生物化学技术

The purity control and the structure verification of compound collections from automated synthesis and combinatorial chemistry play an essential role in the success of medicinal chemistry programs. High performance liquid chromatography (HPLC), mass spectrometry (MS), and l ...

The development of combinatorial chemistry has made a profound impact on the pharmaceutical industry by producing a large number of structurally diverse compounds in a very short amount of time. Combined with high-throughput screening, bioinformatics, and laboratory automatio ...

Combinatorial methods have been applied with a measure of success in the field of metal ion coordination chemistry (1–5). High-throughput screening methods have been used to facilitate the discovery of new catalysts and to design ligands for binding metal ions (6–9). Metal ion coordination ...

Sequencing of the human and other genomes has revolutionized drug discovery. Modern functional genomics methods have brought a wealth of drug discovery targets. Bioinformatic tools are classifying candidate drug targets into different mechanistic classes. Many classes are ap ...

Last year marked the completion of the sequencing effort on the human genome. Advances in the fields of genomics and bioinformatics are widely expected to bring forth a large number of new biochemical targets for drug design by linking specific diseases to single genes or collections thereof. T ...

With the advent of high-throughput technologies in drug discovery, combinatorial chemistry has superseded natural products as the prime source of compounds to be tested in biological screening (1). The reason being that compared with classical synthesis, high-throughput chemis ...

With the current and ever-growing offering of reagents along with the vast palette of organic reactions, virtual libraries accessible to combinatorial chemists have dramatically increased in size. Yet, extracting suitable subsets for experimentation is an essential step in the de ...

Half a century ago, the term “drug discovery” conjured images of adventures into the jungle, beneath the sea, and atop mountains in search of frogs, sponges, lichens, or any unstudied life form that, ground up, might exhibit inhibitory effects toward a major human disease. More romantic and exciting ...

In the past decade, it became clear that some fundamental problems were arising in drug discovery. It was becoming harder to find new chemical entities with substantial advantages over existing drugs. Consequently, it became riskier and more expensive to develop new drug entities.

The cytoskeleton of mammalian cells is a complex assembly of microfilaments microtubules, and intermediate filaments. The thicker fibers are the microtubules which have a diameter of approx 25 nM and an apparently hollow core; microfilaments have a diameter of 6 nM, but the third type of filam ...

The aliphatic polyamines (putrescine, cadaverine, spermidine, and spermine) are flexible polycations, since under physiological conditions they exhibit 2, 3, or 4 positive charges, respectively, and are able to rotate around the carbon-carbon or carbon-nitrogen bonds, imparti ...

Protein kinases have critical roles for the amplification and distribution of the signals that are sent from the cell surface to the cytoplasm after ligand binding. They are generally classified into two groups: protein-serine/threonine kinases, such as cAMP-dependent protein kina ...

The cytosolic calcium concentration, (Ca2+)c, represents in many types of cells a versatile regulatory system involved in several signal transduction pathways of cell activation (1), and is tightly regulated in human platelets. Under basal conditions, platelets maintain the (Ca2+)c ...

The modulatory potency of lectins on cellular activities deserves attention from a cell biological and a clinical point-of-view. In addition to serving as tools to delineate signaling processes that follow carbohydrate-dependent cell binding, plant lectins can apparently affe ...

The interaction of lectins with various normal or malignant cells not infrequently results in their proliferation or death (1-3). Incubation of normal T-lymphocytes with some lectins, such as Con A and PHA stimulates their proliferation and renders them highly cytotoxic and capable of ly ...

One of the major obstacles in postoperative management of lung transplant recipients is differentiating between rejection and infection episodes. In addition, there are no reliable methods routinely to monitor lung allografts to ascertain that they are well tolerated by the host. Co ...

Lectins are highly active biological molecules that are present in large quantities in the human diet. Changes in colonic epithelial glycoconjugates, such as the enhanced expression of the Thomsen-Friedenreich (TF) antigen, are commonly seen in hyperplastic, premalignant, and ma ...

The firefly luciferase-based assay differs from most familiar enzyme-based determinations. Most enzyme assays are based either on the production of a product or the disappearance of a substrate. Usually the compound measured is stable so that its concentration can be determined after a s ...

The green fluorescent protein (GFP; 1–5) from the jellyfish Aequorea Victoria has emerged as an important reporter for monitoring gene expresston, protein localization, cell transformation, and cell lineage in VIVO and in real time. Unlike other bioluminescent reporters, the chromo ...

There are an increasing number of specialized instruments that may be used for the purpose of measuring bioluminescence. Table 1 contains a representative list of different luminometers and cameras that are available. These instruments have been used to detect bioluminescence in a num ...