ADC Development Services Targeting EphA2

Creative Biolabs is a leading provider of comprehensive and high-quality ADCs development services. We offer a variety of antibody-drug conjugation solutions along with other related services like antibody production and drug or linker-payload synthesis services. Now we provide ADC design and construction service targeting the EphA2 biomarker for the treatment of solid tumors. We hope to partner with you to explore new frontiers in therapeutic agents and accelerate your novel drug discovery.

Introduction of EphA2

EphA2 is a glycoprotein receptor encoded by the EPHA2 gene. It is a member of the Eph family that is the largest family of receptor tyrosine kinases (RTK). EphA2 is composed of an extracellular region, an epidermal growth factor-like motif, two fibronectin type-III domains and a cytoplasmic region. EphA2 interacts with its ligands to form the EphA2-Ephrin complexes and induces a bidirectional signaling into both Eph-expressing cells and Ephrin-expressing cells. Besides, EphA2 can also trigger a signaling via forming EphA2-EphA2 homodimers and oligomers without ligands. Ephrin-EphA2 complexes have been found involved in a variety of downstream signaling pathways such as the RAS/MAPK, PI3K/AKT/mTOR and so on. EphA2 also plays a role in the malignant transformation of normal cells, angiogenesis, and metastasis in cancers. Thus, EphA2 is considered as a potential target in the cancer therapy.

EphrinA and progranulin signal through the EphA2 receptor. Fig.1 EphrinA and progranulin signal through the EphA2 receptor. (Chitramuthu, 2016)

Anti-EphA2 ADC in Solid Tumors

The overexpression of EphA2 in solid tumors such as the endometrial cancers has made the protein become a good target in the ADC development. For example, MEDI-547, a new ADC composed of a fully human monoclonal antibody targeting the EphA2 conjugated to the tubulin polymerization inhibitor monomethyl auristatin F (MMAF) through a stable maleimidocaproyl (mc) linker.

Preclinical studies showed that MEDI-547 has significant antitumor activity in orthotopic xenograft tumor models without obvious toxicity. Once MEDI-547 is internalized by the EphA2-positive cells, it releases the payload and results in cytotoxicity. Furthermore, MEDI-547 displays effective therapeutic activity in orthotopic animal models on tumor cells. Thus, MEDI-547 may be a promising therapeutic option for the treatment of solid tumors. So far, the ADC is assessed in the clinical phase I.

Structure of MEDI-547. Fig.2 Structure of MEDI-547. (Xiao, 2013)

What Can We Do for You?

Creative Biolabs is specialized in the custom preparation of ADCs, providing a confidential and efficient service at competitive prices. Every step of ADCs development is subject to Creative Biolabs’ stringent quality control. If you are interested in our services, please contact us for more information. Our ADCs development services include:

References

  1. Chitramuthu, B.; Bateman, A. Progranulin and the receptor tyrosine kinase EphA2, partners in crime?. J Cell Biol. 2016, 215(5): 603-605.
  2. Xiao, Z.; et al. EphA2 immunoconjugate. Antibody-Drug Conjugates and Immunotoxins (241-253). 2013.

For lab research use only, not for any in vivo human use.


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