Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri

Scarborough, R. M.; Rose, Jack W.; Hsu, Mei‐Ling; Phillips, David R.; Fried, Victor A.; Campbell, A M; Nannizzi, L; Charo, Israel F.

doi:10.1016/s0021-9258(18)92826-7

Cited by 361 publications

(58 citation statements)

References 31 publications

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“…Echistatin, isolated in 1988, is a glycoprotein (GP) IIb/IIIa receptor antagonist leading to effective inhibition of fibrinogen-induced platelet aggregation. 21 - 25 Furthermore, Scarborough et al 26 screened 62 snake venoms, leading to the discovery of barbourin from the pygmy rattle snake, Sistrurus miliarius , that specifically inhibited GP IIb/IIIa receptors. These findings ultimately led to the synthesis of eptifibatide ( Table 1 ), a highly effective antiplatelet drug.…”

Section: Clinically Approved Venom-derived Drugsmentioning

confidence: 99%

Therapeutic Potential of Peptides Derived from Animal Venoms: Current Views and Emerging Drugs for Diabetes

Coulter-Parkhill

McClean

Gault

et al. 2021

Clin Med Insights Endocrinol Diabetes

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The therapeutic potential of venom-derived drugs is evident today. Currently, several significant drugs are FDA approved for human use that descend directly from animal venom products, with others having undergone, or progressing through, clinical trials. In addition, there is growing awareness of the important cosmeceutical application of venom-derived products. The success of venom-derived compounds is linked to their increased bioactivity, specificity and stability when compared to synthetically engineered compounds. This review highlights advancements in venom-derived compounds for the treatment of diabetes and related disorders. Exendin-4, originating from the saliva of Gila monster lizard, represents proof-of-concept for this drug discovery pathway in diabetes. More recent evidence emphasises the potential of venom-derived compounds from bees, cone snails, sea anemones, scorpions, snakes and spiders to effectively manage glycaemic control. Such compounds could represent exciting exploitable scaffolds for future drug discovery in diabetes, as well as providing tools to allow for a better understanding of cell signalling pathways linked to insulin secretion and metabolism.

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Section: Clinically Approved Venom-derived Drugsmentioning

confidence: 99%

Therapeutic Potential of Peptides Derived from Animal Venoms: Current Views and Emerging Drugs for Diabetes

Coulter-Parkhill

McClean

Gault

et al. 2021

Clin Med Insights Endocrinol Diabetes

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“…A 10-residue segment of this protein shows 90% homology with a portion of trigramin sequence and that it inhibits fibrinogen-dependent platelet aggregation in a similar way to trigramin [58]. Barbourin, a novel disulfide-rich disintegrin from the venom of the ground rattlesnake (Sistrurus miliarius barbourin), is highly homologous to other snake venom disintegrins, except that it contains the KDG (Lys-Gly-Asp) rather than the RDG recognition motif [59]. These disintegrin peptides have been described as highly potent and selective GPIIb-IIIa antagonists that can be used as antiplatelet agents [60].…”

Section: Disintegrinsmentioning

confidence: 99%

Snake Venom Components: Tools and Cures to Target Cardiovascular Diseases

et al. 2021

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Cardiovascular diseases (CVDs) are considered as a major cause of death worldwide. Therefore, identifying and developing therapeutic strategies to treat and reduce the prevalence of CVDs is a major medical challenge. Several drugs used for the treatment of CVDs, such as captopril, emerged from natural products, namely snake venoms. These venoms are complex mixtures of bioactive molecules, which, among other physiological networks, target the cardiovascular system, leading to them being considered in the development and design of new drugs. In this review, we describe some snake venom molecules targeting the cardiovascular system such as phospholipase A2 (PLA2), natriuretic peptides (NPs), bradykinin-potentiating peptides (BPPs), cysteine-rich secretory proteins (CRISPs), disintegrins, fibrinolytic enzymes, and three-finger toxins (3FTXs). In addition, their molecular targets, and mechanisms of action—vasorelaxation, inhibition of platelet aggregation, cardioprotective activities—are discussed. The dissection of their biological effects at the molecular scale give insights for the development of future snake venom-derived drugs.

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“…The desert vipers of the genera Pseudocerastes and Eristicophis (Viperidae: Viperinae) are an understudied clade. The limited research devoted to characterising their venoms has described haemolysis and oedema [7], inhibition of platelet aggregation [8,9] and procoagulant activity [10,11] by E. macmahonii venom, and anticoagulant and haemorrhagic activity [12], platelet aggregation [13] and cytotoxicity [14] by P. persicus venom. Only one study to date has described the venom of P. urarachnoides, which is a potent procoagulant by activating both factor X and prothrombin [11].…”

Section: Introductionmentioning

confidence: 99%

Pharmacological Characterisation of Pseudocerastes and Eristicophis Viper Venoms Reveal Anticancer (Melanoma) Properties and a Potentially Novel Mode of Fibrinogenolysis

Brouw

Ghezellou

Casewell

et al. 2021

IJMS

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Venoms are a rich source of potential lead compounds for drug discovery, and descriptive studies of venom form the first phase of the biodiscovery process. In this study, we investigated the pharmacological potential of crude Pseudocerastes and Eristicophis snake venoms in haematological disorders and cancer treatment. We assessed their antithrombotic potential using fibrinogen thromboelastography, fibrinogen gels with and without protease inhibitors, and colourimetric fibrinolysis assays. These assays indicated that the anticoagulant properties of the venoms are likely induced by the hydrolysis of phospholipids and by selective fibrinogenolysis. Furthermore, while most fibrinogenolysis occurred by the direct activity of snake venom metalloproteases and serine proteases, modest evidence indicated that fibrinogenolytic activity may also be mediated by selective venom phospholipases and an inhibitory venom-derived serine protease. We also found that the Pseudocerastes venoms significantly reduced the viability of human melanoma (MM96L) cells by more than 80%, while it had almost no effect on the healthy neonatal foreskin fibroblasts (NFF) as determined by viability assays. The bioactive properties of these venoms suggest that they contain a number of toxins suitable for downstream pharmacological development as candidates for antithrombotic or anticancer agents.

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Barbourin. A GPIIb-IIIa-specific integrin antagonist from the venom of Sistrurus m. barbouri

Cited by 361 publications

References 31 publications

Therapeutic Potential of Peptides Derived from Animal Venoms: Current Views and Emerging Drugs for Diabetes

Therapeutic Potential of Peptides Derived from Animal Venoms: Current Views and Emerging Drugs for Diabetes

Snake Venom Components: Tools and Cures to Target Cardiovascular Diseases

Pharmacological Characterisation of Pseudocerastes and Eristicophis Viper Venoms Reveal Anticancer (Melanoma) Properties and a Potentially Novel Mode of Fibrinogenolysis

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