生物化学技术

Despite the great arsenal of analytical techniques, the success of detection, identification and quantitation of pesticide residues depends initially on the analyte extraction and/or concentration method. These methods are the most problematic step in the chemical analyses of r ...

Lysosomal acid lipase (LAL, E.C. 3.1.1.13) is a hydrolase involved in the intracellular degradation of lipoproteins. LAL was first described in fibroblasts (1), and since then found in all analyzed tissues with the exception of erythrocytes (2,3). The enzyme hydrolyzes cholesterol esters a ...

Hormone-sensitive lipase (HSL) catalyzes the rate-limiting step in the hydrolysis of stored triacylglycerols in adipocytes, i.e., the hydrolysis of triacylglycerol to diacylglycerol (for a recent review on HSL, see ref. 1). It also catalyzes the hydrolysis of diacylglycerols and mon ...

Lecithin:cholesterol acyltransferase (LCAT; EC 2.3.1.43) is a 67 kDa glycoprotein that is responsible for cholesterol esterification in plasma (1). LCAT has an important physiological role in the maturation of nascent, discoidal high density lipoproteins (HDL) to mature, spheric ...

In recent years heparin-Sepharose chromatography has revolutionized the purification of enzymes and macromolecules. This method utilizes the specific and electrostatic interactions of heparin with enzymes, growth factors, receptors and blood coagulation factors (1–3). ...

Lipoprotein lipase (LPL) plays a central role in lipoprotein metabolism. LPL is the major enzyme responsible for the hydrolysis of triglycerides in VLDL and chylomicrons. Following hydrolysis of the triglyceride core of lipoproteins, some of the LPL molecules remain associated with c ...

Hepatic lipase (HL) is necessary for efficient clearance of triglyceride-rich lipoproteins from plasma (1). In humans, HL deficiency leads to the accumulation of triglyceride-rich intermediate density lipoproteins (IDL), LDL, and large HDL (2–4). Inhibition of hepatic lipase in rats ...

Through its ability to catalyze the hydrolysis of triglycerides and phospholipids, hepatic lipase (HL) has been shown to influence the metabolism of a broad range of circulating lipoproteins (1). HL is synthesized and secreted by hepatocytes and is found bound, through an ionic interacti ...

The limited availability of purified hormone-sensitive lipase (HSL) has been one of the major obstacles in working with this enzyme. The low tissue abundance (approx 1 �g HSL/g adipose tissue) and the labile and hydrophobic character of HSL, are the major difficulties encountered in its purif ...

Over the past few years, combinatorial chemistry has emerged as an exciting new approach to discover novel drug candidates. It contains many tactics and processes for the rapid synthesis of large, organized collections of lowmolecular-weight compounds without tedious and time-con ...

Cross-linked polymer supports are now ubiquitous throughout the fields of combinatorial chemistry, organic synthesis, and catalysis (1,2). However, problems associated with the heterogeneous nature of the ensuing chemistry and with “on-bead” spectroscopic characteriza ...

Since the introduction of solid-phase peptide synthesis by Merrifield (1) nearly forty years ago, solid-phase techniques have been applied to the construction of a variety of biopolymers and extended into the field of small molecule synthesis. The last decade has seen the emergence of solid ...

Combinatorial chemistry (1–7) has drastically modified the drug discovery process by allowing the rapid simultaneous preparation of numerous organic molecules to feed bioassays. Most of the time, syntheses are carried out using solid-phase methodology (8). The target compounds a ...

The revolution in genomics and proteomics is projected to expand the number of potential therapeutic targets to between 5,000 and 10,000 from the approximately 500 targets that have historically been used by the pharmaceutical industry in the development of drugs (1,2). The research and de ...

An inherent feature of parallel solid phase synthesis is the need to handle a large number of reaction vessels at the same time. Consequently, in order to make demanding synthetic tasks manageable, two categories of synthesizers, manual and automated, have been designed and produced. The main f ...

Small molecules that recognize double-stranded DNA have the capacity to modulate various cellular processes, including DNA replication and repair, gene expression, cell cycle regulation, and growth, and therefore may serve as treatments for cancers or various genetic diseases. C ...

The recent interest in organic solid phase synthesis, triggered by the advent of chemical combinatorial methods (1–7), also accelerated methodology development. Simplification of chemical protocols, their robustness, and amenability to handling large arrays of compounds, pr ...

Very few diseases are directly caused by ion channel mutations, yet many drugs for various diseases work by modulating ion channel activity. This is because ion channels are cellular “gatekeepers,” monitoring intracellular concentrations of Na+, Ca+, K+, or Cl− to control cardiac pacemaki ...

At the heart of host—guest chemistry is the design and construction of artificial receptors. While great progress has been achieved in the specific recognition of a multitude of substrates, rational design has still failed to equal the degree of association strength and substrate specif ...

As human enzymes and cell surface receptors possess handedness, the enantiomers of a racemic pair of compounds may be absorbed, activated, and degraded in different manners. In some instances, two enantiomers of a racemic drug may have different or even opposite pharmacological activit ...