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PHARMACUTICAL RESEARCH PROCESS - Coggle Diagram
PHARMACUTICAL RESEARCH PROCESS
TARGET IDENTIFICATION
begins with
identifying the function of a possible therapeutic target
and its role in the disease
genomics and proteomics
we are interested in druggable targets
TARGET ➡︎
an endogenous macromolecule with physiological function that, in a pathological state, alters its function and causes/develops a disease state
TARGET VALIDATION
shows that a molecular target is directly involved in a disease process, and that modulation of the target is likely to have a therapeutic effect
validate ad much as possible the target-disease connection
instrument for that:
chemical genetics
HIT DISCOVERY
HIT
➡︎
compound that which has the desired activity in a compound screen
goal: identify molecules that interact with the drug target
HTS ASSAY
➝ interaction between a molecule and the validated target POSITIVE or NEGATIVE
Features:
Relevance
-Reproducibility
MIniaturization
LEAD OPTIMIZATION
AIM:
refine several of the most promising 'hits' to create more potent and selective candidates with optimized pharmacokinetics properties
SAR
ADME
Selectivity
Efficacy and toxicity