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Angiogenesis Inhibitors - Europe PMC

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Last Updated: 27 April 2022

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

The compound 29e, which was based on tubulin and zebrafish assays, was found to have noteworthy nanomolar potency against a number of leukaemia cell lines, particularly in K562 cells, where apoptosis was induced, was further investigated under medicinal chemistry conditions. Also, 29e has notably blocked K562 cell proliferation and metastasis in blood vessels and surrounding tissues of the zebrafish xenograft model. 29e may be regarded as an effective anti-angiogenesis and -leukaemia drug candidate, as well as promising physicochemical stability and metabolic stability.

Source link: https://europepmc.org/article/MED/35109719


Cancer combination therapies by angiogenesis inhibitors; a comprehensive review.

Abnormal vaping is one of the most notable features of tumor tissue, largely contributing to tumor immune evasion. Owing to this fact, angiogenesis blockade therapy was developed to combat cancer by limiting the blood and oxygen supply to the malignant cells by impairing the vascular network. Given the predominant role of vascular-endothelium growth factor in the angiogenesis process, the common anti-angiogenic agents are mainly dependent on the targetedness of its actions. Following their administration, cancer cells have mainly demonstrated resistance to anti-angiogenic agents by several pathways, and potentiated local invasiveness and even distant metastasis have been reported.

Source link: https://europepmc.org/article/MED/35392964


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

In patients with melanoma, only little is known about the safety and effectiveness of angiogenesis inhibitor therapy. The aim of this review was to investigate the potential benefits and risks of angiogenesis inhibitor therapy in patients with melanoma. Patients with melanoma were included in randomized controlled trials that investigated the effectiveness and safety of angiogenesis inhibitor therapy in patients with melanoma. No significant difference was found between the treatment groups in OS [HR], 0. 99; 95% confidence interval, 0. 90-1. 09] or PFS]. No significant effect of angiogenesis inhibitor therapy was found on disease control or objective response, nor was there any. In addition, angiogenesis inhibitor therapy raised the risks of hypertension, neurological disease, and diarrhea. Neither significant improvement in OS or PFS in patients with melanoma is made by Angiogenesis inhibitor therapy, nor does it increase the risk of serious adverse events. Therefore, angiogenesis inhibitor therapy is not appropriate for the treatment of melanoma.

Source link: https://europepmc.org/article/MED/35377859


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

After a long-term use of lenvatinib, which reduces vascular endothelial growth factor, we present here a case of drug-induced diffuse hemorrhage, an adverse event in an hepatocellular carcinoma patient treated with a combination of ICIs and angiogenesis inhibitors. Both ICIs and anti-angiogenesis inhibitors cause drug-induced DAH in our case, and their combination can escalate the severity of DAH. Clinicians must be aware that long-term VEGF inhibition may be related to DAH, and should consider the risk management of such adverse events when using this combination therapy.

Source link: https://europepmc.org/article/MED/35449623


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 critical and fascinating scientific topic in the field of malignant tumours. In connection with blood microvessels in cancer cell proliferation, tumor formation, and metastasis, current research importance and concern is being directed. Tyrosine kinases have been widely portrayed as therapeutic agents that can influence tumour formation's angiogenic process. In the current study, we intend to track the developments in the total synthesis of three receptor tyrosine kinase inhibitors. This analysis explores various synthetic routes for these three approved medications that were previously announced as patents. We've also investigated the purification process of these anticancer drugs because the purity of medicines is a significant factor during manufacturing, so we've decided to investigate the purification procedure. It should be noted that the different patents may have described certain manufacturing and purities of desired drug and their intermediates in a different manner.

Source link: https://europepmc.org/article/MED/35235141


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

oleanolic acid, a naturally pentacyclic triterpenoid, inhibited the VEGF/VEGFR2 signaling pathway and angiogenesis in HUVECs, which may be a good VEGF inhibitor. In this paper, a systematic redesign of OA was carried out in order to raise the risk of inhibitory reactions aganist VEGF and anti-angiogenesis potential. As a result, a range of novel OA derivatives, containing a,-unsaturated ketone system in ring A and amide functional group at C-28, were tested for cytotoxicity and ability to reduce VEGF-induced abnormal proliferation of HUVECs. Compared to OA-1 and OA-16, two promising derivatives demonstrated no in vitro cytotoxicity against HUVECs, but showed more potent inhibitory activity against VEGF-induced proliferation and angiogenesis in HUVECs than OA-1. OA-1 and OA-16 inhibited VEGF-induced VEGFR2 transcription, according to the Western blot's findings.

Source link: https://europepmc.org/article/MED/35369968


Clinical efficacy and safety of angiogenesis inhibitors: sex differences and current challenges.

Pharmacological interference with the safeguarding functions of ECs has produced a similar spectrum of adverse effects. An increase in arterial pressure, left ventricular dysfunction that promotes heart disease, thromboembolic events, including pulmonary embolism and stroke, and myocardial infarction are among the most common side effects of VEGF signalling pathway inhibition. This review article explores the current challenges clinicians face when it comes to angiogenesis inhibitor therapy, including the importance of considering sex differences in terms of clinical effectiveness and safety. We also suggest future research considering the role of sex hormone receptors and sex chromosomes. The development of new sex-specific drugs with improved target- and cell-type selectivity may lead to personalized medication for both men and women dependent on anti-angiogenic therapy to reduce adverse effects and enhance therapeutic efficacy.

Source link: https://europepmc.org/article/MED/33739385

* 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