Home LeadArt Biotechnologies Files IPO Prospectus: Pioneering Automation-Driven Chemical Proteomics to Build High-Quality Target Data and an Early-Stage Drug Pipeline Engine

LeadArt Biotechnologies Files IPO Prospectus: Pioneering Automation-Driven Chemical Proteomics to Build High-Quality Target Data and an Early-Stage Drug Pipeline Engine

Feb 21, 2022 08:00 CST Updated 08:00

With the completion of the human genome sequencing, it has become evident that gene expression is intricately complex; the same gene may play entirely different roles under varying conditions and at different stages. It is increasingly recognized that genomics alone cannot answer many questions regarding human life processes. As proteins are the actual executors of gene functions, a deeper understanding of their function, structure, localization, as well as protein-protein and protein-small molecule interactions, is more conducive to elucidating the essence of life phenomena.

 

Each cell contains up to 10,000 different types of proteins, with abundance variations spanning at least six orders of magnitude. This makes it extremely challenging to determine which proteins a drug targets within living cells. Chemical proteomics is an approach used to understand the interactions between small chemical molecules (such as drugs and metabolic small molecules) and proteins in biological systems. It enables the quantitative identification of protein targets of drugs within cells, thereby elucidating drug mechanisms of action or identifying off-target effects.

 

Chemical proteomics is an emerging field that continues to expand, and a comprehensive definition has not yet been established in academia. As a new technology in the post-genomic era, it undoubtedly serves as a bridge linking proteomics with drug target research and novel drug discovery.

 

After three decades of scientific advancement, chemical proteomics, as a groundbreaking technology for drug target analysis, has entered the application phase in the pharmaceutical industry. However, current chemical proteomics workflows remain heavily reliant on manual operations and have not yet been automated. Its widespread adoption faces a series of challenges, including complex procedures, low data reproducibility, limited throughput, and high experimental costs.

 

Leadart is the first biotechnology company in China and among the earliest globally to leverage chemical proteomics technologies for the discovery of innovative protein targets and the development of novel drugs, thereby filling the gap in the commercial application of chemical proteomics in China. Furthermore, by integrating bioautomation technologies and equipment systems, Leadart is committed to building the world’s first automation-driven chemical proteomics drug discovery platform.

 

Ni Feng, Founder and CEO of LeadartIt stated: “Chemical proteomics is, in essence, a matter of precisely and quantitatively sequencing proteins within the drug-binding microenvironment. However, this process is highly labor-intensive and demands extensive experience as well as operational consistency. Ningbo Leadart Biotechnology Co., Ltd. has prioritized the development of an automation-driven chemical proteomics platform, aiming to enable rapid, low-cost matching of drugs with their corresponding proteins and targets in the future. By leveraging increasingly sophisticated computational and AI tools, the company seeks to uncover vast and previously unknown biological insights, accelerate the development of therapeutics targeting ‘undruggable’ targets, and drive exponential growth in the early-stage drug pipeline through its platform.”

 

From Active Compounds to Target Identification to Lead Compounds: A Closed Loop


Drug development is one of the most risky, complex, and time-consuming areas of technological research in human advancement. High R&D costs, long development cycles, and low success rates have long been the “three major burdens” weighing on pharmaceutical companies. Global pharmaceutical companies are competing for the same targets, and the fast-follower strategy has led to pipeline homogenization, making the challenges facing the pharmaceutical industry even more severe.

 

Analysis indicates that currently approved drugs worldwide target fewer than 700 protein targets, while more than 4,000 potential human disease targets remain undeveloped (excluding the even larger number of potential RNA targets). Furthermore, the mechanisms of action for numerous drug targets have yet to be elucidated, primarily because existing target discovery and identification technologies lack high-throughput capabilities. For known targets, the screening approaches employed by global pharmaceutical companies are similar, leading to homogeneous drug pipelines and intense patent competition.

 

The original intention behind the establishment of Leadart was to meet the market demand for innovative drug pipelines and novel targets.

 

Dr. Ni Feng, Founder and CEO of Leadart Biotechnology, brings over 15 years of R&D experience in chemistry and biology. After earning his Ph.D. from Xiamen University, Dr. Ni pursued postdoctoral research in the United States and subsequently worked there, engaging in research projects related to biochemistry, medicinal chemistry, and chemical biology. He ultimately decided to focus on in-depth applied research in chemical proteomics technologies.

 

“During those years, the atmosphere for innovation and entrepreneurship in China was extremely vibrant, allowing many Chinese expatriates and scientists in the United States to sense this momentum. Whenever we encountered cutting-edge technologies, we would immediately consider whether they were needed in China and whether there were already robust solutions available internationally,” Ni Feng recounted.

 

“At that time, only a few academic laboratories had the capability to leverage chemical proteomics technologies for drug target identification, with experimental timelines measured in years. Further refinement of these techniques within individual laboratories could require even more time. By integrating diverse resources to continuously optimize this technology, enabling rapid, high-throughput identification of active molecules or novel targets, it would be possible to establish a highly influential new drug enablement platform.”

 

Co-founders and COOs Yan Jie and Ni Feng were undergraduate classmates at Xiamen University. After earning his bachelor’s degree, Yan Jie obtained a master’s degree from Iowa State University in the United States and subsequently joined U.S. pharmaceutical companies, where he engaged in preclinical and clinical-stage small-molecule drug development. During his 14-year R&D career at companies such as Amgen, he accumulated extensive experience. Yan Jie has also been actively involved in organizing events on cutting-edge biotechnologies and entrepreneurship in the Boston area and other regions of the United States. As one of the founders of BioSpark Group, a non-profit organization based in Boston, he is committed to building a collaborative talent network, enhancing the leadership of Chinese professionals in the life sciences sector, and promoting the commercial translation of advanced biotechnologies. In 2019, Yan Jie resigned from Amgen and returned to China to pursue full-time entrepreneurship. He is currently an on-the-job doctoral candidate in the Engineering Doctorate (Eng.D.) program for Innovative Leading Engineers at Tsinghua University.

 

“Having worked in both industry and venture capital-backed philanthropic organizations, Mr. Yan gained an early awareness of the trends shaping the biopharmaceutical sector and the urgent need to improve new drug development success rates through innovative technologies. Leveraging the emerging technologies I encountered in academia, we began exploring potential directions for our startup,” said Ni Feng.

 

In 2017, Leadart was successively established in Los Angeles, USA, and Ningbo, with its R&D headquarters set up in Ningbo. It strategically partnered with Ningbo University to establish an Innovation Center, and collaborated with the College of Science and Technology of Ningbo University to set up an R&D Center, marking the beginning ofEstablishment of a Chemical Proteomics Technology Platform

 

Ni Feng also invited his doctoral supervisor, Academician Zhao Yufen, to join the founding team. An academician of the Chinese Academy of Sciences, Dr. Zhao brings over 30 years of experience in chemical research and drug development, with profound expertise in peptides and pharmaceutical development. She also serves as the Dean of the Institute of New Drug Technology at Ningbo University.

 

In 2020, Professor He Jiaming of Ningbo University also joined Ningbo Leadart Biotechnology Co., Ltd. as a partner. Dr. He has over 20 years of R&D experience in communications, IT, and automation, and was the primary recipient of the Second Prize of the National Science and Technology Progress Award.

 

To date, the company’s technical and engineering teams comprise over 50 professionals. By integrating cutting-edge biochemical and automation technologies, and leveraging its two core platforms for target identification and target screening, it providesFrom active compounds to target screening & identification, and then to the screening and optimization of lead candidate compounds: a closed-loop R&D process.

 

Exclusive Active Molecular Target Probe Library


Leadart possesses drug post-derivatization technology and a proprietary probe molecule library, along with internationally leading target identification biotechnologies that accelerate the discovery of drug molecules and targets. These capabilities are applicable to the development of various therapeutics, including small molecules, protein-targeted degraders, peptides, and challenging-to-drug targets such as protein-protein interactions (PPIs).

 

According to Ni Feng, traditional drug discovery requires three additional steps, typically conducted independently, to obtain a lead compound after disease target validation. First, early active molecules are identified through high-throughput screening technologies such as HTS, DEL, and AI-assisted methods based on known targets. Next, the target engagement of these hits is verified. Finally, the hits are modified and optimized to yield lead drug candidates. This three-step process is not only time-consuming and complex but also does not guarantee smooth progression through each stage.

 

Chemical proteomics matches targets starting from drug molecules, effectively condensing a three-step process into a single step.“DNA sequencing requires primers to facilitate the amplification of DNA signals, whereas chemical proteomics sequencing relies on probes to enrich protein signals. Therefore, weBuilt a proprietary molecular library comprising thousands of probes“, and is continuously expanding. Hit compounds are obtained from known drugs, bioactive natural product molecules, clinical findings, or phenotypic screening, and then optimized into probes for target identification. Probe molecules are used to label their binding proteins for qualitative and quantitative analysis. The structures of the corresponding drug molecules matched to these proteins, along with their binding affinities, are recorded and compiled in a database to achieve data digitization,” introduced Ni Feng.

 

The drug development model based on phenotype + target identification can significantly shorten the drug development cycle, increase the likelihood of clinical success, substantially reduce investment costs, and offers tremendous appeal and potential value.

 

Ni Feng stated, “In the process of transforming chemical molecules into target probes, we performed corresponding chemical modifications, which amounted to pre-structural modification of drug molecules, yielding numerous intermediate analogs. In addition to optimizing these analogs in line with modern medicinal chemistry principles, we can also identify structurally similar molecules based on their structures and compare them with the probes to discover more drug molecules targeting the same target. Although probe synthesis is labor-intensive, it overall represents a transformative improvement in efficiency.”

 

Currently, Ningbo Leadart Biotechnology Co., Ltd. leverages its proteomic “target fishing probe” technology to rapidly screen for novel drug candidates at the proteome level. The company has established collaborations with more than ten pharmaceutical companies, research institutions, and computational & AI-driven drug discovery firms across China, the United States, and South Korea, continuously advancing its drug pipeline development.


Building a Fully Automated Cell Culture–Drug Screening System


According to Ni Feng, chemists and drug developers have, in a sense, already achieved “compound freedom,” whereas researchers in the biological sciences have not yet attained true “cell freedom.”

 

Cells serve as the foundation and primary vehicle for biological research, as well as important mediators and tools in disease treatment. During early-stage research and new drug development, researchers require large quantities of high-quality cells of various types, and must conduct experiments in accordance with the cells’ “growth cycles.” The need for high-quality, highly consistent, and batch-stable cells is self-evident in its importance to new drug development.

 

With advances in data and computational sciences such as AI, Leadart believes that the biopharmaceutical industry will undergo digital and intelligent transformation, just like other sectors. New computational tools will help biopharmaceutical professionals gain a more efficient understanding of the intricacies of human biology.


However, what is scarce in the biopharmaceutical industry is high-quality big data. Statistics show that over 65% of biopharmaceutical literature and even preclinical data are not reproducible. Therefore, Leadart is committed to obtaining high-quality big data from the perspective of chemical proteomics through automated standard processes, and leveraging an increasing array of AI and computational tools to derive novel biological insights into human proteome networks, thereby accelerating drug R&D, reducing development costs, and improving clinical success rates.

 

Leadart has successfully translated laboratory technologies into commercialized technologies, with products from its wholly-owned subsidiary—Fully Automated Cell Culture Workstation for 24/7 Unattended Cell Culture and Remote Control. In addition, Ningbo Leadart Biotechnology Co., Ltd. is developing an automated system for the entire workflow of phenotypic screening and target identification. Within one year, through “human-machine” collaboration, it aims to achieve a gradual 10- to 100-fold increase in efficiency, while eliminating the complexity and errors associated with manual operations and accumulating highly reliable multidimensional big data.

 

LeadArt’s vision is to become an automated, data-driven drug discovery platform that leads the digital transformation of new drug discovery, empowers the innovative pharmaceutical industry, and delivers high-quality, large-scale pipeline supply. The company’s name, LeadArt, combines “Lead,” referring to lead compounds, with “Art,” signifying the pursuit of higher technical standards and more rigorous criteria in molecular evaluation. LeadArt is committed to advancing the front-loading of drug target systems and refined analytical workflows in new drug research and development.

 

To realize its vision, Ningbo Leadart Biotechnology Co., Ltd. is advancing the deployment of automated drug screening systems and the construction of biological databases, with a plan to establish 20–30 internal and external collaborative early-stage drug pipelines within three years.


In the future, Ningbo Leadart Biotechnology Co., Ltd. will leverage automation to build larger-scale databases, establish an automated platform for target identification and big data analytics, explore the uncharted space of over 4,000 human protein targets, and utilize data-driven insights to uncover a more robust pipeline of early-stage drug candidates both internally and externally, thereby becoming a continuous engine for generating high-quality early-stage drug pipelines.