Bradykinin potentiating peptides (BPPs) from Bothrops jararaca venom were first described in the middle of 1960s and were the first natural inhibitors of the angiotensin-converting enzyme (ACE). BPPs present a classical motif and can be recognized by their typical pyroglutamyl (Pyr)/proline rich sequences presenting, invariably, a proline residue at the C-terminus. In the present study, we describe the isolation and biological characterization of a novel BPP isolated from the skin secretion of the Brazilian tree-frog Phyllomedusa hypochondrialis. This new BPP, named Phypo Xa presents the sequence Pyr-Phe-Arg-Pro-Ser-Tyr-Gln-Ile-Pro-Pro and is able to potentiate bradykinin activities in vivo and in vitro, as well as efficiently and competitively inhibit ACE. This is the first canonical BPP (i.e. Pyr-Aaa(n)-Gln-Ile-Pro-Pro) to be found not only in the frog skin but also in any other natural source other than the snake venoms.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.peptides.2006.10.002DOI Listing

Publication Analysis

Top Keywords

characterization novel
8
bradykinin potentiating
8
skin secretion
8
phyllomedusa hypochondrialis
8
isolation characterization
4
novel bradykinin
4
potentiating peptide
4
bpp
4
peptide bpp
4
bpp skin
4

Similar Publications

Background: Although novel treatments for Alzheimer's disease (AD) have begun to show modest therapeutic effects, agents that target hallmark AD pathology and offer neuroprotection are desired. Erythropoietin (EPO) is a glycoprotein hormone with neuroprotective effects but is faced with challenges including limited brain uptake and increased hematopoietic side effects with long-term dosing. Therefore, EPO has been modified and bound to a chimeric transferrin receptor monoclonal antibody (cTfRMAb); the latter shuttles EPO past the blood-brain barrier (BBB) into brain parenchyma and reduces its plasma exposure and potential for side effects.

View Article and Find Full Text PDF

Drug Development.

Alzheimers Dement

December 2024

Biosplice Therapeutics, Inc., San Diego, CA, USA.

Background: DYRK1A overexpression, common in neurodegenerative diseases like Alzheimer's (AD), contributes to neurofibrillary tangles via Tau protein hyperphosphorylation and amyloid plaque formation, key AD hallmarks. Therefore, DYRK1A has been regarded as a novel target for neurodegenerative diseases. However, developing DYRK1A selective inhibitors has been a difficult challenge due to the highly conserved ATP-binding site of protein kinases, particularly among the CMGC family.

View Article and Find Full Text PDF

Drug Development.

Alzheimers Dement

December 2024

Sharp Therapeutics, Pittsburgh, PA, USA.

Background: Progranulin (GRN) plays a critical role in familial frontotemporal dementia (fFTD), where GRN haploinsufficiency leads to reduction in PGRN levels in the brain, resulting in degeneration of neurons in the frontal lobe of brain responsible for personality, language, and behavior. FTD is the most common dementia in people under 60. Sortilin (Sort1), expressed by neurons, endocytoses, and delivers PGRN rapidly to lysosomes for degradation.

View Article and Find Full Text PDF

Drug Development.

Alzheimers Dement

December 2024

Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.

Background: The present study recapitulates the potency of the novel synthesized piperazine-benzoquinone derivative as a lead molecule selectively targeting AChE along with the antioxidative potential for the management of cognitive decline in Alzheimer's disease.

Method: Novel piperazine-benzoquinone derivative was synthesized implementing appropriate synthetic procedures and was characterized by various spectral and elemental techniques. The purity of this synthetic analogue was ascertained by TLC, melting point determination and elemental analyses.

View Article and Find Full Text PDF

Drug Development.

Alzheimers Dement

December 2024

Rush University Medical Center, Chicago, IL, USA.

Background: Alzheimer's disease is the most dreaded multifactorial neurological illness for which there is currently no known treatment. Although the exact cause of AD is still unknown, several factors related to lifestyle, genetics, and environment are known to have a significant role in the disease's development. Alzheimer's disease is characterized by neuronal loss, neurofibrillary tangles, and senile plaques.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!