The development of VIP–ellipticine conjugates

Moody, Terry W.; Czerwinski, Grzegorz; Tarasova, N.; Moody, Deborah L.; Michejda, Christopher J.

doi:10.1016/j.regpep.2004.03.021

Cited by 16 publications

(13 citation statements)

References 15 publications

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“…Table 2 shows that VIP and PACAP-27 bind with high affinity to SCLC cells with IC 50 values of 10 and 5 nM respectively. In contrast, (NTS 6−11 , VIP 7−28 ; VIPhybrid) [54], (N-stearyl, Nle 17 )VIPhybrid [47] and VIP-LALA-ellipticine (E) [44] bind with moderate affinity to SCLC cells with IC 50 values of 300, 30 and 50 nM, respectively ( Table 2). Ten nM VIP or PACAP increases SCLC colony number to 220 and 380%.…”

Section: Vasoactive Intestinal Peptidementioning

confidence: 99%

Neuropeptides as lung cancer growth factors

Moody¹,

Moreno²,

Jensen³

2015

Peptides

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Section: Vasoactive Intestinal Peptidementioning

confidence: 99%

Neuropeptides as lung cancer growth factors

Moody¹,

Moreno²,

Jensen³

2015

Peptides

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“…The VIP-E conjugates were internalized by cancer cells expressing the VPAC1 receptor and were subsequently metabolized by proteolytic enzymes, leading to the release of ellipticine and cellular cytotoxicity. The VIP-E derivatives exhibited significant cytotoxicity toward breast cancer cells and lung cancer cells in vitro (83,84). Subsequently, Moody et al (85) extended these studies and synthesized VIP-camptothecin (CPT) conjugates that contain a novel carbamate linker with a built-in nucleophile associated releasing group, L2.…”

Section: Targeting Vip Receptor For Cancer Molecular Therapymentioning

confidence: 99%

Vasoactive intestinal peptide receptor-based imaging and treatment of tumors

Tang

Xin

Xie

et al. 2014

International Journal of Oncology

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Vasoactive intestinal peptide receptors (VIPRs) are members of the G-protein-coupled receptor superfamily. These receptors are overexpressed in many common malignant tumors and play a major role in the progression and angiogenesis of a number of malignancies. Therefore, VIPRs may be a valuable target for the molecular imaging of tumors and therapeutic interventions. The specific natural ligand or its analogs can be labeled with a radionuclide and used for tumor receptor imaging, which could be used to visualize VIPR-related surface protein expression in vivo and to monitor the in vivo effects of molecular drugs on tumors. Moreover, the involvement of VIPRs in malignant transformation and angiogenesis renders them potential therapeutic targets for cancer treatment. A variety of VIP antagonists and cytotoxic VIP conjugates have been synthesized and evaluated for VIPR-targeted molecular therapy. The importance of VIPRs in tumor biology and the ability to predict responses to targeted therapy and monitor drug interventions suggest that VIP receptor-based imaging and treatment will be critical for the early diagnosis and management of cancer. Here, we review the current literature regarding VIPRs and their natural ligands and the involvement of VIPRs in tumor growth and angiogenesis, with an emphasis on the present use of VIPRs for the molecular imaging of tumors and therapies targeting VIPRs.

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“…To this end, a vast range of ellipticine derivatives have been prepared and evaluated for potential improvement in cytotoxicity, including ellipticinium salts, [56][57][58][59][60] ellipticine glycosides, [61][62][63] dimers, 64 hybrids [65][66][67][68] and conjugates. [69][70][71][72]…”

Section: Summary Of Biological Activitymentioning

confidence: 99%