Ternatin is a cyclic heptapeptide first isolated from the mushroom C. versicolor that has been shown to have cytotoxic and anti-adipogenic effects in vitro. It inhibits adipogenesis with an IC50 value of 27 nM and becomes cytotoxic to 3T3-L1 mouse adipocytes at 10-fold higher concentrations. Ternatin is reported to inhibit HCT116 cell proliferation with an IC50 value of 71 nM. Note that this metabolite should not be confused with the plant flavonoid of the same name.
Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effect in spontaneously hypertensive rats and cardioprotective effects. These novel findings will be helpful for developing a new understanding of the RAS, a key regulator of blood pressure and fluid balance. The heptapeptide could serve as a model peptide, e.g. in the development and evaluation of analytical methods.
TLN-232, also known as CAP-232, is a synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells.
WIN 66306 is a cyclic heptapeptide antagonist of neurokinin-1 (NK1) and NK2 receptors originally isolated from A. flavipes. It binds to NK1 and NK2 receptors and inhibits contractions induced by substance P in isolated guinea pig ileum in a concentration-dependent manner.
Angiotensin (1-7) (ASP-ARG-VAL-TYR-ILE-HIS-PRO) 是肾素-血管紧张素系统中的内源性七肽。Angiotensin 1-7在心肌细胞中具有抗炎和抗纤维化活性,因此具有心脏保护作用。它能抑制血管紧张素转换酶和释放一氧化氮,是激肽诱导的血管舒张的局部协同调节剂。它阻断 Ang II 诱导的平滑肌细胞增殖和肥大,并显示对内皮的抗血管生成和生长抑制作用。它显示出抗炎活性。