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Single-domain antibody

A single-domain antibody (sdAb), also known as a Nanobody, is an antibody fragment consisting of a single monomeric variable antibody domain. Like a whole antibody, it is able to bind selectively to a specific antigen. With a molecular weight of only 12–15 kDa, single-domain antibodies (sdAbs) are much smaller than common antibodies which are composed of two heavy protein chains and two light chains, and even smaller than Fab fragments and single-chain variable fragments.

Properties
A single-domain antibody is a peptide chain of about 110 amino acids long, comprising one variable domain (VH) of a heavy-chain antibody, or of a common IgG. These peptides have similar affinity to antigens as whole antibodies, but are more heat-resistant and stable towards detergents and high concentrations of urea. Those derived from camelid and fish antibodies are less lipophilic and more soluble in water, owing to their complementarity-determining region 3 (CDR3), which forms an extended loop (coloured orange in the ribbon diagram above) covering the lipophilic site that normally binds to a light chain. In contrast to common antibodies, two out of six single-domain antibodies survived a temperature of 90 °C (194 °F) without losing their ability to bind antigens in a 1999 study. Stability towards gastric acid and proteases depends on the amino acid sequence. Some species have been shown to be active in the intestine after oral application, but their low absorption from the gut impedes the development of systemically active orally administered single-domain antibodies. File:Single domain antibody.tif|thumb|The complex of a single domain antibody and a protein antigen reveals a buried binding site. This property has been shown to result from their extended CDR3 loop, which is able to penetrate such buried sites. == Production ==
Production
From heavy-chain antibodies A single-domain antibody can be obtained by immunization of dromedaries, camels, llamas, alpacas or sharks with the desired antigen and subsequent isolation of the mRNA coding for the variable region (VNAR and VHH) of heavy-chain antibodies. Large phage displayed VNAR and VHH single domain libraries were established from nurse sharks and dromedary camels. Screening techniques like phage display and ribosome display help to identify the clones binding the antigen. From conventional antibodies Alternatively, single-domain antibodies can be made from common murine, rabbit or human IgG with four chains. The process is similar, comprising gene libraries from immunized or naïve donors and display techniques for identification of the most specific antigens. A problem with this approach is that the binding region of common IgG consists of two domains (VH and VL), which tend to dimerize or aggregate because of their lipophilicity. Monomerization is usually accomplished by replacing lipophilic by hydrophilic amino acids, but often results in a loss of affinity to the antigen. If affinity can be retained, the single-domain antibodies can likewise be produced in E. coli, GPC2 and GPC3 were isolated by phage display. The HN3 human single-domain antibodies have been used to create immunotoxins and chimeric antigen receptor (CAR) T cells for treating liver cancer. Blocking the Wnt binding domain of GPC3 by the HN3 human single-domain antibody inhibits Wnt activation in liver cancer cells. == Potential applications ==
Potential applications
Single-domain antibodies allow a broad range of applications in biotechnical as well as therapeutic use due to their small size, simple production and high affinity. The coupling of an anti-GFP Nanobody to a monovalent matrix, called GFP-nanotrap, allows the isolation of GFP-fusion proteins and their interacting partners for further biochemical analyses. Single molecule localization with super-resolution imaging techniques requires the specific delivery of fluorophores into close proximity with a target protein. Due to their large size the use of antibodies coupled to organic dyes can often lead to a misleading signal owing to the distance between the fluorophore and the target protein. The fusion of organic dyes to anti-GFP nanobodies targeting GFP-tagged proteins allows nanometer spatial resolution and minimal linkage error because of the small size and high affinity. The size dividend of nanobodies also benefits the correlative light-electron microscopy study. Without any permeabilization agent, the cytoplasm of the chemically fixed cells are readily accessible to the fluorophore tagged nanobodies. Their small size also allows them to penetrate deeper into volumetric samples than regular antibodies. High ultrastructural quality is preserved in the tissue that is imaged by fluorescence microscope and then electron microscope. This is especially useful for the neuroscience research that requires both molecular labeling and electron microscopic imaging. In diagnostic biosensor applications nanobodies may be used prospectively as a tool. Due to their small size, they can be coupled more densely on biosensor surfaces. In addition to their advantage in targeting less accessible epitopes, their conformational stability also leads to higher resistance to surface regeneration conditions. After immobilizing single-domain antibodies on sensor surfaces sensing human prostate-specific antigen (hPSA) were tested. The nanobodies outperformed the classical antibodies in detecting clinical significant concentrations of hPSA. To increase the crystallization probability of a target molecule, nanobodies can be used as crystallization chaperones. As auxiliary proteins, they can reduce the conformational heterogeneity by binding and stabilizing just a subset of conformational states. They also can mask surfaces interfering with the crystallization while extending regions that form crystal contacts. nanobodies targeting the cell receptor binding domain of the virulence factors toxin A and toxin B of Clostridioides difficile were shown to neutralize cytopathic effects in fibroblasts in vitro. Nanobody conjugates recognizing antigen presenting cells have been successfully used for tumor detection or targeted antigen delivery to generate strong immune response. Orally available single-domain antibodies against E. coli-induced diarrhoea in piglets have been developed and successfully tested. Detergent-stable species targeting a surface protein of Malassezia furfur have been engineered for use in anti-dandruff shampoos. Caplacizumab, a single-domain antibody targeting von Willebrand factor is in clinical trials for the prevention of thrombosis in patients with acute coronary syndrome. A Phase II study examining ALX-0081 in high risk percutaneous coronary intervention has started in September 2009. Ablynx expects that their nanobodies might cross the blood–brain barrier and permeate into large solid tumours more easily than whole antibodies, which would allow for the development of drugs against brain cancers. One of the most common causes of naganaTrypanosoma brucei brucei – can be targeted by sdAbs. Stijlemans et al. 2004 succeeded in inducing effective sdAbs from rabbit and Camelus dromedarius by displaying a variable surface glycoprotein antigen to the vertebrates' immune systems using a phage. In the future, these therapies will surpass natural antibodies by reaching locations currently unreachable due to natural antibodies' larger size. == References ==
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