99mTc labeled VIP analog: evaluation for imaging colorectal cancer

Rao, P. S.; Thakur, Mathew L.; Pallela, Venkat R.; Patti, Ratnakar; Reddy, K. Krishna; Li, H.; Sharma, S.; Pham, H. L.; Diggles, L.; Minami, C.; Marcus, Carol S.

doi:10.1016/s0969-8051(01)00205-0

Cited by 35 publications

(39 citation statements)

References 25 publications

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“…It is therefore very tempting to suggest the use of growth-inhibiting VIP/PACAP analogs for the treatment of human tumors (16 -22). Moreover, a number of clinical and preclinical studies suggest that VIP/PACAP receptors may be promising molecular targets for tumor imaging and targeted radiotherapy (1,4,6,(23)(24)(25)(26). However, previous and present evidence indicates a highly abundant expression of VIP/PACAP receptors in normal human target tissues.…”

Section: Discussionmentioning

confidence: 76%

“…Several human tumors overexpress receptors for small regulatory peptides, e.g., somatostatin, bombesin, vasoactive intestinal peptide (VIP), or pituitary adenylate cyclase-activating peptide (PACAP), an observation which has led to a number of clinical applications in the diagnosis and treatment of tumors (1)(2)(3)(4)(5)(6). VIP is a 28-amino acid neuropeptide, which is widely distributed throughout the brain and periphery, and which structurally belongs to the glucagon-growth hormone releasing factor-secretin superfamily (7)(8)(9).…”

Section: Introductionmentioning

confidence: 99%

“…First, in vitro binding studies have shown that VIP/PACAP receptors are expressed in the great majority of most frequently occurring human tumors, including breast, ovarian, colon, insulinoma, carcinoid, pancreas, glioblastoma, meningioma, pituitary adenoma, and pheochromocytoma (16 -22). Second, VIP/PACAP receptor-positive intestinal and endocrine tumors can be visualized by in vivo VIP receptor scintigraphy (1,4,6,(23)(24)(25)(26). Third, application of VIP and PACAP analogs modulates tumor growth in animal models (2,3,(27)(28)(29)(30)(31)(32)(33).…”

Section: Introductionmentioning

confidence: 99%

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Immunocytochemical Identification of VPAC1, VPAC2, and PAC1 Receptors in Normal and Neoplastic Human Tissues with Subtype-Specific Antibodies

Schulz

Röcken²,

Mawrin

et al. 2004

Clinical Cancer Research

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Section: Discussionmentioning

confidence: 76%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Immunocytochemical Identification of VPAC1, VPAC2, and PAC1 Receptors in Normal and Neoplastic Human Tissues with Subtype-Specific Antibodies

Schulz

Röcken²,

Mawrin

et al. 2004

Clinical Cancer Research

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“…In cancer patients, 99m Tc-TP3654 displayed rapid tumor uptake and early images of tumors were acquired. 95 These findings indicate the potential of 99m Tc-TP3654 for imaging human tumors expressing VIP receptors, and it is worthy of further study.…”

Section: B Vasoactive Intestinal Peptidesmentioning

confidence: 75%

Peptide‐based radiopharmaceuticals: Future tools for diagnostic imaging of cancers and other diseases

Okarvi

2004

Medicinal Research Reviews

208

116

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Small synthetic receptor-binding peptides are the agents of choice for diagnostic imaging and radiotherapy of cancers due to their favorable pharmacokinetics. Molecular modification techniques permit the synthesis of a variety of bioactive peptides with chelating groups, without compromising biological properties. Various techniques have been developed that allow efficient and site-specific labeling of peptides with clinically useful radionuclides such as (99m)Tc, (123)I, (111)In, and (18)F. Among them, (99m)Tc is the radionuclide of choice because of its excellent chemical and imaging characteristics. Recently, many (99m)Tc-labeled peptides have proven to be useful imaging agents. Beside (99m)Tc-labeled peptides, several peptides radiolabeled with (111)In and (123)I have been prepared and characterized. In addition, (18)F-labeled peptides hold clinical potential due to their ability to quantitatively detect and characterize a variety of human diseases using positron-emission tomography. The availability of this wide range of peptides labeled with different radionuclides offers multiple diagnostic and therapeutic applications. Various receptors are over-expressed in particular tumor types and peptides binding to these receptors can be used to visualize tumor lesions scintigraphically. Thus, radiolabeled peptides have potential use as carriers for the delivery of radionuclides to tumors, infarcts, and infected tissues for diagnostic imaging and radiotherapy. Many radiolabeled peptides are currently under investigation to determine their potential as imaging agents. These peptides are designed mainly for thrombus, tumor, and infection/inflammation imaging. This article presents recent developments in small synthetic peptides for imaging of thrombosis, tumors, and infection/inflammation.

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“…However, [Ala 2,8,9,16,19,24,25 ]VIP (analog 8) had high affinity and potency for both VPAC subtypes and was much more metabolically stable than VIP in cells containing each VPAC subtype. These simplified, metabolically stable analogs should be useful for investigating the role of VPAC 1 in biological and pathological processes, for enhanced imaging of tumors overexpressing VIP receptors using VIP receptor scintigraphy (Virgolini, 1997;Thakur et al, 2000Thakur et al, , 2004Rao et al, 2001;Bhargava et al, 2002) as well as for possible VIP receptordirected antitumor treatment for tumors overexpressing VPACs (Gotthardt et al, 2004;Moody et al, 2004;Ou et al, 2005).…”

Section: Simplified Vip Agonists 379mentioning

confidence: 99%

Development of Simplified Vasoactive Intestinal Peptide Analogs with Receptor Selectivity and Stability for Human Vasoactive Intestinal Peptide/Pituitary Adenylate Cyclase-Activating Polypeptide Receptors

Igarashi

Ito²,

Mantey

et al. 2005

J Pharmacol Exp Ther

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Vasoactive intestinal peptide (VIP) is a widespread neurotransmitter whose physiological and pathophysiological actions are mediated by two receptor classes, VIP/pituitary adenylate cyclase-activating polypeptide (VPAC) 1 and VPAC 2 . VIP is a 28-amino acid peptide that is rapidly degraded and simplified; metabolically stable analogs are needed. In this study, we use information from studies of the VIP pharmacophore for VPAC 1 / VPAC 2 to design nine simplified VIP analogs that could have high affinity and selectivity for each VPAC or that retained high affinity for both VPACs and were metabolically stable. From binding studies of their abilities to directly interact with hVPAC 1

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99mTc labeled VIP analog: evaluation for imaging colorectal cancer

Cited by 35 publications

References 25 publications

Immunocytochemical Identification of VPAC1, VPAC2, and PAC1 Receptors in Normal and Neoplastic Human Tissues with Subtype-Specific Antibodies

Immunocytochemical Identification of VPAC1, VPAC2, and PAC1 Receptors in Normal and Neoplastic Human Tissues with Subtype-Specific Antibodies

Peptide‐based radiopharmaceuticals: Future tools for diagnostic imaging of cancers and other diseases

Development of Simplified Vasoactive Intestinal Peptide Analogs with Receptor Selectivity and Stability for Human Vasoactive Intestinal Peptide/Pituitary Adenylate Cyclase-Activating Polypeptide Receptors

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