Welcome to HitGen

HitGen Inc.

HitGen has established a drug discovery research platform for small molecules and nucleic acid drugs centered on the design, synthesis and screening of DNA encoded chemical libraries (DELs), fragment-based drug discovery (FBDD) and structure-based drug design (SBDD) technologies.

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HitGen Inc. is a biotech company headquartered in Chengdu, China, with subsidiaries in Cambridge, UK and Houston, USA. It became a publicly listed company in Shanghai Stock Exchange in April 2020 (ticker code 688222.SH).  HitGen has established a drug discovery research platform for small molecules and nucleic acid drug centered on the design, synthesis and screening of DNA encoded chemical libraries (DELs), fragment-based drug discovery (FBDD) and structure-based drug design (SBDD) technologies. HitGen's DELs currently contains more than 1 trillion novel, diverse, drug-like small molecules and macrocyclic compounds. These compounds are members of DELs synthesized from many thousands of distinct chemical scaffolds, designed with tractable chemistry, and have yielded proven results for the discovery of small molecule leads against precedented and unprecedented classes of biological targets.

 

Through its acquisition of Cambridge UK based Vernalis R&D Ltd before the end of 2020, a leader in FBDD/SBDD, HitGen now has a research team of over 500 scientists and offers a full set of research capabilities from recombinant protein expression and purification, structural biology, assay development, screening, DEL synthesis, nucleic acid and small molecule chemical synthesis, computational and medicinal chemistry, biochemistry and biophysics, cell biology, in vivo pharmacology, DMPK, CMC, etc., to enable drug discovery research from target gene to IND filing.

 

HitGen RNA therapeutics R&D platform includes key capabilities such as bioinformatics, organic chemistry and medicinal chemistry,RNA biology, molecular biology and cell biology, translational research and clinical research. The platform not only provides high quality services to support internal and external RNA therapeutics R&D projects, but also carries out siRNA sequence design, siRNA parallel synthesis and chemical modification/conjugation, mRNA and protein knock-down assays in both engineered cell lines and primary cell lines, stability test, off-target assessment, bio-distribution and other relate in vitro/in vivo assays for activity and toxicity study, etc. HitGen has also established its own pipelines in early stages to discover novel RNA therapeutics, aiming for providing new treatment for unmet medical needs in oncology and immunology.

 

HitGen operates a flexible business model, ranging from a single capability-based fee for services (FFS,e.g., protein expression and purification, structural biology, bioinformatics, computational chemistry, medicinal chemistry, nucleic and organic chemistry, analytical chemistry, biophysics, PK, PD, etc.), DEL screening, DEL design, synthesis and characterization, integrated drug discovery projects, risk sharing projects, collaborative ventures to program out-licensing. HitGen has approximately 20 in-house drug discovery programs at different stages of research & development. At present, 4 programs have obtained IND approvals by NMPA and entered into clinical trials. HitGen is collaborating with pharmaceutical, biotech and chemical companies, foundations and research institutes in North America, Europe, Asia, Africa and Australia to enable the discovery and development of novel medicines and agrochemicals.


For more information, please call +86-28-85197385, +1-508-840-9646 or visit www.hitgen.com.

For media inquiries: media@hitgen.com

For investor inquiries: investors@hitgen.com  

For business development: bd@hitgen.com  


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History and Honor

  • 2020
  • 2019
  • 2018
  • 2017
  • 2016
  • 2015
  • 2014
  • 2013
  • 2012

Publications

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Case Studies

  • Novel BRD4 Degrader Discovery using DEL Technology
    DEL selection is an affinity-based approach to recognize compounds interacting with the target, including the compounds modulating target function(s) or simply binding to the protein. The architecture of a DNA Encoded Compound is very similar to proteolysis targeting chimeras (PROTAC) as shown in the following figure. Both DEL compound and PROTAC molecule require covalent linkage of two molecules with known attachment points that have minimal impact to the binding.
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  • Identification of Transferase NAA50 Inhibitors by DEL Selection
    The two isomers of the selected compound DEL951-34-888-1668 were synthesized and tested by SPR in the presence of CoA and AcCoA and biochemical assay. The chiral isomer 4a has been found as a very potent inhibitor with improved MW, Ligand Efficiency, and tPSA. The interaction of compound 4a and NAA50 has been further confirmed by co-crystal structure by Pfizer (pdb code: 6WFN).
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  • FBDD Case Studies
    We have pioneered the use of off-rate screening (ORS) to kinetically sample hit-to-lead chemical space, combining our expertise in cheminformatics, compound library synthesis and use of surface plasmon resonance (SPR), to enable screening of unpurified reaction products. This has been applied to the rapid generation of lead compounds from fragment hits without purification of compound libraries or the use of protein structure (Murray, J. B. et al., J. Med. Chem. 2014).
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