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Anil Mathew Tharappel

Anil Mathew Tharappel
College of Pharmacy University of Arizona

Ph.D
Drug discovery in antivirals, antifungals, metabolic syndrome

About

29
Publications
4,443
Reads
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456
Citations
Citations since 2017
13 Research Items
355 Citations
2017201820192020202120222023020406080100120
2017201820192020202120222023020406080100120
2017201820192020202120222023020406080100120
2017201820192020202120222023020406080100120
Introduction
Human infectious diseases, Target based assay development, Screening, Drug- target interaction, Preclinical studies
Additional affiliations
November 2020 - present
The University of Arizona
Position
  • PostDoc Position
Description
  • Target-based assay development, Screening, Mechanism of action, pathogenicity for fungal and viral targets
October 2018 - October 2020
Wadsworth Center, NYS Department of Health
Position
  • Research Affiliate
Description
  • Target based assay development and Screening Small molecules, Mechanism of action, viral and fungal pathogenesis

Publications

Publications (29)
Article
Full-text available
A monoclonal antibody-based immunodot test was compared to a polymerase chain reaction (PCR) assay for managing white spot syndrome virus (WSSV) on shrimp farms at Kundapur and Kumta situated in Udupi and Uttar Kannada Districts, respectively, of Karnataka on the west coast of India. Of 12 grow-out farms in Kundapur, 6 (F1 to F6) yielded shrimp sam...
Conference Paper
Full-text available
Objective Increased 11β-hydroxysteroid dehydrogenase type 1 (HSD11β1) activity has been associated with metabolic syndrome including hyperglycemia. In this regard, selective inhibitors of HSD11β1have considerable potential for treating type 2 diabetes mellitus and other co-morbidities associated with the metabolic syndrome. In the present study, we...
Conference Paper
Retinoid X Receptor α (RXRα) regulates intracellular receptor signaling pathways involved in, among others, glucose and lipid metabolism and has potential to impact multiple risk factors associated with the metabolic syndrome. We report the pharmacological activity of CNX-013-B2, a potent and selective RXRα agonist with pan-PPAR activity, upon qd d...
Article
Full-text available
Objectives: AMP activated protein kinase (AMPK) regulates the coordination of anabolic and catabolic processes and is an attractive therapeutic target for T2DM, obesity and metabolic syndrome. We report the anti-hyperglycemic and anti-hyperlipidemic effects of CNX-012-570 is an orally bioavailable small molecule (molecular weight of 530 Daltons) th...
Conference Paper
Increased 11β-hydroxysteroid dehydrogenase type 1 (HSD11β1) activity has been associated with symptoms of the metabolic syndrome including hyperglycemia. In this regard, selective inhibitors of HSD11B1 have considerable potential for treating type 2 diabetes mellitus and other co-morbidities associated with the metabolic syndrome. In the present st...
Article
Drug resistance is a significant concern in the treatment of diseases, including cryptococcosis caused by Cryptococcus neoformans (Cne) and Cryptococcus gattii (Cga). Alternative drug targets are necessary to overcome drug resistance before it attains a critical stage. Splicing of inteins from pro-protein precursors is crucial for activities of ess...
Article
Full-text available
Multidrug-resistant pathogens are of significant concern in recent years. Hence new antifungal and anti-bacterial drug targets are urgently needed before the situation goes beyond control. Inteins are polypeptides that self-splice from exteins without the need for cofactors or external energy, resulting in joining of extein fragments. Inteins are p...
Article
Full-text available
Zika virus (ZIKV) causes significant human diseases without specific therapy. Previously we found erythrosin B, an FDA-approved food additive, inhibited viral NS2B−NS3 interactions, leading to inhibition of ZIKV infection in cell culture. In this study, we performed pharmacokinetic and in vivo studies to demonstrate the efficacy of erythrosin B aga...
Article
Full-text available
Significance Cryptococcus neoformans is an opportunistic human pathogen, causing cryptococcal meningitis in immunocompromised individuals, with a mortality rate of more than 50%. We previously found that the Prp8 intein was a viable drug target for C. neoformans . In an effort to find new therapies, we developed screening assays and identified a sm...
Article
Full-text available
Many flaviviruses including the Dengue virus (DENV), Zika virus (ZIKV), West Nile virus, Yellow Fever virus, and Japanese encephalitis virus are significant human pathogens, unfortunately without any specific therapy. Here, we demonstrate that methylene blue, an FDA-approved drug, is a broad-spectrum and potent antiviral against Zika virus and Deng...
Article
Full-text available
Coronavirus disease 2019 (COVID-19), caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), has spread worldwide since its first incidence in Wuhan, China, in December 2019. Although the case fatality rate of COVID-19 appears to be lower than that of SARS and Middle East respiratory syndrome (MERS), the higher transmissibility of S...
Article
Full-text available
Zika virus (ZIKV) outbreaks have been reported worldwide, including a recent occurrence in Brazil where it spread rapidly, and an association with increased cases of microcephaly was observed in addition to neurological issues such as GBS that were reported during previous outbreaks. Following infection of neuronal tissues, ZIKV can cause inflammat...
Article
Full-text available
Flaviviruses causes significant human disease. Recent outbreaks of the Zika virus highlight the need to develop effective therapies for this class of viruses. Previously we identified niclosamide as a broad-spectrum inhibitor for flaviviruses by targeting the interface between viral protease NS3 and its cofactor NS2B. Here, we screened a small libr...
Article
Full-text available
The recent outbreak of the betacoronavirus SARS-CoV-2 has become a significant concern to public health care worldwide. As of August 19, 2020, more than 22,140,472 people are infected, and over 781,135 people have died due to this deadly virus. In the USA alone, over 5,482,602 people are currently infected, and more than 171,823 people have died. S...
Chapter
Full-text available
Aquaculture is one of the few fast growing food production sector is facing serious problem due to microbial diseases (viral, bacterial and fungal). Estimated loss due to one pathogen, WSS virus of shrimp is Rs. 1000 Crores per year in India. My area of research is developing simple farmer level diagnostics and oral vaccine for aquaculture. The phi...
Article
Full-text available
The re-emergence of Zika virus (ZIKV) and Ebola virus (EBOV) poses serious and continued threats to the global public health. Effective therapeutics for these maladies is an unmet need. Here, we show that emetine, an anti-protozoal agent, potently inhibits ZIKV and EBOV infection with a low nanomolar half maximal inhibitory concentration (IC50) in...
Conference Paper
CNX-010-710 is a selective small molecule inhibitor of 11-Hydroxysteroid dehydrogenase (11-HSDβ1) with IC50 of 7nM (human) and 64nM (mouse) iso¬forms iso¬forms and displays good tissue distribution and inhibition in mice. Treatment of db/db mice with CNX-010-710 (30 mpk, bid) for 8 weeks caused significant reduction of 17% fasting glucose (333±7 vs...
Conference Paper
Full-text available
Physiological adaptation induced by endurance exercise training has been proven to be protective against obesity and associated metabolic dysfunction as well as maintenance of oxidative muscle mass. Hence an orally active agent with ability to mimic or potentiate the genetic effects of exercise endurance is considered superlative in the space of me...
Article
Full-text available
Background: 11ß-hydroxysteroid dehydrogenase type1 (11β-HSD1) converts inactive glucocorticoids to active glucocorticoids which, in excess, leads to development of the various risk factors of the metabolic syndrome. Recent studies clearly suggest that both increased expression and activity of 11β-HSD1 in metabolically active tissues such as liver,...
Conference Paper
Full-text available
Treatment of 6 weeks old db/db mice orally with 2.5, 5.0 and 10 mg/kg CNX-013-B2 qd (9am) for 8 weeks resulted in a reduction of 20 - 28% in fasting plasma glucose, 11 - 30% in fed plasma glucose, 3 - 24% in Glucose AUC24hrs, 1.4 - 2.4% in HbA1c, 14 - 21% in serum triglyceride and 33 - 42% in LDL-C levels. Though decreases in fasting and fed serum...
Conference Paper
Full-text available
Objectives: AMPK Kinase regulates the coordination of anabolic and catabolic processes and can be an attractive therapeutic target to treat T2DM. We report the anti-hyperglycemic and anti-hyperlipidemic effects of CNX-012-CPD, orally bioavailable small molecule direct activator of AMPK in multiple disease animal models. Methods: Male C57BL/6 mice f...
Conference Paper
Full-text available
Type 2 Diabetes (T2DM) is characterized by the abnormal glucose and lipid metabolism due in part to resistance to the actions of insulin in different tissues. AMPK, a serine/threonine kinase, a cellular energy sensor that regulates the coordination of anabolic and catabolic processes and can be an attractive therapeutic target to treat T2DM. We rep...
Article
Full-text available
Since its first report in 1994, white spot syndrome virus (WSSV) has become widespread in India. We have developed a simple, rapid and sensitive monoclonal antibody (MAb)-based immunodot test for detection of WSSV. Four MAbs of IgG isotype were produced against an Indian isolate of WSSV: 1 MAb recognised a 28 kDa viral protein while the other 3 rec...
Article
Full-text available
Survival and shell quality of juvenile tiger shrimp, Penaeus monodon, exposed to a plant derived toxicant, saponin, were investigated. The 96 h LC50 was 132.07 mg l-1 of saponin. The juvenile tiger shrimp tested against 5, 10, 15 and 20% concentrations of the 96 h LC50 value of saponin for 3, 6, 9, 12, 15 and 18 days recorded shell softening rangin...

Questions

Question (1)
Question
Manual homogenization using glass homogenizer takes lot of time, difficult to handle 50-100 tissue samples per day. Issue with mechanical homogenizer is it can destroy the fungal cells too.

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