Targeting EGFR Overexpression at the Surface of Colorectal Cancer Cells by Exploiting Amidated BODIPY ‐Peptide Conjugates

AbstractThree BODIPY ‐peptide conjugates designed to target the epidermal growth factor receptor (EGFR) at the extracellular domain were synthesized and their specificity for binding to EGFR was investigated. Peptide sequences containing seven amino acids, GLARLLT (2) and KLARLLT (3), and 13 amino acids, GYHWYGYTPQNVI (4), were conjugated to carboxyl BODIPY dye (1) by amide bond formation in up to 73% yields. The BODIPY ‐peptide conjugates and their “parent” peptides were determined to bind to EGFR experimentally using SPR analysis, and were further investigated using computational methods (AUTODOCK). Results of SPR, competitive binding, and docking studies propose that conjugate6 including the GYHWYGYTPQNVI sequence binds to EGFR more effectively than conjugates5 and7, bearing the smaller peptide sequences. Findings in human carcinoma HEp2 cells overexpressing EGFR showed nontoxic behavior in the presence of activated light (1.5 J/cm2) and in the absence of light for all BODIPYs. Furthermore, conjugate6 showed about 5 ‐fold higher accumulation within HEp2 cells compared with conjugates5 and7, localizing preferentially in the cell ER and lysosomes. Our findings suggest that BODIPY ‐peptide conjugate6 is a promising contrast agent for detection of colorectal cancer and potentially other EGFR over ‐expressing cancers.
Source: Photochemistry and Photobiology - Category: Science Authors: Tags: SPECIAL ISSUE RESEARCH ARTICLE Source Type: research

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Authors: Kim MY Abstract Induction of apoptosis in human cancer cells by Sasa quelpaertensis Nakai has been considered to be a potential therapeutic target for cancer treatment; however, the underlying mechanisms of action are not well understood. The present study investigated the role of nitric oxide (NO•) and inhibitors of apoptosis (IAPs) during apoptosis induced by Sasa quelpaertensis Nakai extracts (SQE) in p53-wild type (WT) and p53-null HCT116 colon carcinoma cells. Trypan blue exclusion and Annexin V/propidium iodide assays were used to test for antiproliferation, and apoptosis and cell cycle. Griess ...
Source: Oncology Letters - Category: Cancer & Oncology Tags: Oncol Lett Source Type: research
o Gangemi The human microbiota is made up of the fungi, bacteria, protozoa and viruses cohabiting within the human body. An altered microbiota can provoke diseases such as cancer. The mechanisms by which a modified microbiota can intervene in the onset and progression of neoplastic diseases are manifold. For instance, these include the effects on the immune system and the onset of obesity. A different mechanism seems to be constituted by the continuous and bidirectional relationships existing between microbiota and miRNAs. MiRNAs emerged as a novel group of small endogenous non-coding RNAs from that control gene expres...
Source: Cancers - Category: Cancer & Oncology Authors: Tags: Review Source Type: research
Conclusion: Our study reveals that miR-206 functions as a tumor metastasis suppressor and sheds new light on the clinical significance of miR-206 in NSCLC therapy. PMID: 32206066 [PubMed - in process]
Source: Cellular and Molecular Biology Letters - Category: Biochemistry Authors: Tags: Cell Mol Biol Lett Source Type: research
AbstractCleavage of the MUC1 glycoprotein yields two subunits, an extracellular alpha-subunit bound to a smaller transmembrane beta-subunit. Monoclonal antibodies (mAbs) directed against the MUC1 alpha –beta junction comprising the SEA domain, a stable cell-surface moiety, were generated. Sequencing of all seven anti-SEA domain mAbs showed that they clustered into four groups and sequences of all groups are presented here. mAb DMB5F3 with picomolar affinity for the MUC1 SEA target was selected f or further evaluation. Immunohistochemical staining of a series of malignancies with DMB5F3 including lung, prostate, breas...
Source: Cancer Immunology, Immunotherapy - Category: Cancer & Oncology Source Type: research
AbstractThis review appraises the current literature on carcinogenic risks in anti-neutrophilic cytoplasmic autoantibody (ANCA) associated vasculitis (AAV). Patients with AAV are often at increased risk of developing non-melanoma skin carcinomas (NMSCs), haematological malignancies, bladder, breast, lung, prostate, and colorectal carcinomas. Reported cancer incidence in these patients ranged from 10 to 26%. Cancer risks at the time of diagnosis of AAV and disease outcomes along the trajectory of AAV that may lead to chronic kidney disease (CKD); dialysis and transplantation are summarized. Inherent carcinogenic risks as pa...
Source: Clinical Rheumatology - Category: Rheumatology Source Type: research
ConclusionsHere, we discuss the role of ErbB4 in normal physiology and in breast, lung, colorectal, gastric, pancreatic, prostate, bladder, and brain cancers, as well as in hepatocellular carcinoma, cholangiocarcinoma, and melanoma. Understanding the role of ErbB4 in cancer is not only important for the treatment of tumors, but also for the treatment of other disorders in which ErbB4 plays a major role, e.g. cardiovascular disease.
Source: Cellular Oncology - Category: Cancer & Oncology Source Type: research
Authors: Votava J, Kachlik D, Hoch J Abstract Total mesorectal excision (TME) was first described 40 years ago by Richard Heald. The purpose of this article is to point out importance of this surgical procedure. Starting from first attempts to surgically cure rectal carcinoma in the 19th century through Miles' operation at the beginning of the 20th century results were not satisfactory due to high number of local recurrences after resections for rectal cancer. Progress in surgical technique and knowledge of anatomy and embryology of the rectum led to development of TME. Principle of TME is surprisingly simple: remo...
Source: Acta Chirurgica Belgica - Category: Surgery Tags: Acta Chir Belg Source Type: research
DR DANIEL ALBO (Augusta, GA): There is a significant shift in the presentation of colorectal cancer in population-based studies. Currently, 3 of 10 rectal cancers are actually diagnosed before the age of 50 years. I noticed that you focused your study on colon cancer patients. Did you notice a significant number of these patients who present with rectal disease as a primary site, in particular, the carcinomatosis data set? Those are known to have an even more aggressive prognostic factor of outcomes.
Source: Journal of the American College of Surgeons - Category: Surgery Tags: Southern surgical association article Source Type: research
Abstract BACKGROUND: Hepatocellular carcinoma (HCC) recurrence and development of de novo malignancy (DNM) after liver transplantation (LT) are the major causes of late recipient death. METHODS: We analyzed the incidence of extrahepatic DNM following living donor LT according to the status of pretransplant hepatic malignancy. We selected 2,076 adult patients who underwent primary LDLT during 7 years from January 2010 to December 2016. RESULTS: The pretransplant hepatic malignancy group (n = 1,012) showed 45 cases (4.4%) of the following extrahepatic DNMs: posttransplant lymphoproliferative disease (PTLD)...
Source: J Korean Med Sci - Category: General Medicine Authors: Tags: J Korean Med Sci Source Type: research
Abstract The response to preoperative chemotherapy is useful for predicting prognosis in unresectable and resectable disease. However, the prognostic benefit of chemotherapy prior to hepatectomy in patients with colorectal carcinoma and resectable or marginally resectable liver metastases remains unclear. The present study investigated the effect of preoperative chemotherapy on the prognosis of patients with colorectal cancer and resectable or marginally resectable synchronous liver metastasis. A total of 106 patients were retrospectively reviewed, who underwent hepatectomy for colorectal metastasis. The prognosis...
Source: Clinical Colorectal Cancer - Category: Cancer & Oncology Authors: Tags: Mol Clin Oncol Source Type: research
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