نتایج جستجو برای: chemosensitizers

تعداد نتایج: 102  

Journal: :Bioorganic & medicinal chemistry letters 2011
Willmen Youngsaye Benjamin Vincent Cathy L Hartland Barbara J Morgan Sara J Buhrlage Stephen Johnston Joshua A Bittker Lawrence MacPherson Sivaraman Dandapani Michelle Palmer Luke Whitesell Susan Lindquist Stuart L Schreiber Benito Munoz

The effectiveness of the potent antifungal drug fluconazole is being compromised by the rise of drug-resistant fungal pathogens. While inhibition of Hsp90 or calcineurin can reverse drug resistance in Candida, such inhibitors also impair the homologous human host protein and fungal-selective chemosensitizers remain rare. The MLPCN library was screened to identify compounds that selectively reve...

Journal: :Clinical cancer research : an official journal of the American Association for Cancer Research 1996
M Lehnert R de Giuli P R Twentyman

Clinical studies of agents capable of reversing P-glycoprotein (Pgp)-mediated multidrug resistance have attracted much attention in recent years. One question of interest in such studies is whether the concentrations achieved by chemosensitizers are sufficient to inhibit Pgp function. The goal of the present study was to develop a reliable ex vivo bioassay for analysis of the Pgp-inhibiting act...

Journal: :Cancer letters 2014
Velthe Drinberg Rivka Bitcover Wolf Rajchenbach Dan Peer

Inherent and acquired multiple drug resistance (MDR) to chemotherapeutic drugs is a major obstacle in cancer treatment. The ATP Binding Cassettes (ABC) transporter super family that act as extrusion pumps such as P-glycoprotein and multidrug-resistance-associated-proteins have prominent roles in cancer MDR. One of the most efficient strategies to modulate this active drug efflux from the cells ...

2015
Yusuke Oku Naoyuki Nishiya Toshiya Shito Reiichiro Yamamoto Yasufumi Yamamoto Chihiro Oyama Yoshimasa Uehara

YAP and TAZ oncoproteins confer malignancy and drug resistance to various cancer types. We screened for small molecules that inhibit the nuclear localization of YAP/TAZ. Dasatinib, statins and pazopanib inhibited the nuclear localization and target gene expression of YAP and TAZ. All three drugs induced phosphorylation of YAP and TAZ, and pazopanib induced proteasomal degradation of YAP/TAZ. Th...

2015
Izabela Ła̧cka Marek T. Konieczny Anita Bułakowska Marie Kodedová Dana Gašková Indresh K. Maurya Rajendra Prasad Sławomir Milewski

Three structurally related oxathiolone fused chalcone derivatives appeared effective chemosensitizers, able to restore in part sensitivity to fluconazole of multidrug-resistant C. albicans strains. Compound 21 effectively chemosensitized cells resistant due to the overexpression of the MDR1 gene, compound 6 reduced resistance of cells overexpressing the ABC-type drug transporters CDR1/CDR2 and ...

Journal: :Bioorganic & medicinal chemistry 2005
Isabel Masip Nuria Cortés Maria-José Abad Marisa Guardiola Enrique Pérez-Payá José Ferragut Antonio Ferrer-Montiel Angel Messeguer

Herein is reported the optimized solid-phase synthesis of a library of 5,120 trimeric N-alkylglycines (peptoids) using the positional scanning format and the submonomer strategy. Diversity at the N-terminal position was generated from 20 commercially available primary amines, whereas 16 primary amines were employed for the middle and C-terminal positions of the trimers. Formation of undesirable...

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