Heparin Analogues: A New Family of Anticancer Drugs

Corliss, Julie

doi:10.1093/jnci/81.18.1346

Cited by 3 publications

(3 citation statements)

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“…The PDGF A‐chain contains an amino acid sequence that specifically binds to heparin, causing inactivation of the growth factor 217. In a discussion at a meeting218 it was reported that suramin, a heparin analogue, antagonizes tumor growth factors such as PDGF by interacting with positively charged heparin‐binding sites of the growth factors.…”

Section: Platelet‐derived Growth Factormentioning

confidence: 99%

Actions of heparin that may affect the malignant process

Engelberg¹

1999

Cancer

118

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BACKGROUND Heparin has many actions that may affect the malignant process, especially metastasis. METHODS The author conducted an extensive review of the available medical literature about heparin activity that may apply to important factors involved in the malignant process. RESULTS Thrombin is generated by tumors, and the resultant fibrin formation impedes natural killer cell activity. Microthrombi arrest tumor cells in capillaries. Heparin prevents the formation of thrombin and neutralizes its activity. Angiogenesis has an important role in metastasis; heparin minimizes angiogenesis via the inhibition of vascular endothelial growth factor, tissue factor, and platelet activating factor. It decreases tumor cell adhesion to vascular endothelium as it inhibits selectin and chemokine actions, and it also decreases the replication and activity of some oncogenic viruses. Matrix metalloproteinases, serine proteases, and heparanases have an important role in metastasis. Heparin decreases their activation and limits their effects. It competitively inhibits tumor cell attachment to heparan sulfate proteoglycans. It blocks the oncogenic action of ornithine decarboxylase and enhances the antineoplastic effect of transforming growth factor‐β. Heparin inhibits activator protein‐1, which is the nuclear target of many oncogenic signal transduction pathways, and it potently inhibits casein kinase II, which has carcinogenic activity. Platelet‐derived growth factor, which has oncogenic effects, is also inhibited by heparin, as are reverse transcriptase, telomerase, and topoisomerase prooncogenic actions. CONCLUSIONS These various heparin actions justify clinical investigation of its possible beneficial effect on malignant disease. Cancer 1999;85:257–72. © 1999 American Cancer Society.

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Section: Platelet‐derived Growth Factormentioning

confidence: 99%

Actions of heparin that may affect the malignant process

Engelberg¹

1999

Cancer

118

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“…Structurally, heparin is a highly sulfated glycosaminoglycan, and suramin is a polysulfonated naphthylurea. In the 1980s, the term “heparin-like structure” of suramin was proposed [ 26 ]. Regarding the structural and physiologic properties of the negatively charged polymers, suramin is assumed to be a heparin-related analog or heparinoid [ 26 – 28 ].…”

Section: Introductionmentioning

confidence: 99%

“…In the 1980s, the term “heparin-like structure” of suramin was proposed [ 26 ]. Regarding the structural and physiologic properties of the negatively charged polymers, suramin is assumed to be a heparin-related analog or heparinoid [ 26 – 28 ]. Due to their polyanionic properties, both heparin and suramin may interact with a variety of proteins and molecules [ 29 , 30 ].…”

Section: Introductionmentioning

confidence: 99%

Suramin, an antiparasitic drug, stimulates adipocyte differentiation and promotes adipogenesis

Li,

Dong,

Han

et al. 2023

Lipids Health Dis

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Background Previous studies demonstrated that mast cells with their degranulated component heparin are the major endogenous factors that stimulate preadipocyte differentiation and promote fascial adipogenesis, and this effect is related to the structure of heparin. Regarding the structural and physiological properties of the negatively charged polymers, hexasulfonated suramin, a centuries-old medicine that is still used for treating African trypanosomiasis and onchocerciasis, is assumed to be a heparin-related analog or heparinoid. This investigation aims to elucidate the influence of suramin on the adipogenesis. Methods To assess the influence exerted by suramin on adipogenic differentiation of primary white adipocytes in rats, this exploration was conducted both in vitro and in vivo. Moreover, it was attempted to explore the role played by the sulfonic acid groups present in suramin in mediating this adipogenic process. Results Suramin demonstrated a dose- and time-dependent propensity to stimulate the adipogenic differentiation of rat preadipocytes isolated from the superficial fascia tissue and from adult adipose tissue. This stimulation was concomitant with a notable upregulation in expression levels of pivotal adipogenic factors as the adipocyte differentiation process unfolded. Intraperitoneal injection of suramin into rats slightly increased adipogenesis in the superficial fascia and in the epididymal and inguinal fat depots. PPADS, NF023, and NF449 are suramin analogs respectively containing 2, 6, and 8 sulfonic acid groups, among which the last two moderately promoted lipid droplet formation and adipocyte differentiation. The number and position of sulfonate groups may be related to the adipogenic effect of suramin. Conclusions Suramin emerges as a noteworthy pharmaceutical agent with the unique capability to significantly induce adipocyte differentiation, thereby fostering adipogenesis.

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Review : Synthetic Polymers with Intrinsic Anticancer Activity

Seymour

1991

Journal of Bioactive and Compatible Polymers

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Heparin Analogues: A New Family of Anticancer Drugs

Cited by 3 publications

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Actions of heparin that may affect the malignant process

Actions of heparin that may affect the malignant process

Suramin, an antiparasitic drug, stimulates adipocyte differentiation and promotes adipogenesis

Review : Synthetic Polymers with Intrinsic Anticancer Activity

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