8 results match your criteria hpaf-ii compounds

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Cryptic Biosynthesis of the Berkeleypenostatins from Coculture of Extremophilic sp.

J Nat Prod 2021 05 6;84(5):1656-1665. Epub 2021 May 6.

Coculture fermentation of and yielded berkeleypenostatins A-G (-) as well as the previously reported berkeleylactones A-H, the known macrolide A26771B, citrinin, and patulin. As was true with the berkeleylactones, there was no evidence of the berkeleypenostatins in either axenic culture. The structures were deduced from analyses of spectral data, and the absolute configuration of berkeleypenostatin A () was determined by single-crystal X-ray crystallography. Read More

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Aphanin, a triterpenoid from Amoora rohituka inhibits K-Ras mutant activity and STAT3 in pancreatic carcinoma cells.

Tumour Biol 2016 Sep 22;37(9):12455-12464. Epub 2016 Jun 22.

Tumor Biology and Experimental Therapeutics Program, Institute of Oncology Research (IOR), Bellinzona, Switzerland.

Mutations of the K-Ras gene occur in over 90 % of pancreatic carcinomas, and to date, no targeted therapies exist for this genetically defined subset of cancers. STAT3 plays a critical role in KRAS-driven pancreatic tumorigenesis, suggesting its potential as a therapeutic target in this cancer. Therefore, finding novel and potential drugs to inhibit oncogenic K-Ras is a major challenge in cancer therapy. Read More

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September 2016

Targeting cMET with INC280 impairs tumour growth and improves efficacy of gemcitabine in a pancreatic cancer model.

BMC Cancer 2015 Feb 19;15:71. Epub 2015 Feb 19.

Department of Surgery, University Hospital Regensburg, University of Regensburg, Franz-Josef-Strauss Allee 11, 93053, Regensburg, Germany.

Background: Expression and activation of the cMET receptor have been implicated in tumor progression and resistance to chemotherapy in human pancreatic cancer. In this regard we assessed the effects of targeting cMET in pancreatic cancer models in vitro and in vivo.

Methods: Human (L3. Read More

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February 2015

An engineered cysteine-modified diabody for imaging activated leukocyte cell adhesion molecule (ALCAM)-positive tumors.

Mol Imaging Biol 2012 Jun;14(3):336-47

Crump Institute for Molecular Imaging, Department of Molecular and Medical Pharmacology, David Geffen School of Medicine at University of California, Los Angeles, Los Angeles, CA, USA.

Purpose: The purpose of this study was to generate and evaluate a positron emission tomography (PET) radiotracer targeting activated leukocyte cell adhesion molecule (ALCAM).

Procedures: A human anti-ALCAM single chain variable fragment was reformatted to produce a covalent dimer, termed a cys-diabody (CysDb). Purified CysDb was characterized by gel electrophoresis and size exclusion chromatography, and immunoreactivity was assessed by flow cytometry and immunofluorescence. Read More

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Mucin overexpression limits the effectiveness of 5-FU by reducing intracellular drug uptake and antineoplastic drug effects in pancreatic tumours.

Eur J Cancer 2009 Jan 4;45(1):164-73. Epub 2008 Dec 4.

Northeastern University, Bouvé College of Health Sciences, Department of Pharmaceutical Sciences, Boston, MA 02115, USA.

Current treatments for pancreatic cancer have failed to effectively manage the disease, and hence, more effective treatment approaches are urgently needed. Studies suggest that mucin O-glycosylation limits the cytotoxic effect of fluorouracil (5-FU) against the growth of human pancreatic cancer cells in vitro. In the present study, we investigated the relationship between the levels of mucin O-glycosylation expressed in pancreatic tumours and the antitumour effect of 5-FU. Read More

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January 2009

High-throughput analysis of HGF-stimulated cell scattering.

J Biomol Screen 2008 Oct 23;13(9):847-54. Epub 2008 Sep 23.

Department of Drug Design and Optimization/Automated Lead Optimization, Merck Research Laboratories Boston, Boston, Massachusetts 02115, USA.

Historically, only relatively low-throughput or expensive methods have been available to measure cell migration. Hepatocyte growth factor (HGF) is a ligand for the tyrosine kinase receptor Met that, in addition to mediating proliferation and survival, increases cell motility and metastasis. The authors have developed a high-throughput imaging assay for measuring inhibition of HGF-induced scattering in human HPAF-II pancreatic adenocarcinoma cells. Read More

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October 2008

Mucin impedes cytotoxic effect of 5-FU against growth of human pancreatic cancer cells: overcoming cellular barriers for therapeutic gain.

Br J Cancer 2007 Oct 2;97(7):910-8. Epub 2007 Oct 2.

Department of Pharmaceutical Sciences, Northeastern University, 360 Huntington Avenue, Bouvé College of Health Sciences, Boston, MA 02115, USA.

Mucins are high molecular weight glycoproteins expressed on the apical surface of normal epithelial cells. In cancer disease mucins are overexpressed on the entire cellular surface. Overexpression of MUC1 mucin in pancreatic tumours has been correlated with poor patient survival. Read More

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October 2007

Evaluation of antimitotic activity of Rotula aquatica (Lour): a traditional herb used in treatment of cancer.

Indian J Exp Biol 2004 Sep;42(9):893-9

Department of Pharmacognosy and Phytochemistry, Prin K M Kundnani College of Pharmacy, 47, R G Thadani Marg, Worli, Mumbai 400 018, India.

Rotula aquatica was extensively used by vaidyas (Ayurvedic practioners) in holistic treatment of cancer. In the present study, an attempt has been made to evaluate the antimitotic activity of R. aquatica. Read More

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September 2004
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