Browsing ICR Divisions by author "Jackman, Ann"
Now showing items 1-7 of 7
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Antifolates targeted specifically to the folate receptor
(ELSEVIER SCIENCE BV, 2004-04-29)Most antifolate drugs are efficiently transported by the reduced-folate carrier (RFC). However, several also bind with high affinity to the a-isoform of the folate receptor (alpha-FR) and there is evidence to suggest that ... -
ExPLOITATION OF THE FOLATE RECEPTOR IN THE MANAGEMENT OF CANCER AND INFLAMMATORY DISEASE
(ELSEVIER ACADEMIC PRESS INC, 2008)Over the last 25+ years, the folate receptor (FR) has emerged as an attractive tumor biomarker with the potential to be exploited for therapeutic purposes. Increasing evidence suggests that this enclocytosing protein can ... -
Folate Receptor beta as a Potential Delivery Route for Novel Folate Antagonists to Macrophages in the Synovial Tissue of Rheumatoid Arthritis Patients
(WILEY, 2009-01)Objective. To determine the expression of folate receptor beta (FR beta) in synovial biopsy tissues and peripheral blood lymphocytes from rheumatoid arthritis (RA) patients and to identify novel folate antagonists that are ... -
Imaging pharmacodynamics of the alpha-folate receptor-targeted thymidylate synthase inhibitor BGC 945
(AMER ASSOC CANCER RESEARCH, 2008-05-15)The assessment of tissue-specific pharmacodynamics is desirable in the development of tumor-targeted therapies. Plasma deoxyuridine (dUrd) levels, a measure of systemic thymidylate synthase (TS) inhibition, has limited ... -
Modulation of both endogenous folates and thymidine enhance the therapeutic efficacy of thymidylate synthase inhibitors
(AMER ASSOC CANCER RESEARCH, 2001-05-01)Plasma levels of folates and thymidine in mice are about 10-fold higher than in humans and may influence the therapeutic efficacy of thymidylate synthase (TS) Inhibitors, such as 5-fluorouracil (5FU) and the antifolates ... -
Phase I and pharmacologic study of oral ZD9331, a novel nonpolyglutamated thymidylate synthase inhibitor, in adult patients with solid tumors
(2002-04-01)Purpose: To assess the toxicity profile and dose-limiting toxicities (DLTs), to determine the maximum-tolerated dose, and to study the pharmacokinetics of ZD9331 when administered orally to patients with advanced solid ... -
The role of alpha-folate receptor-mediated transport in the antitumor activity of antifolate drugs
(AMER ASSOC CANCER RESEARCH, 2004-02-01)Purpose: Raltitrexed, pemetrexed, lometrexol, and ZD9331 are antifolate drugs transported into cells via the ubiquitously expressed reduced-folate carrier. They display also high affinity for the alpha-folate receptor ...