| Letters
in Drug Design & Discovery
ISSN: 1570-1808
Letters in Drug Design &
Discovery
Volume 3, Number 7, September 2006
| Artificial Neural Network Modeling
of Phytoestrogen Binding to Estrogen Receptors Pp.
436-442 |
S. Agatonovic-Kustrin &
J.V. Turner
A QSAR incorporating theoretical descriptors
was developed utilizing sequential multiple-output
artificial neural networks. Significant steric,
constitutional, topological and electronic descriptors
were identified including quaternary carbon, aromatic
oxygen, valence connectivity index, H-bonding, hydrophilic
surface and shape descriptors. |
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| The Role of Glioma Microenvironment
in Immune Modulation: Potential Targets for Intervention
Pp. 443-451 |
Mahua Dey, S. Farzana Hussain
& Amy B. Heimberger
Malignant gliomas are associated with poor
prognoses despite surgical, radiation and chemotherapy
interventions and the future design of glioma immunotherapy
clinical trials will need to address immune modulation
at multiple levels for efficacious results. This
review discusses emerging data that provides novel
insights into immune modulation and the next generation
of immunotherapy, focusing on the synergistic functioning
of the tumor immune microenvironment with systematic
immune activation. |
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| Ruthenium Polypyridyl Complexes:
Synthesis, Characterization and Biological Activity on
Leishmania (L) Mexicana Pp. 454-458 |
Maribel Navarro, Oscar A. Corona
S, Ibis Colmenares & Edgar Marchan
[Ru(bipy)2phendiamine](PF6)2
and [Ru(phen)2phendione](PF6)2
were tested in vitro on Leishmania (L) mexicana
promastigotes, showed a moderated growth inhibition
of the parasite at low concentration. Leishmanistatic
activity could be related to ruthenium complexes-DNA
parasite interactions as possible mechanism of action. |
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| Targeting 5-Lipoxygenase Signaling
Pathways to Reverse Drug Resistance in Cancer Pp.
459-461 |
Alfonso Catalano & Antonio
Procopio
5-Lipoxygenase (5-LO), which leads to the biosynthesis
of eicosanoids, is frequently detected in cancer
patients. This review describes the evidence that
inhibitors of 5-LO can promote apoptosis in cancer
cells and they can be used to overcome resistance
to chemotherapeutic agents. |
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| Insights from Affinity Labeling
into Nucleotide- and Coenzyme-Dependent Enzyme Catalysis
and Regulation Pp. 462-480 |
Roberta F. Colman
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| Platelet Synthesis of DOPEGAL,
the Free Radical Generating Metabolite of Norepinephrine:
Potential Target for Protective Therapy in Arteriosclerosis
Pp. 481-487 |
W.J. Burke, S.W. Li, K.N. Gillespie,
H.D. Chung, K. Jagadeesan & J.H. Joist
Free radical damage and platelet interaction with
injured endothelial cells are implicated in initiation
of arteriosclerosis. This study was designed to
determine if platelet monoamine oxidase (MAO) synthesizes
3,4-dihydroxyphenylglycolaldehyde (DOPEGAL) the
free radical generating metabolite of norepinephrine
(NE) and if serum DOPEGAL levels increase in patients
with risk factors for arteriosclerosis associated
with elevated NE levels. We conclude that platelet
MAO synthesizes DOPEGAL from NE in a manner dependent
on both NE and platelet concentrations. DOPEGAL
could contribute to arteriosclerosis in medical
conditions with elevated NE levels. Platelet synthesis
of DOPEGAL provides a target for protective therapy
to prevent arteriosclerosis in these conditions. |
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| Mycophenolic Acid Use in Glomerulonephritis
Pp. 488-493 |
Elisabetta Bertoni, Alessandra
Stagnitto, Silvia Farsetti & Maurizio Salvadori
Mycophenolic acid (MPA), the active metabolite of
MMF, is a reversible and non competitive inhibitor
of inosine monophosphate dehydrogenase (IMPDH) the
rate-limiting enzyme for the de novo pathway of
purine synthesis. Consequently, MPA inhibits preferentially
lymphocyte proliferation. Its efficacy is mostly
documented in organ transplantation. We have reviewed
the efficacy in glomerulonephritis. |
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| Synthesis and Biological Evaluation
of Coumarin Linked Fluoroquinolones, Phthalimides and
Naphthalimides as Potential DNA Gyrase Inhibitors Pp.
494-502 |
Ahmed Kamal, M. Satyanarayana,
V. Devaiah, V. Rohini, J. S. Yadav, B. Mullick &
V. Nagaraja
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| Adipopharmacology, a Novel Drug
Discovery Approach: A Metabotrophic Perspective Pp.
503-505 |
G.N. Chaldakov, M. Fiore, A.B.
Tonchev & L. Aloe
Adipopharmacology connotes adipotargeting studies
aimed at drug discovery. Here we focus on adipopharmacology
of nerve growth factor,brain-derived neurotrophic
factor, ciliary neurotrophic factor and metallothioneins.
Because these factors improve glucose, lipid and
antioxidant metabolism, we named them metabotrophic
factors (metabotrophins). |
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| New Heterocyclic Hydrazones in
the Search for Antitubercular Agents: Synthesis and In
Vitro Evaluations Pp. 506-512 |
A. Bijev
16 Hydrazones containing pyrrole cycle were synthesized
as potential tuberculostatics and nine showed 92-100%
inhibition of M. tuberculosis H37Rv
at 6.25 µg/mL. Two leads exhibited low minimum
inhibitory concentrations (MIC) and excellent selectivity
indexes (SI). |
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