The progression of malignant melanoma is characterized by overexpression of a number of matrix metalloproteinases (MMPs), especially MMP-2, which play a critical role in the degradation of basement membranes and the extracellular matrix. Consequently, we assessed a drug targeting strategy in which the protease activity of MMP-2 is exploited to release an anticancer agent from a macromolecular c...

Neuropeptide Y (NPY) from the brain of an amphibian from the order Gymnophiona (the caecilian, Typhlonectes natans) was characterized. We cloned a 790 base pair cDNA encoding the caecilian NPY precursor. The open reading frame consisted of 291 bases, indicating an NPY precursor of 97 amino acids. Both deduced and isolated NPY primary structures were Tyr-Pro-Ser-Lys-Pro-Asp-AsnPro-Gly-Glu-Asp-Al...

Collagenase (matrix metalloproteinase 1) cleaves type I, II, and III collagen helices at a specific site between Gly-Ile or Gly-Leu bonds (residues 775 and 776, P1-P1'). To understand the mechanism of collagen processing, mutations around the cleavage site have been introduced into the cloned murine pro alpha 1(I) collagen (Col1a1) gene. These mutant constructs have been transfected into homozy...

Sesame peptide powder (SPP) exhibited angiotensin I-converting enzyme (ACE) inhibitory activity, and significantly and temporarily decreased the systolic blood pressure (SBP) in spontaneously hypertensive rats (SHRs) by a single administration (1 and 10 mg/kg). Six peptide ACE inhibitors were isolated and identified from SPP. The representative peptides, Leu-Val-Tyr, Leu-Gln-Pro and Leu-Lys-Tyr...

The mechanism by which the angiotensin I (AI) converting enzyme inhibitor SQ20,881 (<GluTrp-Pro-Arg-Pro-Gln-Ile-Pro-Pro) blocks the pressor response to exogenous AI was studied in mo in the intact anesthetized dog. When administered as a single dose 250 times that of Injected AI (250 nmoles/kg) into either the pulmonary or systemic circulation, SQ20,881 produced inhibition of pulmonary conversi...

The mechanism by which the angiotensin I (AI) converting enzyme inhibitor SQ20,881 (<GluTrp-Pro-Arg-Pro-Gln-Ile-Pro-Pro) blocks the pressor response to exogenous AI was studied in mo in the intact anesthetized dog. When administered as a single dose 250 times that of Injected AI (250 nmoles/kg) into either the pulmonary or systemic circulation, SQ20,881 produced inhibition of pulmonary conversi...

The mechanism by which the angiotensin I (AI) converting enzyme inhibitor SQ20,881 (<GluTrp-Pro-Arg-Pro-Gln-Ile-Pro-Pro) blocks the pressor response to exogenous AI was studied in mo in the intact anesthetized dog. When administered as a single dose 250 times that of Injected AI (250 nmoles/kg) into either the pulmonary or systemic circulation, SQ20,881 produced inhibition of pulmonary conversi...

The mechanism by which the angiotensin I (AI) converting enzyme inhibitor SQ20,881 (<GluTrp-Pro-Arg-Pro-Gln-Ile-Pro-Pro) blocks the pressor response to exogenous AI was studied in mo in the intact anesthetized dog. When administered as a single dose 250 times that of Injected AI (250 nmoles/kg) into either the pulmonary or systemic circulation, SQ20,881 produced inhibition of pulmonary conversi...

The full primary structure of the very potent opioid peptide dynorphin, from porcine pituitary, has been determined. It is (H)Tyr-Gly-Gly-Phe-Leu-Arg-Arg-Ile-Arg-Pro-Lys-Leu-Lys-Trp-Asp-Asn-Gln(OH). The synthetic peptide with this sequence behaves identically to natural dynorphin in a number of ways, and it has the same potency in the guinea pig ileum myenteric plexus--longitudinal muscle bioas...

Casein kinase II from bovine brain transfers about one mole of phosphate to a serine residue near the COOH terminus of the heavy chain of myosin isolated from bovine brain. We have purified and characterized a peptide that contains this phosphoserine. The peptide was generated by chymotryptic and thermolytic digestion and was isolated by gel filtration, Fe3+ affinity chromatography, and reverse...