Quinazolines

Publication Title: 
PloS One

Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease that causes progressive paralysis due to motor neuron death. Several lines of published evidence suggested that inhibition of epidermal growth factor receptor (EGFR) signaling might protect neurons from degeneration. To test this hypothesis in vivo, we treated the SOD1 transgenic mouse model of ALS with erlotinib, an EGFR inhibitor clinically approved for oncology indications.

Author(s): 
Le Pichon, Claire E.
Dominguez, Sara L.
Solanoy, Hilda
Ngu, Hai
Lewin-Koh, Nicholas
Chen, Mark
Eastham-Anderson, Jeffrey
Watts, Ryan
Scearce-Levie, Kimberly
Publication Title: 
Antimicrobial Agents and Chemotherapy

Tetra-acetamide pyrroloquinazolinediamine (PQD-A4) and bis-ethylcarbamyl pyrroloquinazolinediamine (PQD-BE) are new derivatives of pyrroloquinazolinediamine (PQD) and are being investigated as potential chemotherapeutic agents for the treatment of malaria. Comparative studies to assess the therapeutic indices of PQD-A4, PQD-BE, and PQD were conducted in Plasmodium berghei-infected rats following daily intragastric dosing for three consecutive days. Artesunate (AS), a standard drug for treatment of severe malaria, was used as a comparator.

Author(s): 
Xie, Lisa H.
Li, Qigui
Lin, Ai J.
Smith, Kirsten
Zhang, Jing
Skillman, Donald S.
Publication Title: 
Cancer Prevention Research (Philadelphia, Pa.)

Chemoprevention of head and neck squamous cell carcinoma (HNSCC), a disease associated with high mortality rates and frequent occurrence of second primary tumor (SPT), is an important clinical goal. The epidermal growth factor receptor (EGFR)-signal transducer and activator of transcription (STAT)-3 signaling pathway is known to play a key role in HNSCC growth, survival, and prognosis, thereby serving as a potential therapeutic target in the treatment of HNSCC.

Author(s): 
Leeman-Neill, Rebecca J.
Seethala, Raja R.
Singh, Shivendra V.
Freilino, Maria L.
Bednash, Joseph S.
Thomas, Sufi M.
Panahandeh, Mary C.
Gooding, William E.
Joyce, Sonali C.
Lingen, Mark W.
Neill, Daniel B.
Grandis, Jennifer R.
Publication Title: 
Journal of Ethnopharmacology

Experiments were conducted to evaluate the scientific basis of the use of the trikatu group of acrids (long pepper, black pepper and ginger) in the large number of prescriptions in Ayurveda. [3H] vasicine and [3H] sparteine were taken as test drugs. Piper longum (long pepper) increased the blood levels of vasicine by nearly 233%. Under the influence of piperine, the active principle of Piper species, sparteine blood levels increased more than 100%. The results suggest that these acrids have the capacity to increase the bioavailability of certain drugs.

Author(s): 
Atal, C. K.
Zutshi, U.
Rao, P. G.
Publication Title: 
Cancer Prevention Research (Philadelphia, Pa.)

Chemoprevention of head and neck squamous cell carcinoma (HNSCC), a disease associated with high mortality rates and frequent occurrence of second primary tumor (SPT), is an important clinical goal. The epidermal growth factor receptor (EGFR)-signal transducer and activator of transcription (STAT)-3 signaling pathway is known to play a key role in HNSCC growth, survival, and prognosis, thereby serving as a potential therapeutic target in the treatment of HNSCC.

Author(s): 
Leeman-Neill, Rebecca J.
Seethala, Raja R.
Singh, Shivendra V.
Freilino, Maria L.
Bednash, Joseph S.
Thomas, Sufi M.
Panahandeh, Mary C.
Gooding, William E.
Joyce, Sonali C.
Lingen, Mark W.
Neill, Daniel B.
Grandis, Jennifer R.
Publication Title: 
Phytomedicine: International Journal of Phytotherapy and Phytopharmacology

Adhatoda vasica Nees, Acanthaceae, is well known plant in Ayurveda and Unani medicine. The purpose of this study was to characterize the most bioactive phytochemicals viz., vasicine, vasicinone, vasicine acetate, 2-acetyl benzyl amine, vasicinolone present in the chloroform fraction having anti-inflammatory and antimicrobial activities. The anti-inflammatory activity was tested by using carrageenan and CFA-model induced paw oedema. The antimicrobial activity of isolated compounds was assessed by using the microdilution method.

Author(s): 
Singh, Bharat
Sharma, Ram Avtar
Publication Title: 
Clinical Cancer Research: An Official Journal of the American Association for Cancer Research

PURPOSE: To examine the enzyme kinetics of gefitinib and erlotinib metabolism by individual cytochrome P450 (CYP) enzymes, and to compare their effects on CYP3A activity, with the aim to better understand mechanisms underlying pharmacokinetic variability and clinical effects. EXPERIMENTAL DESIGN: Enzyme kinetics were examined by incubating gefitinib or erlotinib (1.5-50 micromol/L) with recombinant human CYP3A4, CYP3A5, CYP2D6, CYP1A1, CYP1A2, and CYP1B1 (10-160 pmol/mL).

Author(s): 
Li, Jing
Zhao, Ming
He, Ping
Hidalgo, Manuel
Baker, Sharyn D.
Publication Title: 
The Journal of Clinical Investigation

Probiotic bacteria can potentially have beneficial effects on the clinical course of several intestinal disorders, but our understanding of probiotic action is limited. We have identified a probiotic bacteria-derived soluble protein, p40, from Lactobacillus rhamnosus GG (LGG), which prevents cytokine-induced apoptosis in intestinal epithelial cells. In the current study, we analyzed the mechanisms by which p40 regulates cellular responses in intestinal epithelial cells and p40's effects on experimental colitis using mouse models.

Author(s): 
Yan, Fang
Cao, Hanwei
Cover, Timothy L.
Washington, M. Kay
Shi, Yan
Liu, LinShu
Chaturvedi, Rupesh
Peek, Richard M.
Wilson, Keith T.
Polk, D. Brent
Publication Title: 
Cancer Biology & Therapy

The inverse correlation between levels of dietary calcium and colorectal cancer (CRC) incidence has been extensively investigated. However, the impact of supplemental calcium on cancer therapy remains unknown. We used four models of CRC, Caco-2 and HCT116 human cancer cell lines and Apc (Min/+) and azoxymethane carcinogen-induced mouse models, to investigate the impact of a western-style diet low in calcium (0.05%) vs. a similar diet but supplemented with calcium (5%) on therapeutic targeting of the epidermal growth factor receptor (EGFR).

Author(s): 
Rinella, Erica S.
Bankaitis, Eric D.
Threadgill, David W.
Publication Title: 
PloS One

Molecule-targeted therapies are being widely developed and deployed, but they are frequently less effective in clinical trials than predicted based upon preclinical studies. Frequently, only a single model or genetic background is utilized using diets that are not relevant to that consumed by most cancer patients, which may contribute to the lack of predictability of many preclinical therapeutic studies. Inhibition of epidermal growth factor receptor (EGFR) in colorectal cancer was used to investigate potential causes for low predictive values of many preclinical studies.

Author(s): 
Rinella, Erica S.
Threadgill, David W.

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