Design, synthesis, and evaluation of Bothrops venom serine protease peptidic inhibitors

Silva, G.M.; Souza, Daniel Henrique Berto De; Waitman, K.B.; Ebram, Matteo Celano; Fessel, Melissa Regina; Zainescu, Iuliu Cezar; Portaro, Fernanda Calheta Vieira; Heras, Montserrat; Andrade, Sofia

doi:10.1590/1678-9199-jvatitd-2020-0066

Cited by 9 publications

(2 citation statements)

References 22 publications

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“…Ongoing efforts to develop alternative therapeutics for the treatment of SBE have targeted the inhibition of major toxic components of snake venom. In this regard, inhibitors of sPLA2, [60–62] SVMPs [63–69] and SVSPs [70,71] have shown varying degrees of promise at protecting against the lethal effects of some medically important snake venoms in preclinical studies. Given that some enzymatically active snake venom toxins are dependent on metal ions as cofactors, small‐molecule metal chelators have also been investigated in the search of novel treatment [72–74] .…”

Section: Toward Novel Small‐molecule Snake Antivenom Therapeuticsmentioning

confidence: 99%

Prospects and Challenges of Developing Plant‐Derived Snake Antivenin Natural Products: A Focus on West Africa

et al. 2021

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Snakebite envenomation (SBE) is an important public health issue that is now receiving renewed attention following its reclassification as a Neglected Tropical Disease (NTD). Most incidences occur in rural areas of resource‐limited countries, as such, timely and appropriate medical care for SBE is often inaccessible. The administration of anti‐snake venom serum (ASV) is the only effective definitive treatment of SBE, but treatment failure to available ASVs is not uncommon. Emerging evidence highlights the potential of small‐molecule compounds as inhibitors against toxins of snake venom. This presents an encouraging prospect to develop an alternative therapeutic option for the treatment SBE, that may be amenable for use at the point of care in resource‐constraint settings. In view of the pivotal role of natural products in modern drug discovery programmes, there is considerable interest in ethno‐pharmacological mining of medicinal plants and plant‐derived medicinal compounds toward developing novel snake venom‐neutralising therapeutics. In this review, we compile a collection of medicinal plants used in the treatment of SBE in West Africa and highlight their promise as potential botanical drugs or as sources of novel small‐molecule compounds for the treatment of SBE. The challenges that must be surmounted to bring this to fruition including the need for (sub) regional collaboration have been discussed.

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Section: Toward Novel Small‐molecule Snake Antivenom Therapeuticsmentioning

confidence: 99%

Prospects and Challenges of Developing Plant‐Derived Snake Antivenin Natural Products: A Focus on West Africa

et al. 2021

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“…In order to investigate human CatD inhibitors for the design and development of tools and agents of scientific and therapeutic interest, snake venoms belonging to the genera Bothrops, Crotalus, and Lachesis have been used as natural sources of biologically active molecules able to act selectively and specifically on different cellular targets [37,38]. Of all the bioactive molecules present in snake venoms, phospholipases A 2 (svPLA 2 ) are among the most frequently encountered and studied [39,40]; these proteins have established physical-chemical properties and a variety of pharmacologic and toxic effects in snakebite envenomation, such as myonecrosis, anticoagulation, platelet aggregation inhibition, neurotoxicity, cardiotoxicity, hypotension and edema formation [41][42][43][44][45].…”

Section: Introductionmentioning

confidence: 99%

New multienzymatic complex formed between human cathepsin D and snake venom phospholipase A2

Moraes

Francisco

Dill

et al. 2022

J. Venom. Anim. Toxins incl. Trop. Dis

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Background: Cathepsin D (CatD) is a lysosomal proteolytic enzyme expressed in almost all tissues and organs. This protease is a multifunctional enzyme responsible for essential biological processes such as cell cycle regulation, differentiation, migration, tissue remodeling, neuronal growth, ovulation, and apoptosis. The overexpression and hypersecretion of CatD have been correlated with cancer aggressiveness and tumor progression, stimulating cancer cell proliferation, fibroblast growth, and angiogenesis. In addition, some studies report its participation in neurodegenerative diseases and inflammatory processes. In this regard, the search for new inhibitors from natural products could be an alternative against the harmful effects of this enzyme. Methods: An investigation was carried out to analyze CatD interaction with snake venom toxins in an attempt to find inhibitory molecules. Interestingly, human CatD shows the ability to bind strongly to snake venom phospholipases A 2 (svPLA 2 ), forming a stable muti-enzymatic complex that maintains the catalytic activity of both CatD and PLA 2 . In addition, this complex remains active even under exposure to the specific

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Snake venom, a potential treatment for melanoma. A systematic review

Bialves

Bastos

Cordeiro

et al. 2023

International Journal of Biological Macromolecules

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Design, synthesis, and evaluation of Bothrops venom serine protease peptidic inhibitors

Cited by 9 publications

References 22 publications

Prospects and Challenges of Developing Plant‐Derived Snake Antivenin Natural Products: A Focus on West Africa

Prospects and Challenges of Developing Plant‐Derived Snake Antivenin Natural Products: A Focus on West Africa

New multienzymatic complex formed between human cathepsin D and snake venom phospholipase A2

Snake venom, a potential treatment for melanoma. A systematic review

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