The epidermal growth factor receptor as a therapeutic target in glioblastoma multiforme and other malignant neoplasms.

Abstract:

:The epidermal growth factor receptor (EGFR) is dysregulated in various tumour types such as glioblastoma multiforme (GBM), breast cancer, ovarian carcinoma, non-small cell lung cancer and other cancers. As the intracellular tyrosine kinase of the EGFR activates signalling cascades leading to cell proliferation, angiogenesis and inhibition of apoptosis, the EGFR represents an attractive target in cancer therapy. In GBM which is the most common primary central nervous system tumour in adults, the EGFR is overexpressed in about 40 to 50% of cases, and almost half of these co-express the mutant receptor subtype EGFRvIII. This EGFR variant is constitutively activated, and thereby may contribute to the aggressive and refractory course of GBM which is associated with a median survival of only 40 to 60 weeks from diagnosis. Various trials are ongoing focusing on EGFR and EGFRvIII as new therapeutic targets in GBM. Anti-EGFR monoclonal antibodies (MAbs), e.g. cetuximab, and tyrosine kinase inhibitors (TKIs), e.g. erlotinib and gefitinib, are the most advanced in clinical development. Several trials are investigating MAbs or TKIs in combination with other agents such as inhibitors of the mammalian target of rapamycin. Other still preliminary approaches targeting the EGFR are small interfering RNA, antisense RNA and ribozymes, which lead to degradation of EGFR mRNA. Further studies are needed to define their clinical potential, to identify biological predictors of response and thus to characterize subgroups of patients who will benefit from treatment with these new agents.

authors

Loew S,Schmidt U,Unterberg A,Halatsch ME

doi

10.2174/187152009788680019

subject

Has Abstract

pub_date

2009-07-01 00:00:00

pages

703-15

issue

6

eissn

1871-5206

issn

1875-5992

journal_volume

9

pub_type

杂志文章,评审
  • Pro-apoptotic activity of BH3-only proteins and BH3 mimetics: from theory to potential cancer therapy.

    abstract::The evasion of cancer cells from the induction of cell death pathways results in the resistance of tumor to current treatment modalities. Therefore, the resistance to cell death, one of the hallmarks of cancer, is a major target in the development of new approaches to selectively affect cancer cells. The complex inter...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152012802650084

    authors: Hartman ML,Czyz M

    更新日期:2012-10-01 00:00:00

  • Design and Discovery of Novel Quinoxaline Derivatives as Dual DNA Intercalators and Topoisomerase II Inhibitors.

    abstract::Backgroun/Methods: In attempt to develop new potent anti-tumor agents, a series of quinoxaline derivatives was designed and synthesized. The novel compounds were tested in vitro for their anti-proliferative activities against HePG-2, MCF-7 and HCT-116 cell lines. Additionally, DNA binding affinities as well as DNA-top...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520617666170710182405

    authors: Eissa IH,El-Naggar AM,El-Sattar NEAA,Youssef ASA

    更新日期:2018-01-01 00:00:00

  • Encapsulation of Imatinib in Targeted KIT-5 Nanoparticles for Reducing its Cardiotoxicity and Hepatotoxicity.

    abstract:BACKGROUND:Using imatinib, a tyrosine kinase inhibitor drug used in lymphoblastic leukemia, has always had limitations due to its cardiotoxicity and hepatotoxicity side effects. The objective of this study is to develop a target-oriented drug carrier to minimize these adverse effects by the controlled release of the dr...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200619174323

    authors: Varshosaz J,Fardshouraki S,Mirian M,Safaeian L,Jandaghian S,Taymouri S

    更新日期:2020-01-01 00:00:00

  • Synthesis of New Benzimidazole and Benzothiazole Disulfide Metal Complexes as G-quadruplex Binding Ligands.

    abstract::Compounds that can bind and stabilize non-canonical DNA structures are named quadruplex and are of interest in anticancer drug design due to their selective inhibitions of telomerase and consequent effects on cell proliferation. In this study, we report novel Co/Cu [II] complex compounds as G-quadruplex DNA binding li...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520616666160204111637

    authors: Saour K,Lafta D

    更新日期:2016-01-01 00:00:00

  • Novel molecular anti-colorectalcancer conjugate:chlorambucil-adipic acid dihydrizide-glutamine.

    abstract::Cancer is one of the most fatal diseases in the world and it has been years that finding new drugs and chemotherapeutic techniques with lowest side effects become one of the most important challenging matters needs really hard efforts. Chlorambucil (CBL), an ancient direct-acting alkylating anticancer agent, is common...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113139990132

    authors: Tabasi MA,Amanlou M,Siadat SD,Nourmohammadi Z,Omoomi FD,Ebrahimi SE,Aghasadeghi MR,Rahimi P,Pourhosseini S,Mehravi B,Ardestani MS

    更新日期:2013-11-01 00:00:00

  • miRNAs Modulate the Dichotomy of Cisplatin Resistance or Sensitivity in Breast Cancer: An Update of Therapeutic Implications.

    abstract::Cisplatin has a broad-spectrum antitumor activity and is widely used for the treatment of various malignant tumors. However, acquired or intrinsic resistance of cisplatin is a major problem for patients during the therapy. Recently, it has been reported cancer stem cell (CSC)-derived drug resistance is a great challen...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200903145939

    authors: Safi A,Bastami M,Delghir S,Ilkhani K,Seif F,Alivand MR

    更新日期:2020-09-03 00:00:00

  • Potential Molecular Targeted Therapeutics: Role of PI3-K/Akt/mTOR Inhibition in Cancer.

    abstract::Primary liver cancer is one of the most commonly occurring cancers worldwide. Hepatocellular carcinoma (HCC) represents the majority of primary liver cancer and is the 3rd most common cause of cancer-related deaths globally. Survival rates of patients with HCC are dependent upon early detection as concomitant liver dy...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520615666150716104408

    authors: Sokolowski KM,Koprowski S,Kunnimalaiyaan S,Balamurugan M,Gamblin TC,Kunnimalaiyaan M

    更新日期:2016-01-01 00:00:00

  • Latest Evidence on the Role of Multiparametric Magnetic Resonance Imaging in Active Surveillance for Insignificant Prostate Cancer: A Systematic Review.

    abstract:OBJECTIVE:Multiparametric Magnetic Resonance Imaging (mpMRI) has become a very useful tool in the management of PCa. Particularly, there is a great interest in using mpMRI for men on Active Surveillance (AS) for low risk PCa. The aim of this systematic review was to critically review the latest literature concerning th...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520618666180105105413

    authors: Cantiello F,Manno S,Russo GI,Cimino S,Privitera S,Morgia G,Cicione A,Damiano R

    更新日期:2018-01-01 00:00:00

  • Virtual Screening of Natural Products to Select Compounds with Potential Anticancer Activity.

    abstract::Cancer is the main cause of death, so the search for active agents to be used in the therapy of this disease, is necessary. According to studies conducted, substances derived from natural products have shown to be promising in this endeavor. To these researches, one can associate with the aid of computational chemistr...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520618666181119110934

    authors: Cavalcanti ÉBVS,Félix MB,Scotti L,Scotti MT

    更新日期:2019-01-01 00:00:00

  • Drug targeting strategies for photodynamic therapy.

    abstract::In human pathologies, therapeutic treatments are often limited by the lack of selectivity of drugs and their elevated effective concentrations. Targeting these agents to a defined tissue could enhance their selectivity and then diminish their side effects when compared to drugs that accumulate in the entire body. Targ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152012800617830

    authors: Schmitt F,Juillerat-Jeanneret L

    更新日期:2012-06-01 00:00:00

  • Dinuclear berenil-platinum (II) complexes as modulators of apoptosis in human MCF-7 and MDA-MB231 breast cancer cells.

    abstract::The metabolism of alkylating agents is accompanied by the generation of reactive oxygen species. The aim of this study was to treat estrogen receptor-positive and estrogen receptor-negative human breast cancer cells, MCF-7 and MDA-MB-231, respectively, with cisplatin and five different berenil-platinum (II) complexes,...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520614666140623120809

    authors: Agnieszka G,Ewa A,Anna B,Krzysztof B,Monika C,Elżbieta S

    更新日期:2014-01-01 00:00:00

  • Combination of DC Vaccine and Conventional Chemotherapeutics.

    abstract::Recently mutual interactions of chemotherapy and immunotherapy have been widely accepted, and several synergistic mechanisms have been elucidated as well. Although much attention has focused on the combination of DC vaccine and chemotherapy, there are still many problems remaining to be resolved, including the optimal...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520615666150907094139

    authors: Dong W,Wei R,Shen H,Ni Y,Meng L,Du J

    更新日期:2016-01-01 00:00:00

  • Antileukemic Properties of Sesquiterpene Lactones: A Systematic Review.

    abstract::This review summarizes the reported molecular mechanisms underlying the antileukemic property of Sesquiterpene Lactones (SLs). This systematic review was registered in the PROSPERO database and conducted following the PRISMA Statements. The MeSH terms, Sesquiterpenes, Lactones and Leukemia were used in four databases ...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520617666170918130126

    authors: da Silva Castro E,Alves Antunes LA,Revoredo Lobo JF,Ratcliffe NA,Borges RM,Rocha L,Burth P,Fonte Amorim LM

    更新日期:2018-01-01 00:00:00

  • A Comparison of the Inhibitory Effects of Anti-Cancer Drugs on Thioredoxin Reductase and Glutathione S-Transferase in Rat Liver.

    abstract:BACKGROUND:While Thioredoxin Reductase (TrxR) plays an important role in regulation of the intracellular redox balance and various signalling pathways, Glutathione S-Transferase (GSTs) enzymes belong to the detoxification family that catalyse the conjugation of glutathione with various endogenous and xenobiotic electro...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520618666180910093335

    authors: Ozgencli I,Kilic D,Guller U,Ciftci M,Kufrevioglu OI,Budak H

    更新日期:2018-01-01 00:00:00

  • Combination of Histone Deacetylase Inhibitor with Cu(II) 5,5- diethylbarbiturate Complex Induces Apoptosis in Breast Cancer Stem Cells: A Promising Novel Approach.

    abstract:BACKGROUND:Cancer stem cells (CSC) are subpopulation within the tumor that acts a part in the initiation, progression, recurrence, resistance to drugs and metastasis of cancer. It is well known that epigenetic changes lead to tumor formation in cancer stem cells and show drug resistance. Epigenetic modulators and /or t...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520621666201207090702

    authors: Erkisa M,Aztopal N,Erturk E,Ulukaya E,Yilmaz VT,Ari F

    更新日期:2020-12-06 00:00:00

  • Epidrugs in the Immunotherapy of Cutaneous and Uveal Melanoma.

    abstract::Epigenetic modifications can affect numerous mechanisms used by neoplastic cells to evade immune control. In melanoma epigenetic defects, caused by dysregulations in the expression of genome writers, erasers, or readers, play a significant role in the reduced expression of molecules required for efficient immune recog...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520616666160425110401

    authors: Venza M,Visalli M,Catalano T,Beninati C,Teti D,Venza I

    更新日期:2017-01-01 00:00:00

  • lncRNAs as Potential Targets in Small Cell Lung Cancer: MYC -dependent Regulation.

    abstract:BACKGROUND:Small Cell Lung Cancer (SCLC) is a highly aggressive malignancy. MYC family oncogenes are amplified and overexpressed in 20% of SCLCs, showing that MYC oncogenes and MYC regulated genes are strong candidates as therapeutic targets for SCLC. c-MYC plays a fundamental role in cancer stem cell properties and ma...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200721130700

    authors: Tokgun O,Tokgun PE,Inci K,Akca H

    更新日期:2020-01-01 00:00:00

  • Oxaliplapin and capecitabine (XELOX) based chemotherapy in the treatment of metastatic colorectal cancer: the right choice in elderly patients.

    abstract:PURPOSE:Elderly patients with metastatic colorectal cancer (mCRC) differ from the general population and are underrepresented in clinical trials. We, retrospectively, analyzed the safety and efficacy of XELOX regimen in the treatment of elderly patients affected by mCRC. PATIENTS AND METHODS:One-hundred-eleven consecu...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113136660347

    authors: Berretta M,Aprile G,Nasti G,Urbani M,Bearz A,Lutrino S,Foltran L,Ferrari L,Talamini R,Fiorica F,Lleshi A,Canzonieri V,Lestuzzi C,Borsatti E,Fisichella R,Tirelli U

    更新日期:2013-11-01 00:00:00

  • Oncogenic MicroRNA-27a is a target for genistein in ovarian cancer cells.

    abstract::MicroRNAs (miRNAs) are emerging as important regulators in various pathobiological processes in cancer. Genistein, as a major isoflavonoid isolated from dietary soybean, possesses a wide variety of biological activities particularly in cancer prevention. However, the molecular mechanisms by which genistein elicits its...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/18715206113139990006

    authors: Xu L,Xiang J,Shen J,Zou X,Zhai S,Yin Y,Li P,Wang X,Sun Q

    更新日期:2013-09-01 00:00:00

  • Human Papillomavirus E7 Oncoprotein Promotes Proliferation and Migration through the Transcription Factor E2F1 in Cervical Cancer Cells.

    abstract:BACKGROUND:High-risk human papillomavirus (HR-HPV) persistent infection is the main cause of cervical cancer and its precancerous lesions. A previous study showed that HPV16 and HPV58 infections were the most common infection types in the local region. Some studies also declared that HPV58 E7 variants increased the ris...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666201106085227

    authors: Tian S,Zhang L,Li Y,Cao D,Quan S,Guo Y,Yang X,Yang T

    更新日期:2020-11-05 00:00:00

  • Physiological modulation approaches to improve cancer chemotherapy : a review.

    abstract::The success of anticancer therapy is limited due to the resistance caused by tumor cells to cytotoxic agents, which interfere with the effectiveness of various chemotherapeutic agents. Several mechanisms for decreased effectiveness of anti-cancer drugs have been examined however the most widely studied mechanism is th...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113136660364

    authors: Kumar R,Kaur M,Silakari O

    更新日期:2014-06-01 00:00:00

  • Deoxypodophyllotoxin isolated from Juniperus communis induces apoptosis in breast cancer cells.

    abstract::The study of anticancer properties from natural products has regained popularity as natural molecules provide a high diversity of chemical structures with specific biological and medicinal activity. Based on a documented library of the most common medicinal plants used by the indigenous people of North America, we scr...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520614666140608150448

    authors: Benzina S,Harquail J,Jean S,Beauregard AP,Colquhoun CD,Carroll M,Bos A,Gray CA,Robichaud GA

    更新日期:2015-01-01 00:00:00

  • Therapeutic Monoclonal Antibodies in Clinical Practice against Cancer.

    abstract::The importance of monoclonal antibodies in oncology has increased drastically following the discovery of Milstein and Kohler. Since the first approval of the monoclonal antibody, i.e. Rituximab in 1997 by the FDA, there was a decline in further applications but this number has significantly increased over the last thr...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520620666200703191653

    authors: Kaur N,Goyal A,Sindhu RK

    更新日期:2020-01-01 00:00:00

  • Multiple Pharmacological Properties of a Novel Parthenin Analog P16 as Evident by its Cytostatic and Antiangiogenic Potential Against Pancreatic Adenocarcinoma PANC -1 Cells.

    abstract::Pancreatic ductal adenocarcinoma (PDA) remains one of the deadliest types of cancers. Median survival rate is very poor with the currently available chemotherapeutical regimens. Therefore, discovery of new antineoplastic agents against PDA is one of the focused areas of contemporary research. The present study was und...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1871520615666150824153906

    authors: Goswami A,Shah BA,Batra N,Kumar A,Guru SK,Bhushan S,Malik FA,Joshi A,Singh J

    更新日期:2016-01-01 00:00:00

  • Natural Compounds A Weapon to Ameliorate Breast Cancer Cells: A Review.

    abstract::Breast cancer is the heterogeneous disease and leading cause of death in women, worldwide. It is generally caused by the perturbation of various signaling pathways responsible for cell apoptosis. Due to genetic variability, different signaling pathways are disrupted in different breast cancer patients; so, to overcome...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1871520616666160826150659

    authors: Thakur RS,Ahirwar B

    更新日期:2017-01-01 00:00:00

  • Oncologists' current opinion on the treatment of colon carcinoma.

    abstract::Colorectal cancer is a major global health problem with more than a million new cases diagnosed worldwide in 2005. In the United States, this malignancy is the third most common with 145,000 new cases and the second most lethal with 56,000 deaths in 2005. Unfortunately, preclinical diagnostic screening in the U.S. pop...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152007781668742

    authors: Majer M,Akerley W,Kuwada SK

    更新日期:2007-09-01 00:00:00

  • Sphingolipid modulation: a strategy for cancer therapy.

    abstract::Sphingolipids are membrane lipids that play important roles in the regulation of cell functions and homeostasis. Alterations in their metabolism have been associated with several pathologies. For this reason, therapeutic strategies based on the design of small molecules to restore sphingolipid levels to their physiolo...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152012800228643

    authors: Delgado A,Fabrias G,Bedia C,Casas J,Abad JL

    更新日期:2012-05-01 00:00:00

  • Management of elderly patients with diffuse large B-cell lymphomas.

    abstract::Life expectancy has impressively increased over the past century and the US population over 65 years is rapidly growing, especially those over 80 years. In fact, persons older than 80 years have increased by more than 250% between the years 1960 and 2000, and it is expected that the population aged >75 years will trip...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/18715206113136660363

    authors: Ciancia R,Tirelli U,Ribera J,Spina M

    更新日期:2013-11-01 00:00:00

  • The cytotoxic effect of emetine and CGP-74514A studied with the hollow fiber model and ArrayScan assay in neuroendocrine tumors in vitro.

    abstract::Emetine and CGP-74514A have previously shown antitumor activity in neuroendocrine tumor cell lines. The aim of this study was to investigate the cytotoxic activity of the drugs in a three-dimensional model and to study if the mechanism of the cytotoxic activity was induction of apoptosis. An in vitro hollow fiber mode...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/187152012802650147

    authors: Larsson DE,Hassan SB,Oberg K,Granberg D

    更新日期:2012-09-01 00:00:00

  • Cancer chemoprevention by garlic and its organosulfur compounds-panacea or promise?

    abstract::Of late medicinal plants and functional foods rich in bioactive phytochemicals have received growing attention as potential agents for cancer chemoprevention. Accumulating evidence from epidemiological studies as well as laboratory data supports the anticancer properties of garlic widely used as a medicinal herb and s...

    journal_title:Anti-cancer agents in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/187152008783961879

    authors: Nagini S

    更新日期:2008-04-01 00:00:00