Synthesis and biological activity of ketomethylene pseudopeptide analogs as thrombin inhibitors

Leifeng Cheng; Christopher A. Goodwin; Michael F. Schully; Vijay V. Kakkar; Goran Claeson

doi:10.1021/jm00096a010

Synthesis and biological activity of ketomethylene pseudopeptide analogs as thrombin inhibitors

Journal of Medicinal Chemistry ◽

10.1021/jm00096a010 ◽

1992 ◽

Vol 35 (18) ◽

pp. 3364-3369 ◽

Cited By ~ 35

Author(s):

Leifeng Cheng ◽

Christopher A. Goodwin ◽

Michael F. Schully ◽

Vijay V. Kakkar ◽

Goran Claeson

Keyword(s):

Biological Activity ◽

Thrombin Inhibitors

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Sequence Identification of Bioactive Peptides from Amaranth Seed Proteins (Amaranthus hypochondriacus spp.)

Molecules ◽

10.3390/molecules24173033 ◽

2019 ◽

Vol 24 (17) ◽

pp. 3033 ◽

Cited By ~ 7

Author(s):

Alexis Ayala-Niño ◽

Gabriela Mariana Rodríguez-Serrano ◽

Luis Guillermo González-Olivares ◽

Elizabeth Contreras-López ◽

Patricia Regal-López ◽

...

Keyword(s):

Biological Activity ◽

Bioactive Peptides ◽

Continuous Process ◽

Seed Proteins ◽

Thrombin Inhibitors ◽

Amaranthus Hypochondriacus ◽

Potential Source ◽

Sequence Identification ◽

Amaranth Seed ◽

Bioactive Potential

Amaranthus hypochondriacus spp. is a commonly grown cereal in Latin America, known for its high protein content. The objective of this study was to separate and identify bioactive peptides found in amaranth seeds through enzymatically-assisted hydrolysis using alcalase and flavourzyme. Hydrolysis was carried out for each enzyme separately and compared to two-step continuous process where both enzymes were combined. The biological activity of the resulting three hydrolysates was analyzed, finding, in general, higher bioactive potential of the hydrolysate obtained in a continuous process (combined enzymes). Its fractions were separated by RP-HPLC, and their bioactivity was analyzed. In particular, two fractions showed the highest biological activity as ACE inhibitors with IC50 at 0.158 and 0.134, thrombin inhibitors with IC50 of 167 and 155, and antioxidants in ABTS assay with SC50 at 1.375 and 0.992 mg/L, respectively. Further sequence analysis of the bioactive peptides was carried out using MALDI-TOF, which identified amino acid chains that have not been reported as bioactive so far. Bibliographic survey allowed identification of similarities between peptides reported in amaranth and other proteins. In conclusion, amaranth proteins are a potential source of peptides with multifunctional activity.

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Mannich bases of scutellarein as thrombin-inhibitors: Design, synthesis, biological activity and solubility

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2012.10.015 ◽

2012 ◽

Vol 20 (24) ◽

pp. 6919-6923 ◽

Cited By ~ 33

Author(s):

Nian-Guang Li ◽

Shu-Lin Song ◽

Min-Zhe Shen ◽

Yu-Ping Tang ◽

Zhi-Hao Shi ◽

...

Keyword(s):

Biological Activity ◽

Mannich Bases ◽

Thrombin Inhibitors ◽

Design Synthesis

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Virus-Like Particles in a Human Breast Cancer: Structural Similarity to Previously Reported Particles

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100072332 ◽

1973 ◽

Vol 31 ◽

pp. 378-379

Author(s):

G. Kasnic ◽

S. E. Stewart ◽

C. Urbanski

Keyword(s):

Breast Cancer ◽

Biological Activity ◽

Human Breast Cancer ◽

Osteogenic Sarcoma ◽

Human Tumor ◽

Structural Similarity ◽

Cell Tumor ◽

Human Breast ◽

Human Tumor Cell ◽

Type Particle

We have reported the maturation of an intracisternal A-type particle in murine plasma cell tumor cultures and three human tumor cell cultures (rhabdomyosarcoma, lung adenocarcinoma, and osteogenic sarcoma) after IUDR-DMSO activation. In all of these studies the A-type particle seems to develop into a form with an electron dense nucleoid, presumably mature, which is also intracisternal. A similar intracisternal A-type particle has been described in leukemic guinea pigs. Although no biological activity has yet been demonstrated for these particles, on morphologic grounds, and by the manner in which they develop within the cell, they may represent members of the same family of viruses.

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Effects of Vincristine on Endothelial Microtubules in the Spinal Cord

Proceedings, annual meeting, Electron Microscopy Society of America ◽

10.1017/s0424820100090270 ◽

1976 ◽

Vol 34 ◽

pp. 58-59

Author(s):

John L. Beggs ◽

John D. Waggener ◽

Wanda Miller

Keyword(s):

Spinal Cord ◽

Biological Activity ◽

Horseradish Peroxidase ◽

Transport Mechanism ◽

Vasogenic Edema ◽

Vesicular Transport ◽

Close Proximity

Microtubules (MT) are versatile organelles participating in a wide variety of biological activity. MT involvement in the movement and transport of cytoplasmic components has been well documented. In the course of our study on trauma-induced vasogenic edema in the spinal cord we have concluded that endothelial vesicles contribute to the edema process. Using horseradish peroxidase as a vascular tracer, labeled endothelial vesicles were present in all situations expected if a vesicular transport mechanism was in operation. Frequently,labeled vesicles coalesced to form channels that appeared to traverse the endothelium. The presence of MT in close proximity to labeled vesicles sugg ested that MT may play a role in vesicular activity.

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