10929 Technology Place, Suite B
San Diego, 92127
United States of America, California
Phone: 858 485 9101
Fax: 858 485 9131
Sapient Discovery offers powerful and proven structure-based approach to drug discovery in the identificationn and optimization of leads from protein structures termed, Genes-to-Leads®, combines three technologies the (i) Augmented Homology ModelingTM, (ii) Genes to LeadsTM small molecule lead generation, and (iii) Fragments to LeadsTM for fragment based lead discovery with X-ray crystallography, (iv) X-ray crystallography based determination of the mode of binding such inhibitors/antagonists to protein drug targets.
Augmented Homology ModelingTM: A structural bioinformatics based method to derive highly accurate three-dimensional protein models with proprietary loop building.
Genes to Leads™ Technology A rapid lead generation technology for peptide/non-peptide, small molecule drug leads based upon differential three-dimensional structures derived from the dynamic conformations and intrinsic structural differences between drug targets and anti-targets within weeks.
Fragments to Leads™: Experimental approach to find lead molecule with confirmation of mechanistic binding. Sapient Discovery has over 10,000 (still growing) unique drug-like fragments with enough synthetic handles, that could be used against novel targets for identifying novel, drug-like, small molecule lead molecules and subsequent optimization.
X-ray Crystallography based solving of three-dimensional structures of novel proteins, antibodies, antibody-antigen and protein-small molecule complexes. Cloning, expression, purification, proprietary crystallization methods, structure-determination and refinement have been established at Sapient Discovery. Experienced team in place for using this technique in structure-based drug design and optimization by deriving co-crystal structures of lead compounds.
Lead Optimization with Structural Pharmacogenomics: Sapient Discovery has extensive experience in determining and rank ordering the binding of an inhibitor or drug with its respective target and its associated polymorphisms. Polymorphisms in drug targets arise from mutations that arise due drug exposure and/or genetic variation. Sapient Discovery’s structural pharmacogenomics platform provides a practical way to address the implications of the distribution of polymorphisms by race, gender, and genetic predisposition to disease using which potential new drugs are estimated to work for the largest fraction of the patient population.