| Letters
in Drug Design & Discovery
ISSN: 1570-1808
Letters in Drug Design &
Discovery
Volume 3, Number 10, December 2006
| Prediction of the Conformation
of the Human P2X7 Receptor Pp. 675-682 |
Peter P. Mager, P. Illes &
H. Walther
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| The Chemokine CXCL10 as a Therapeutic
Target in Animal Models of Neuroinflammatory Disease
Pp. 683-688 |
R. Gonzalez, Jenny L. Hardison,
J. Glaser, Michael T. Liu, Thomas E. Lane &
Hans S. Keirstead
The chemokine CXCL10 is upregulated in several
neuroinflammatory disorders and plays a critical
role in MS and SCI animal models. The studies reviewed
here demonstrate the feasibility of using a neutralizing
antibody against CXCL10 to reduce the Th1 mediated
detrimental neuroinflammatory response typical of
MS and SCI, while enhancing tissue sparing, axonal
sprouting and angiogenesis. |
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| Bridged Piperazines and Piperidines
as CCR1 Antagonists with Oral Activity in Models of Arthritis
and Multiple Sclerosis Pp. 689-694 |
L. Revesz, B. Bollbuck, T. Buhl,
J. Dawson, R. Feifel, R. Heng, P. Hiestand, H. Sparrer,
A. Schlapbach, R. Waelchli & P. Loetscher
Compound 2 of a series of bridged piperazines and
piperidines coupled to 2-acetylamino-4-chloro-5-methoxy
cinnamic acid exhibited the desired equal potency
against human, mouse and rat CCR1 (IC50=20;
22; 28nM). 2 showed a superior pharmacokinetic profile
and inhibited the clinical grades in rat acute EAE
(experimental autoimmune encephalomyelitis) and
knee swelling in rat AIA (antigen induced arthritis)
at doses of 30 and 15 mg/kg p.o. bid. |
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| Future Prospects for Old Chemotherapeutic
Drugs in the Target-Specific Era; Pharmaceutics, Combinations,
Co-Drugs and Prodrugs with Melphalan as an Example
Pp. 695-703 |
M. Wickström, H. Lövborg
& J. Gullbo
Melphalan (R1=H; R2=OH) is
one of the classical alkylating agents that have
been used in cancer therapy for almost fifty years,
and still has a place in modern chemotherapy with
new regimens, combinations and pharmaceutical compositions.
Being derived from a natural amino acid (Phe) the
molecule invites to chemical modification to construct
targeted derivatives, as discussed in the present
article. |
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| Optimization and Therapeutic Activity
of Liposome-Conjugated Monoclonal Antibodies Against the
ErbB family of Receptor Tyrosine Kinases: First Step in
the Development of Therapeutic Antibody/Liposomal Anticancer
Drug Combinations Pp. 704-713 |
Gigi N.C. Chiu, Troy O. Harasym,
Paul G. Tardi, Marcel B. Bally & Dawn N. Waterhouse
Long circulating liposome carriers that have
covalently attached, therapeutically active monoclonal
antibodies (mAb) specific for EGFR (HER1) or HER2
were designed with foci on extended circulation
lifetime, improved mAb delivery to tumors and selection
of a coupling strategy that did not compromise the
anti-tumor activity of the mAb.
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| Bleomycin-Induced Oxidative Stress
and Lung Injury in Rats: Inhibition by Curcumin
Pp. 714-722 |
D. Punithavathi, M. Babu, V.
Arumugam & N. Venkatesan
Numerous studies suggest that oxidative stress may
play a role in bleomycin-induced lung injury and
fibrosis. This article reports the evidence that
curcumin can inhibit bleomycin-induced oxidative
stress, indicating that the strategy of utilizing
curcumin in conditions of increased oxidative stress
has important implications for lung diseases. |
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| Relaxation Behavior and Crystallization
Kinetics of Amorphous Acetaminophen Pp. 723-730 |
G.T. Rengarajan & M. Beiner
Relaxation behavior and crystallization kinetics
of amorphous acetaminophen are studied by dielectric
spectroscopy and standard DSC. The α
and β
processes are parameterized based on dielectric
scans at various temperatures and measurements during
isothermal crystallization are used to specify the
crystallization behavior. |
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| Maintenance Treatment of Opioid
Dependence and Patterns of Non-Prescribed Drug Use: Results
of a 4-Year Trial Pp. 731-740 |
Salvatore M. Giacomuzzi, M.
Ertl, M. Pavlic, K. Libiseller, Y. Riemer, G. Kemmler,
H. Rössler, P. Grubwieser, W. Rabl & H.
Hinterhuber
The study was designed to establish the extent to
which participants in maintenance treatment programmes
(methadone and sublingual buprenorphine) used opioids,
benzodiazepines, ethanol, cocaine and amphetamines,
and to define the pattern of such use over time.
Hereby analytical techniques used included enzyme-multiplied
immunoassay and gas chromatography-mass spectrometry.
In summary, the present data indicate that nonprescribed
drug use remains a persistent problem for patients
in maintenance treatment. Most misused substances
include mainly opioids and benzodiazepines. Nonprescribed
morphine has replaced heroin. |
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| Oleoylethanolamide: a Molecular
Cross-Talk with Leptin in Feeding Behaviour Regulation
Pp. 741-746 |
B. Brito, R. Castro & A.C.
de León
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| Synthesis and Preliminary Evaluation
of L-Dopa/Benserazide Conjugates as Dual Acting Codrugs
Pp. 747-752 |
A. Di Stefano, P. Sozio, A.
Iannitelli, A. Cocco, G. Orlando & M. Ricciutelli
The synthesis and "in vitro"
chemical and enzymatic stability of Dopa/Benserazide
conjugates (2, 3) as dual acting codrugs. Our findings
indicate that compounds 2 and 3 show good stability
toward g.i. hydrolysis releasing LD and benserazide
in rat plasma after enzymatic hydrolysis. |
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| Gracilins G-I, Cytotoxic Bisnorditerpenes
from Spongionella pulchella, and the Anti-Adhesive Properties
of Gracilin B Pp. 753-760 |
A. Rueda, A. Losada, R. Fernández,
C. Cabañas, Luis F. García Fernández,
F. Reyes & C. Cuevas
The isolation, structural characterization and cytotoxic
properties of three new bisnorditerpenes (Gracilins
G-I) are described. In addition, the anti adhesive
properties of Gracilin B are also disclosed. |
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| Synthesis and Biochemical Evaluation
of a Range of Non-Substituted Phenyl Alkyl Triazole-Based
Compounds as Potential Inhibitors of the Enzyme Complex
17α-Hydroxylase/17,20-Lyase
(P45017α)
Pp. 761-765 |
Caroline P. Owen, Chirag H.
Patel, S. Dhanani & S. Ahmed
We report the synthesis and biochemical evaluation
of a number of triazole-based compounds as potential
inhibitors of P45017α. |
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