CLL cell apoptosis induced by nitric oxide synthase inhibitors: correlation with lipid solubility and NOS1 dissociation constant.
Publication
, Journal Article
Levesque, MC; Ghosh, DK; Beasley, BE; Chen, Y; Volkheimer, AD; O'Loughlin, CW; Gockerman, JP; Moore, JO; Weinberg, JB
Published in: Leuk Res
July 2008
Nitric oxide synthase (NOS) inhibitors induce chronic lymphocytic leukemia (CLL) cell apoptosis and have potential as CLL therapeutics. We determined the half-maximal concentration (ED(50)) of 22 NOS inhibitors that induced CLL cell death in vitro. There was a direct correlation of the NOS1 (but not NOS2) dissociation constant (K(d)) and the hydrophobicity partitioning coefficient of each NOS inhibitor and its ED(50). NOS inhibitors that bound tightly to CLL cell NOS1 and were hydrophobic potently induced CLL cell death. CLL cell RNA and protein analyses confirmed CLL cell NOS1 expression. Our studies permit the rational selection of NOS inhibitors for testing as CLL therapeutics.
Duke Scholars
Published In
Leuk Res
DOI
ISSN
0145-2126
Publication Date
July 2008
Volume
32
Issue
7
Start / End Page
1061 / 1070
Location
England
Related Subject Headings
- Solubility
- Reverse Transcriptase Polymerase Chain Reaction
- Nitric Oxide Synthase
- Lipid Metabolism
- Leukemia, Lymphocytic, Chronic, B-Cell
- Immunology
- Humans
- Enzyme Inhibitors
- DNA Primers
- Coculture Techniques
Citation
APA
Chicago
ICMJE
MLA
NLM
Levesque, M. C., Ghosh, D. K., Beasley, B. E., Chen, Y., Volkheimer, A. D., O’Loughlin, C. W., … Weinberg, J. B. (2008). CLL cell apoptosis induced by nitric oxide synthase inhibitors: correlation with lipid solubility and NOS1 dissociation constant. Leuk Res, 32(7), 1061–1070. https://doi.org/10.1016/j.leukres.2007.11.026
Levesque, Marc C., Dipak K. Ghosh, Bethany E. Beasley, Youwei Chen, Alicia D. Volkheimer, Charles W. O’Loughlin, Jon P. Gockerman, Joseph O. Moore, and J Brice Weinberg. “CLL cell apoptosis induced by nitric oxide synthase inhibitors: correlation with lipid solubility and NOS1 dissociation constant.” Leuk Res 32, no. 7 (July 2008): 1061–70. https://doi.org/10.1016/j.leukres.2007.11.026.
Levesque MC, Ghosh DK, Beasley BE, Chen Y, Volkheimer AD, O’Loughlin CW, et al. CLL cell apoptosis induced by nitric oxide synthase inhibitors: correlation with lipid solubility and NOS1 dissociation constant. Leuk Res. 2008 Jul;32(7):1061–70.
Levesque, Marc C., et al. “CLL cell apoptosis induced by nitric oxide synthase inhibitors: correlation with lipid solubility and NOS1 dissociation constant.” Leuk Res, vol. 32, no. 7, July 2008, pp. 1061–70. Pubmed, doi:10.1016/j.leukres.2007.11.026.
Levesque MC, Ghosh DK, Beasley BE, Chen Y, Volkheimer AD, O’Loughlin CW, Gockerman JP, Moore JO, Weinberg JB. CLL cell apoptosis induced by nitric oxide synthase inhibitors: correlation with lipid solubility and NOS1 dissociation constant. Leuk Res. 2008 Jul;32(7):1061–1070.
Published In
Leuk Res
DOI
ISSN
0145-2126
Publication Date
July 2008
Volume
32
Issue
7
Start / End Page
1061 / 1070
Location
England
Related Subject Headings
- Solubility
- Reverse Transcriptase Polymerase Chain Reaction
- Nitric Oxide Synthase
- Lipid Metabolism
- Leukemia, Lymphocytic, Chronic, B-Cell
- Immunology
- Humans
- Enzyme Inhibitors
- DNA Primers
- Coculture Techniques