Epsilon Molecular Engineering Co., Ltd. (Headquarters: Saitama City, Saitama Prefecture, President and CEO: Naoto Nemoto, hereinafter referred to as "the Company") is pleased to announce that a scientific paper on the humanized artificial library of next-generation antibody VHH (*1), " PharmaLogical® Library" (*2), jointly developed with Mitsui Information Co., Ltd. (Headquarters: Minato-ku, Tokyo, President and CEO: Kengo Asano), was published online in Antibodies on January 30, 2022 (local time) ( https://www.mdpi.com/2073-4468/11/1/10 ).
Antibodies is an international, peer-reviewed, open-access journal on antibodies.
VHH is the variable region of heavy chain antibodies produced by camelid animals, which are expected to be next-generation antibody drugs. VHH is attracting attention because it has excellent properties for pharmaceutical applications. Various artificial libraries have been constructed as a way to efficiently obtain VHH, but a challenge is that they do not possess the structural characteristics of VHH derived from camelid animals. To solve this problem, our company has worked to design a humanized VHH artificial library that can reproduce the structural characteristics of VHH derived from camelid animals, and has developed the " PharmaLogical® Library".
Our company has built a screening platform that combines this innovative VHH library, " PharmaLogical® Library," with our core technology, cDNA display technology (*3). We are deploying "The Month," a unique VHH high-throughput screening platform that can obtain dozens or more VHHs in a short period of about one month from a library with a vast diversity of 10 trillion to 100 trillion molecules, possessing high affinity and stability at the nM to pM level.
" The Month ," which began operation in April 2021 , is currently used by our company in joint research and development with domestic and international pharmaceutical companies, as well as in our own projects. It has received very high praise because it enables the acquisition of highly affinity and stable humanized VHH for target molecules that were difficult to obtain using conventional VHH libraries and screening methods.
Furthermore, we are constantly working on technological innovations in VHH, such as AI-integrated in silico screening and the construction of the second-generation " PharmaLogical® Library" to accelerate screening, and are advancing its implementation in society. Through our technology and pipeline, we will continue to create next-generation antibody VHH drugs and contribute to patients.
[ Features of PharmaLogical® Library]
- Designed based on crystal structure analysis data of VHH antibodies.
This humanized artificial VHH library was designed based on structural characteristics obtained from co-crystal structure analysis data of human FR sequences already in clinical use and VHH antigens. Therefore, it can reproduce the structural diversity of CDR3, which is a characteristic of VHH antibodies. Furthermore, the CDRs that form the antigen recognition sites were designed based on structural characteristics information obtained from alpaca-derived VHH, and by greatly randomizing the CDR3, which is known to contribute most to antigen binding, even greater diversity is achieved.
- Designed to suppress the frequency of amino acid appearance that causes heterogeneity in formulation.
Amino acids that are easily modified, as well as those that can cause major structural changes such as cysteine and proline residues, can lead to heterogeneity in the formulation process. By designing CDRs that suppress the frequency of these amino acids, it is possible to minimize the challenges that arise in the drug discovery process.
*1 VHH: This refers to the variable domain of heavy chain antibody, which is composed solely of heavy chains found in camelid animals. It has superior stability and physical properties compared to ordinary antibodies.
*2 " PharmaLogical " is a registered trademark of our company.
*3 cDNA display technology: A technology that allows the acquisition of target proteins in vitro by matching genotypes/phenotypes. It is possible to screen 10 trillion to 100 trillion types of molecules at once.
About Epsilon Molecular Engineering Co., Ltd.
Epsilon Molecular Engineering Co., Ltd. (EME) is a bio-venture company that has been developing innovative modality pharmaceuticals based on evolutionary molecular engineering since 2016. Leveraging its unique screening technology and molecular design methods, EME engages in collaborative research and development not only in pharmaceutical development but also in diagnostic agents and regenerative medicine reagents. With the corporate mission of "Creating the future with biomolecules," EME aims to contribute broadly to society and people's lives.
Homepage: https://www.epsilon-mol.co.jp/
[About Mitsui Information Co., Ltd.]
Mitsui Information Co., Ltd. (MKI), under the slogan "Connecting with Knowledge, Creating the Future," acts as a business strategy partner centered on ICT, co-creating IT strategies with clients and supporting their digital transformation. Leveraging the "KNOWLEDGE" cultivated over half a century of technology and expertise, MKI will continue to take on challenges as a "value creation company" that creates value together with its clients.
Homepage: https://www.mki.co.jp/
*Company names and product names mentioned in this release are trademarks or registered trademarks of their respective companies.
[Contact]
Epsilon Molecular Engineering Co., Ltd.
Pharmaceutical Development Division, Business Development Section
E-mail: contact_eme@epsilon-mol.co.jp