analgesics ; Anticonvulsants ; Semicarbazones ; gamma-Aminobutyric Acid (56-12-2)
Language	English
Publishing date	2007-05-17
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	218133-2
ISSN	1520-4804 ; 0022-2623
ISSN (online)	1520-4804
ISSN	0022-2623
DOI	10.1021/jm061431g
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Article: Synthesis of N4-(2,4-dimethylphenyl) semicarbazones as 4-aminobutyrate aminotransferase inhibitors.

Yogeeswari, Perumal / Sriram, Dharmarajan / Thirumurugan, Rathinasabapathy / Jeewanlal, Logantha Ramamoorthy / Jit, Sunil / Ragavendran, Jegadeesan Vaigunda / Kavya, Ramkumar / Rakhra, Kavya / Saraswat, Vivek

Acta pharmaceutica (Zagreb, Croatia)

2006 Volume 56, Issue 3, Page(s) 259–272

Abstract: Several 2,4-dimethylphenyl substituted semicarbazones were synthesized in three steps involving aryl urea and aryl semicarbazide formation. The structures were confirmed by spectral and elemental analyses. All the compounds were evaluated for ... ...

Abstract	Several 2,4-dimethylphenyl substituted semicarbazones were synthesized in three steps involving aryl urea and aryl semicarbazide formation. The structures were confirmed by spectral and elemental analyses. All the compounds were evaluated for anticonvulsant activity by using a series of test models, including maximal electroshock seizure, subcutaneous pentylenetetrazole and subcutaneous strychnine seizure threshold tests. The compounds were also evaluated for behavioural impairement and depression activity. In the neurochemical investigation, potent compounds were evaluated for their effects on rat brain gamma-aminobutyric acid (GABA) levels and in vitro gamma-aminobutyrate transaminase (Pseudomonas fluorescens) activity. Preliminary studies suggest that these compounds exhibit anticonvulsant activity via a GABA-mediated mechanism.
MeSH term(s)	4-Aminobutyrate Transaminase/antagonists & inhibitors ; Animals ; Anticonvulsants/chemical synthesis ; Anticonvulsants/pharmacology ; Behavior, Animal/drug effects ; Brain/metabolism ; Disease Models, Animal ; Male ; Mice ; Rats ; Rats, Sprague-Dawley ; Rats, Wistar ; Seizures/drug therapy ; Semicarbazones/chemical synthesis ; Semicarbazones/pharmacology ; gamma-Aminobutyric Acid/drug effects ; gamma-Aminobutyric Acid/metabolism
Chemical Substances	Anticonvulsants ; Semicarbazones ; gamma-Aminobutyric Acid (56-12-2) ; 4-Aminobutyrate Transaminase (EC 2.6.1.19)
Language	English
Publishing date	2006-09
Publishing country	Croatia
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1111806-4
ISSN	1846-9558 ; 1330-0075
ISSN (online)	1846-9558
ISSN	1330-0075
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