Search Results - "Hosagrahara, Vinayak P."

Raising HDL cholesterol without inducing hepatic steatosis and hypertriglyceridemia by a selective LXR modulator by Miao, Bowman, Zondlo, Susan, Gibbs, Sandy, Cromley, Debra, Hosagrahara, Vinayak P., Kirchgessner, Todd G., Billheimer, Jeffrey, Mukherjee, Ranjan

“…Liver X receptors (LXRs) are ligand-activated transcription factors that belong to the nuclear receptor superfamily. LXRs activate transcription of a spectrum…”
Get full text

Evaluation of Pharmaceutical Excipients as Cosolvents in 4-Methyl Umbelliferone Glucuronidation in Human Liver Microsomes: Applications for Compounds with Low Solubility by Argikar, Upendra A., Liang, Guiqing, Bushee, Jennifer L., Hosagrahara, Vinayak P., Lee, Wendy

“…Standard incubation procedures for carrying out microsomal assays involve the use of less than 1% w/v organic solvents to minimize the potential inhibitory…”
Get full text

Discovery of Imidazo[1,2‑a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis by Tantry, Subramanyam J, Markad, Shankar D, Shinde, Vikas, Bhat, Jyothi, Balakrishnan, Gayathri, Gupta, Amit K, Ambady, Anisha, Raichurkar, Anandkumar, Kedari, Chaitanyakumar, Sharma, Sreevalli, Mudugal, Naina V, Narayan, Ashwini, Naveen Kumar, C. N, Nanduri, Robert, Bharath, Sowmya, Reddy, Jitendar, Panduga, Vijender, Prabhakar, K. R, Kandaswamy, Karthikeyan, Saralaya, Ramanatha, Kaur, Parvinder, Dinesh, Neela, Guptha, Supreeth, Rich, Kirsty, Murray, David, Plant, Helen, Preston, Marian, Ashton, Helen, Plant, Darren, Walsh, Jarrod, Alcock, Peter, Naylor, Kathryn, Collier, Matthew, Whiteaker, James, McLaughlin, Robert E, Mallya, Meenakshi, Panda, Manoranjan, Rudrapatna, Suresh, Ramachandran, Vasanthi, Shandil, Radha, Sambandamurthy, Vasan K, Mdluli, Khisi, Cooper, Christopher B, Rubin, Harvey, Yano, Takahiro, Iyer, Pravin, Narayanan, Shridhar, Kavanagh, Stefan, Mukherjee, Kakoli, Balasubramanian, V, Hosagrahara, Vinayak P, Solapure, Suresh, Ravishankar, Sudha, Hameed P, Shahul

“…The approval of bedaquiline to treat tuberculosis has validated adenosine triphosphate (ATP) synthase as an attractive target to kill Mycobacterium…”
Get full text

Discovery of Pyrazolopyridones as a Novel Class of Noncovalent DprE1 Inhibitor with Potent Anti-Mycobacterial Activity by Panda, Manoranjan, Ramachandran, Sreekanth, Ramachandran, Vasanthi, Shirude, Pravin S, Humnabadkar, Vaishali, Nagalapur, Kavitha, Sharma, Sreevalli, Kaur, Parvinder, Guptha, Supreeth, Narayan, Ashwini, Mahadevaswamy, Jyothi, Ambady, Anisha, Hegde, Naina, Rudrapatna, Suresh S, Hosagrahara, Vinayak P, Sambandamurthy, Vasan K, Raichurkar, Anandkumar

“…A novel pyrazolopyridone class of inhibitors was identified from whole cell screening against Mycobacterium tuberculosis (Mtb). The series exhibits excellent…”
Get full text

The Discovery of N‑(1-Methyl-5-(trifluoromethyl)‑1H‑pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)‑1H‑indole-1-carboxamide (Acrizanib), a VEGFR‑2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration by Adams, Christopher M, Anderson, Karen, Artman, Gerald, Bizec, Jean-Claude, Cepeda, Rosemarie, Elliott, Jason, Fassbender, Elizabeth, Ghosh, Malay, Hanks, Shawn, Hardegger, Leo A, Hosagrahara, Vinayak P, Jaffee, Bruce, Jendza, Keith, Ji, Nan, Johnson, Leland, Lee, Wendy, Liu, Donglei, Liu, Fang, Long, Debby, Ma, Fupeng, Mainolfi, Nello, Meredith, Erik L, Miranda, Karl, Peng, Yao, Poor, Stephen, Powers, James, Qiu, Yubin, Rao, Chang, Shen, Siyuan, Sivak, Jeremy M, Solovay, Catherine, Tarsa, Peter, Woolfenden, Amber, Zhang, Chun, Zhang, Yiqin

“…A noninvasive topical ocular therapy for the treatment of neovascular or “wet” age-related macular degeneration would provide a patient administered…”
Get full text

Functional analysis of human microsomal epoxide hydrolase genetic variants by Hosagrahara, Vinayak P., Rettie, Allan E., Hassett, Christopher, Omiecinski, Curtis J.

“…Human microsomal epoxide hydrolase (EPHX1) is active in the metabolism of many potentially carcinogenic or otherwise genotoxic epoxides, such as those derived…”
Get full text

Discovery of Oral VEGFR‑2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration by Meredith, Erik L, Mainolfi, Nello, Poor, Stephen, Qiu, Yubin, Miranda, Karl, Powers, James, Liu, Donglei, Ma, Fupeng, Solovay, Catherine, Rao, Chang, Johnson, Leland, Ji, Nan, Artman, Gerald, Hardegger, Leo, Hanks, Shawn, Shen, Siyuan, Woolfenden, Amber, Fassbender, Elizabeth, Sivak, Jeremy M, Zhang, Yiqin, Long, Debby, Cepeda, Rosemarie, Liu, Fang, Hosagrahara, Vinayak P, Lee, Wendy, Tarsa, Peter, Anderson, Karen, Elliott, Jason, Jaffee, Bruce

“…The benefit of intravitreal anti-VEGF therapy in treating wet age-related macular degeneration (AMD) is well established. Identification of VEGFR-2 inhibitors…”
Get full text

Identification and Mitigation of a Reactive Metabolite Liability Associated with Aminoimidazoles by Srivastava, Abhishek, Ramachandran, Sreekanth, Hameed, Shahul P, Ahuja, VijayKamal, Hosagrahara, Vinayak P

“…Reactive metabolites (RMs) have been implicated as causal factors in many drug-associated idiosyncratic toxicities. This study aims at identification and…”
Get full text

Evaluation of the metabolism, bioactivation and pharmacokinetics of triaminopyrimidine analogs toward selection of a potential candidate for antimalarial therapy by Srivastava, Abhishek, Panduga, Vijender, Saralaya, Ramanatha, K. R., Prabhakar, Hameed, Shahul, Solapure, Suresh, Hosagrahara, Vinayak P.

“…1. During the course of metabolic profiling of lead Compound 1, glutathione (GSH) conjugates were detected in rat bile, suggesting the formation of reactive…”
Get full text

Lipid Peroxide-Mediated Oxidative Rearrangement of the Pyrazinone Carboxamide Core of Neutrophil Elastase Inhibitor AZD9819 in Blood Plasma Samples by Gu, Chungang, Lewis, Richard J, Wells, Andrew S, Svensson, Per H, Hosagrahara, Vinayak P, Johnsson, Eskil, Hallström, Gösta

“…This study focused on the mechanistic interpretation of ex vivo oxidation of a candidate drug in blood plasma samples. An unexpected lipid peroxide-mediated…”
Get full text

Evaluation of Pharmaceutical Excipients as Cosolvents in 4-Methyl Umbelliferone Glucuronidation in Human Liver Microsomes: Applications for Compounds with Low Solubility by Upendra A.ARGIKAR, Guiqing LIANG, Jennifer L.BUSHEE, Vinayak P.HOSAGRAHARA, Wendy LEE

“…Summary: Standard incubation procedures for carrying out microsomal assays involve the use of less than 1% w/v organic solvents to minimize the potential…”
Get full text

Induction of the Metabolism of Midazolam by Rifampin in Cultured Porcine Hepatocytes: Preliminary Evidence for CYP3A Isoforms in Pigs by HOSAGRAHARA, V. P, HANSEN, L. K, REMMEL, R. P

“…The induction of putative CYP3A isoforms in cultured porcine hepatocytes was evaluated by measurement of midazolam metabolism, a model substrate of the CYP3A…”
Get full text

Evaluation of the effect of culture matrices on induction of CYP3A isoforms in cultured porcine hepatocytes by Hosagrahara, Vinayak P, Hansen, Linda K, Beilman, Gregory J, Remmel, Rory P

“…Several bioartificial liver devices have been developed as temporary therapy for patients suffering from fulminant hepatic failure. Some of these devices…”
Get full text

The Discovery of N -(1-Methyl-5-(trifluoromethyl)-1 H -pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1 H -indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration by Adams, Christopher M., Anderson, Karen, Artman, Gerald, Bizec, Jean-Claude, Cepeda, Rosemarie, Elliott, Jason, Fassbender, Elizabeth, Ghosh, Malay, Hanks, Shawn, Hardegger, Leo A., Hosagrahara, Vinayak P., Jaffee, Bruce, Jendza, Keith, Ji, Nan, Johnson, Leland, Lee, Wendy, Liu, Donglei, Liu, Fang, Long, Debby, Ma, Fupeng, Mainolfi, Nello, Meredith, Erik L., Miranda, Karl, Peng, Yao, Poor, Stephen, Powers, James, Qiu, Yubin, Rao, Chang, Shen, Siyuan, Sivak, Jeremy M., Solovay, Catherine, Tarsa, Peter, Woolfenden, Amber, Zhang, Chun, Zhang, Yiqin

Get full text

Concise review of the cytochrome P450s and their roles in toxicology by OMIECINSKI, C. J, REMMEL, R. P, HOSAGRAHARA, V. P

Get full text

Reactivity of mefenamic acid 1-o-acyl glucuronide with proteins in vitro and ex vivo by McGurk, K A, Remmel, R P, Hosagrahara, V P, Tosh, D, Burchell, B

“…Mefenamic acid is a nonsteroidal anti-inflammatory drug commonly used in analgesia. The use of this drug has been implicated in several cases of nephrotoxicity…”
Get more information