Protein Tyrosine Kinases (PTKs) and Protein Tyrosine Phosphatases (PTPs) coordinate and regulate the phosphorylation level in the body needed for normal cellular functions like cell growth, adhesion, differentiation, migration, survival, and apoptosis. Perturbations in the finely regulated PTKs and PTPs can lead to abnormal cell signaling, resulting in inflammatory diseases, immune-related conditions, obesity, diabetes, cancer, etc. Thus, PTPs and PTKs make excellent therapeutic targets. Primary or acquired resistance to kinase inhibitors heightens our interest in targeting PTPs to modulate these aberrations that result in disease. Understanding how these PTPs function and how they are regulated is a pivotal step to target them to treat human diseases. This thesis will focus on understanding the functional importance and regulation mechanism of PTPs to target them to treat human diseases.