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Angiogenesis Inhibitors - PubMed

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Last Updated: 27 April 2022

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Alveolar Hemorrhage Caused by the Combination of Immune Checkpoint Inhibitors (ICIs) and Angiogenesis Inhibitors: The Underlying Long-Term Vascular Endothelial Growth Factor (VEGF) Inhibition.

Here's a case of drug-induced diffuse hemorrhage, an adverse occurrence in a patient with hepatocellular carcinoma treated with a mixture of ICIs and angiogenesis inhibitors after long-term use of lenvatinib, which reduces the vascular endothelial growth factor. Both ICIs and anti-angiogenesis inhibitors result in drug-induced DAH, and their combination can elevate the risk of DAH. Clinicians must be aware that long-term VEGF inhibition may be related to DAH, and that clinicians should consider the risk mitigation of such adverse events when using this combination therapy.

Source link: https://doi.org/10.7759/cureus.23272


Cancer combination therapies by angiogenesis inhibitors; a comprehensive review.

Abnormal vaping is one of the most prominent features of tumor tissue, largely contributing to tumor immune evasion. Angiogenesis blockade therapy was developed to combat cancer by limiting the vascular network in the malignant cells, contributing to this fact. The most important role of a vascular-endothelium growth factor in the angiogenesis process is dependent on the targetedness of its actions. Following their administration, cancer cells have been found to be resistant to anti-angiogenic agents by several pathways, but also potentiated local invasiveness and distant metastasis have been observed.

Source link: https://doi.org/10.1186/s12964-022-00838-y


Efficacy and safety of angiogenesis inhibitors in melanoma: a meta-analysis of seven randomized controlled trials.

Little is known about the safety and efficacy of angiogenesis inhibitor therapy in patients with melanoma. The aim of this research was to determine the risks and risks of angiogenesis inhibitor therapy in patients with melanoma. Patients with melanoma were included in randomized controlled trials that investigated the efficacy and safety of angiogenesis inhibitor therapy in patients with melanoma. No significant effect of angiogenesis inhibitor therapy was found on disease control or objective response, but not so elusive versus objective response. The sample size for analysis of disease control was sufficient, according to TSA's reports. In addition, angiogenesis inhibitor therapy has increased the risk of hypertension, neurological disorders, and diarrhea. Patients with melanoma have no significant improvement in OS or PFS, and notably cause an elevated risk of major adverse events. Angiogenesis inhibitor therapy does not appear to have any significant improvement in OS or PFS in patients with melanoma. Hence, angiogenesis inhibitor therapy is not appropriate for the treatment of melanoma.

Source link: https://doi.org/10.1097/CMR.0000000000000812


Design and semisynthesis of oleanolic acid derivatives as VEGF inhibitors: Inhibition of VEGF-induced proliferation, angiogenesis, and VEGFR2 activation in HUVECs.

Angiogenesis inhibitors targeting the VEGF signaling pathway are being developed into medications for the treatment of vain diseases, such as cancer, rheumatoid arthritis, and age-related macular degeneration. oleanolic acid, a natural pentacyclic triterpenoid, inhibited the VEGF/VEGFR2 signaling pathway and angiogenesis in HUVECs, which may be a good VEGF inhibitor. HUVECs were injected with a cyano-unsaturated ketone system in ring A and amide functional group, respectively, and assessed for cytotoxicity and ability to reduce VEGF-induced abnormal proliferation of HUVECs. Compared to OA-1 and OA-16, two promising derivatives of cytotoxicity against HUVECs were no in vitro cytotoxicity against HUVECs, but OA-1 and OA-16 showed stronger inhibition of VEGF-induced proliferation and angiogenesis in HUVECs, as opposed to OA-16. OA-1 and OA-16 inhibited VEGF-induced VEGFR2 gene expression, according to the Western blot results.

Source link: https://doi.org/10.1016/S1875-5364(22)60159-6


A patent review on efficient strategies for the total synthesis of pazopanib, regorafenib and lenvatinib as novel anti-angiogenesis receptor tyrosine kinase inhibitors for cancer therapy.

Angiogenesis is a vital and interesting scientific topic in the field of malignant tumors. Current research focus and attention are being directed in conjunction with blood microvessels in cancer cell proliferation, tumor formation, and metastasis. Tyrosine kinases have been widely reported as therapeutic goals that influence the angiogenic process in tumour formation. We're in the current review we'll be monitoring the latest developments in the total synthesis of three receptor tyrosine kinase inhibitors. This report explores several synthetic routes for these three approved medications that were previously only available as patents. We have chosen to investigate the purification process of these anticancer drugs as well. The purity of drugs is a very important component during manufacturing, so we've decided to investigate the purification procedure of these anticancer medicines as well. The production of desired drug and their intermediates may have been described by various patents in addition to the above.

Source link: https://doi.org/10.1007/s11030-022-10406-8


Angiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors.

The compound 29e based on tubulin and zebrafish assays demonstrated noteworthily nanomolar potency against a variety of leukaemia cell lines, especially in K562 cells, where apoptosis was induced. The 29e stably binds to the tubulin colchicine site, according to cellular microtubule networks disruption results. The zebrafish xenograft model also dramatically inhibited K562 cell proliferation and metastasis in blood vessels and surrounding tissues.

Source link: https://doi.org/10.1080/14756366.2022.2032688


Discovery of N-(1,3,4-thiadiazol-2-yl)benzamide derivatives containing a 6,7-methoxyquinoline structure as novel EGFR/HER-2 dual-target inhibitors against cancer growth and angiogenesis.

The inhibition effect on healthy breast cells and lung cells was weak, according to CCK-8 and 3D cell viability assays, showing that the target compounds had excellent anti-proliferation ability against breast cancer cells and lung cancer cells, especially against SK-BR-3 cells. In the SK-BR-3 cell xenograft model, notably, but nonetheless, the YH-9could effectively reduce breast cancer growth and angiogenesis with little toxicity. In vitroandin vivoresults, YH-9 was found to have a high drug activity as a dual-target EGFR/HER-2 inhibitor, reducing breast cancer growth and angiogenesis.

Source link: https://doi.org/10.1016/j.bioorg.2021.105469

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions

* Please keep in mind that all text is summarized by machine, we do not bear any responsibility, and you should always check original source before taking any actions