Plants defend themselves from other organisms by elaborating bioactive chemical
defences. This is the essential basis of the use of herbal medicines that still represents a
major therapeutic resort for much of humanity However, at the outset, it must be stated that
any plant that is not part of our evolved dietary cultures is potentially dangerous.
Commercial herbal medicinal preparations approved by expert regulatory authorities have a
significant place in mainstream conventional medicine and in complementary medicine.
Tuyển tập các báo cáo nghiên cứu về y học được đăng trên tạp chí y học Critical Care giúp cho các bạn có thêm kiến thức về ngành y học đề tài: Bimodal action of the flavonoid quercetin on basophil function: an investigation of the putative biochemical targets...
Most drugs against malaria that are available or under development target
a single process of the parasite infective cycle, favouring the appearance of
resistant mutants which are easily spread in areas under chemotherapeutic
Annexin B1 fromCysticercus cellulosaehas recently been identified using
immunological screening in an attempt to find novel antigens for vaccine
development against cysticercosis. The protein possesses anticoagulant
activity and carries significant therapeutic potential due to its thrombus-targeting and thrombolytic properties.
The copines are a family of C2- and von Willebrand factor A-domain-con-taining proteins that have been proposed to respond to increases in intra-cellular calcium by translocating to the plasma membrane. The copines
have been reported to interact with a range of cell signalling and cytoskele-tal proteins, which may therefore be targeted to the membrane following
increases in cellular calcium.
PUF proteins regulate both stability and translation through sequence-spe-cific binding to the 3¢ UTR of target mRNA transcripts. Binding is medi-ated by a conserved PUF domain, which contains eight repeats of
approximately 36 amino acids each. Found in all eukaryotes, they have
been related to several developmental processes.
There are seven members of the proprotein convertase (PC) family of secre-ted serine proteases that cleave their substrates at basic amino acids,
thereby activating a variety of hormones, growth factors, and viruses.
PC1⁄3, PC2 and PC5⁄6A are the only members of the PC family that are
targeted to dense core secretory granules, where they carry out the process-ing of proteins that are secreted from the cell in a regulated manner.
Of the fourPlasmodiumspecies that cause human malaria,Plasmodium fal-ciparumis responsible for the most severe form of the disease and this par-asite is developing resistance to the major antimalarial drugs. Therefore, in
order to control malaria it is necessary to identify new drug targets.
The currently accepted model of moult control in crusta-ceans relies entirely on the hypothesis that moult-inhibiting
hormone (MIH) and crustacean hyperglycaemic hormone
(CHH) repress ecdysteroid synthesis of the target tissue
(Y-organ) only during intermoult, and that changes in syn-thesis and/or release of these neurohormones are central to
The characterization of the gene encodingLeishmania
donovaniphosphofructokinase (PFK) and the biochemical
properties of the expressedenzyme are reported.L. donovani
has a singlePFKgene copyperhaploidgenome that encodes
a polypeptide with a deducedmolecular mass of 53 988 and
a pI of 9.26. The predicted amino acid sequence contains a
C-terminal tripeptide that conforms to an established signal
for glycosome targeting.
The discovery of a new drug is a challenging task that includes (a) identifica-
tion of a biochemical target for certain diseases and (b) screening of a large
number of compounds from libraries of compounds arising from synthetic
chemistry, combinatorial chemistry, and natural product isolation for lead gen-
eration. The lead compound is then optimized based on biological activity,
selectivity, pharmacokinetic property, and metabolism.
The modern drug discovery process, in general, involves the identiﬁcation of a biochemical target (usually protein target), screening of synthetic compounds or compound libraries from combinatorial chemistry/natural sources for a lead compound, and optimization of the lead compound (activity, selectivity, pharmacokinetics, etc.) for recommending a potential clinical candidate.
Candida albicansis the most prevalent yeast pathogen in humans, and
recently it has become increasingly resistant to the current antifungal
agents. In this study we investigatedC. albicansdihydroorotate dehydroge-nase (DHODH, EC 18.104.22.168), which catalyzes the fourth step ofde novo
pyrimidine synthesis, as a new target for controlling infection.
MicroRNAs (miRNAs) regulate gene expression post-transcriptionally by
binding to target mRNAs in a sequence-specific manner. A large number
of genes appear to be the target of miRNAs, and an essential role for
miRNAs in the regulation of various conserved cell signaling cascades,
such as mitogen-activated protein kinase, Notch and Hedgehog
Ammonium assimilation is tightly regulated in nitrogen-fixing bacteria; the
target of regulation is primarily the activity of the key enzyme glutamine
synthetase that is regulated by reversible covalent modification by AMP
groups in reactions catalysed by the bifunctional adenylyltransferase
(ATase). The properties and regulation of ATase fromEscherichia colihave
been studied in great detail.
The building blocks of most signal transduction pathways are pairs of
enzymes, such as kinases and phosphatases, that control the activity of pro-tein targets by covalent modification. It has previously been shown [Gold-beter A & Koshland DE (1981)Proc Natl Acad Sci USA78, 6840–6844]
that these systems can be highly sensitive to changes in stimuli if their cata-lysing enzymes are saturated with their target protein substrates.
The 6-kDa early secretory antigenic target (ESAT-6) and culture filtrate
protein-10 (CFP-10), expressed from the region of deletion-1 (RD1) of
Mycobacterium tuberculosisH37Rv, are known to play a key role in viru-lence. In this study, we explored the thermodynamic and biochemical chan-ges associated with the formation of the 1 : 1 heterodimeric complex
between ESAT-6 and CFP-10.
Hepatic insulin resistance in the leptin-receptor defective Zucker fa⁄fa rat
is associated with impaired glycogen synthesis and increased activity of
phosphorylase-a. We investigated the coupling between phosphorylase-a
and glycogen synthesis in hepatocytes from fa⁄fa rats by modulating the
concentration of phosphorylase-a.
Discovery of a new chemical entity that exerts pharmacological effects for
curing or treating diseases or relieving symptoms is only the first step in
the drug developmental process. In the developmental cycle of a new
drug, the delivery of a desired amount of a therapeutic agent to the target
at a specific time or duration is as important as its discovery. In order
to realize the optimal therapeutic outcomes, a delivery system should
be designed to achieve the optimal drug concentration at a predetermined
rate and at the desired location....