Structure-Based Identification of Small-Molecule Angiotensin-Converting Enzyme 2 Activators as Novel Antihypertensive Agents

Structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agents.

Angiotensin-converting enzyme 2 (ACE2) is a key renin-angiotensin system enzyme involved in balancing the adverse effects of angiotensin II on the cardiovascular system, and its overexpression by gene transfer is beneficial in cardiovascular disease. Therefore, our objectives were 2-fold: to identify compounds that enhance ACE2 activity using a novel conformation-based rational drug discovery s...

Small molecule glucokinase activators as novel anti-diabetic agents.

The monomeric enzyme GK (glucokinase) has a low affinity for glucose and, quantitatively, is largely expressed in the liver and pancreatic beta-cells, playing a key 'glucose sensing' role to regulate hepatic glucose balance and insulin secretion. Mutations of GK in man can be inactivating, to cause a form of diabetes mellitus, or activating, to lower blood glucose levels. Recently, models of GK...

Inhibitory Effects of Germinal Angiotensin Converting Enzyme by Medicinal Plants Used in Iranian Traditional Medicine as Antihypertensive

Background & Aim: Medicinal plants are used in traditional medicine for the treatment of different diseases such as hypertension. Since inhibition of angiotensin converting enzyme (ACE) is one of the involved mechanisms in control of hypertension, in this study the inhibitory effect of 20 medicinal plants on ACE was investigated. Methods: The medicinal plants were collected, powdered, extracted...

Angiotensin Converting Enzyme in Sarcoidosis

Structure-based discovery of a novel angiotensin-converting enzyme 2 inhibitor.

Angiotensin-converting enzyme 2 (ACE2) is considered an important therapeutic target for controlling cardiovascular diseases and severe acute respiratory syndrome (SARS) outbreaks. Recently solved high-resolution crystal structures of the apo-bound and inhibitor-bound forms of ACE2 have provided the basis for a novel molecular docking approach in an attempt to identify ACE2 inhibitors and compo...