Very Late Antigen-4 blocker-BIO 1211



BIO 1211, is a non-covalent, small-molecule, cyclohexanecarboxylic acid base compound, tight-binding inhibitor (Koff =1.4×10-4 s-1, dissociation constant [Kd]= 70 pM) of VLA-4 (Very Late Antigen-4, α4β1), which with a structure of N-[[4-[[[(2-methylphenyl) amino] carbonyl] amino]-phenyl] acetyl]-L-leucyl-La-aspartyl-L-valyl-L-proline. It is a late activator VLA-4 integrin antagonist for the potential treatment of inflammatory conditions. The in vitro inhibitory concentration of 50% (IC50) of BIO 1211 was 1 to 2 nM (34), which is approximately 10-fold more potent than the CS-1 ligand mimic used previously in sheep. VLA-4 inhibitors show anti-inflammatory action by inhibition of binding between adhesion factors and leukocytes, but with no loss of basophil function, and they have the advantage of specificity not seen with existing drugs.

Biological Activity

VLA4 or CD49d/CD29 is a α4β1 integrin with pivotal role in controlling of immune cells migration into inflamed tissue. Two major integrin functions, related to cell adhesion, are usually assigned to VLA4. BIO-1211, an α4β1-selective tight-binding peptide analog selective for activated receptor, inhibits early and late airway responses following antigen exposure in a sheep model of allergic airway disease, and it also reverses established antigen-induced hyper-responsiveness. BIO-1211 can effectively disrupt migration of immune cells and reduce subsequent cerebral cortex inflammation, and it has a short half-live so that it can eliminate from the body in the event of serious side effects upon necessitate termination of therapy. BIO-1211 could be a helpful medicine for blocking trans-endothelium migration of immune cells toward controlling neuro-inflammatory diseases.


BIO-1211 Peptide has been identified as a highly active VLA4 antagonist with good bioavailability in rats, dogs, and monkeys. This compound is a powerful VLA4 antagonist and displays 200-fold selectivity for the activated form of α4β1 (KD = 70 pM; IC50 = 0.004 mM), and it stimulated expression of ligand-induced epitopes on the integrin β1 subunit, a property consistent with occupancy of the receptor's ligand-binding site. In addition, this orally active compound is also selective for α4β1 over a range of other integrins (IC50>100 mM for α1β1, α5β1 and α6β1). In spite of this compound being orally active and can be administrated easily, it is cheaper than its counterpart molecule NTZ (Natalizumab), but there are still no comprehensive reports about the BIO-1211 prophylactic effects on induction of neuro-inflammatory conditions.


1. Nourollah Ramroodi, Masood Khani, Zohre Ganjali, Mohammad Reza Javan, Nima Sanadgol, Roghayeh Khalseh, Hadi Ravan, Ehsan Sanadgol, Mohammad Abdollahi. Prophylactic Effect of BIO-1211 Small-Molecule Antagonist of VLA-4 in the EAE Mouse Model of Multiple Sclerosis. Immunological Investigations, 2015, 44(7): 694-712.

2. Ko-chung Lin, Humayun S. Ateeq, Sherry H. Hsiung, Lillian T. Chong, Craig N. Zimmerman, Alfredo Castro, Wen-cherng Lee, Charles E. Hammond, Sandhya Kalkunte, Ling-Ling Chen, R. Blake Pepinsky, Diane R. Leone, Andrew G. Sprague, William M. Abraham, Alan Gill, Roy R. Lobb, Steven P. Adams. Selective, Tight-Binding Inhibitors of Integrin α4β1 That Inhibit Allergic Airway Responses. J. Med. Chem. 1999, 42, 920-934.

3. Ling Ling Chen, Adrian Whitty, Roy R. Lobb, Steven P. Adams, R. Blake Pepinsky. Multiple Activation States of Integrin α4β1 Detected through Their Different Affinities for a Small Molecule Ligand. J. Biol. Chem., 1999, 274, 13167-13175.

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