KLK2

Kallikrein-1 (KLK1) is a serine protease enzyme encoded by the KLK1 gene in humans. It is a member of the kallikrein subfamily of serine proteases, which are involved in a variety of physiological processes. KLK1 is primarily known for its role in the kinin-kallikrein system, where it is responsible for the cleavage of kininogen to produce bradykinin, a potent vasodilator.

Structure

KLK1 is synthesized as a preproenzyme and undergoes several post-translational modifications to become an active enzyme. The mature enzyme consists of a single polypeptide chain with a molecular weight of approximately 30 kDa. The active site of KLK1 contains the classic serine protease triad: histidine, aspartate, and serine.

Function

KLK1 plays a crucial role in the regulation of blood pressure and electrolyte balance through the production of bradykinin. Bradykinin acts on B2 receptors to induce vasodilation, increase vascular permeability, and stimulate the release of other mediators such as prostaglandins and nitric oxide.

In addition to its role in the kinin-kallikrein system, KLK1 is involved in various other physiological processes, including inflammation, pain, and tissue remodeling. It is expressed in a wide range of tissues, including the kidney, pancreas, and salivary glands.

Clinical Significance

Alterations in KLK1 expression or activity have been implicated in several pathological conditions. For instance, reduced KLK1 activity is associated with hypertension, while increased activity has been observed in certain inflammatory diseases. KLK1 is also being investigated as a potential therapeutic target for conditions such as diabetic nephropathy and cardiovascular disease.

Research and Therapeutic Applications

Research into KLK1 has led to the development of kallikrein inhibitors and bradykinin receptor antagonists as potential therapeutic agents. These compounds are being explored for their ability to modulate the kinin-kallikrein system in diseases characterized by excessive inflammation or abnormal blood pressure regulation.

Also see

• Kallikrein
• Bradykinin
• Serine protease
• Kinin-kallikrein system
• Hypertension