Targeted Molecular Recognition

AngioDesign focuses on the rational design of enhanced, next-generation drugs for proven disease targets and its first target is Angiotensin-Converting Enzyme (ACE). AngioDesign is using 3-D structure-guided design to synthesize a new class of domain-selective ACE inhibitors, alone and in combination with other inhibitors, for cardiovascular and other non-communicable diseases.



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Crystal structure of LisW-S in complex with tACE

N- and C-domains have different substrate affinities

Reversing the adverse effects of Ang and BK

Crystal structure of LisW-S in complex with ACE

Crystal structure of tACE, the equivalent of the C-domain

Surface and ribbon representations

Crystal structure of kAW in complex with tACE

Crystal structure of lisinopril

Targeted molecular recognition

The figure on the left is a cartoon representation showing an overview of the tACE co-crystal structure with lisW-S.
The figure on the right is a stick representation showing lisW-S interactions in the active site: comparison between N- and C- domain residues.

Next-generation innovation combining clinical safety and efficacy

Differentiation – first-in-class dual C-domain/NEP inhibitors with blockbuster potential to treat hypertension and heart failure

AngioDesign has a well-differentiated alternative to existing heart drugs

The combination of a C-domain-selective ACEi plus an NEP inhibitor:

  • Decreases blood pressure and normalises contraction of the blood vessels without influencing vascular permeability and endothelial cell function
  • These features may be beneficial in the treatment of high blood pressure but without the side effects of cough and angioedema associated with the inhibition of NEP and the non-domain-selective inhibition of ACE
  • This combination therapy has important clinical relevance and may be a new approach in the treatment of hypertension and heart failure.