A homogeneous time-resolved fluorescence-based high-throughput screening for discovery of inhibitors of Nef-sdAb19 interaction.


:The human immunodeficiency virus (HIV) protein negative factor (Nef) is important for AIDS pathogenesis. An anti-Nef single-domain antibody (sdAb19) derived from camelids has been previously generated and shown to effectively block the physiological functions of Nef in vitro and in vivo in nef-transgenic mice. However, sdAb19 must be ectopically expressed within the target cell to be able to exert its neutralizing effect on Nef, while the extra-cellular administration method turned out to be ineffective. This might suggest a default of the stability or/and deliverability of sdAb19. The identification of small molecule compounds capable of inhibiting the Nef-sdAb19 interaction and mimicking the neutralizing activity of sdAb19 in vivo would therefore be the means of circumventing the problem encountered with sdAb19. Here we describe the development of a high-throughput screening method combining the homogeneous time-resolved fluorescence (HTRF) and the microscale thermophoresis (MST) techniques for the identification of small-molecule compounds inhibiting the Nef-sdAb19 interaction by binding to Nef protein. Eight small-molecule compounds have been selected for their ability to significantly inhibit the Nef-sdAb19 interaction and to bind to Nef. These molecules could be further assessed for their potential of being the Nef-neutralizing agents in the future.


Int J Oncol


Fan X,Wei J,Xiong H,Liu X,Benichou S,Gao X,Liu L




Has Abstract


2015-10-01 00:00:00












  • Cyclooxygenase-2 promotes tumor lymphangiogenesis and lymph node metastasis in oral squamous cell carcinoma.

    abstract::Oral squamous cell carcinoma (OSCC) is the sixth most common cancer and frequently metastasizes to the cervical lymph nodes, leading to poor survival of patients with OSCC. However, the mechanism of lymph node metastasis is not fully understood. To clarify the molecular mechanism un...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Morita Y,Hata K,Nakanishi M,Nishisho T,Yura Y,Yoneda T

    更新日期:2012-09-01 00:00:00

  • Patched 2, located in 1p32-34, is not mutated in high stage neuroblastoma tumors.

    abstract::Neuroblastoma is a childhood malignancy originating from cells of the sympathetic nervous system, exhibiting a marked diversity in outcome, with spontaneous regression at one end of the spectrum and severe disease and death at the other end. Features associated with frequent recurrence, a poor prognosis, and high tumo...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Jögi A,Abel F,Sjöberg RM,Toftgård R,Zaphiropoulos PG,Påhlman S,Martinsson T,Axelson H

    更新日期:2000-05-01 00:00:00

  • Sulforaphane and its metabolite mediate growth arrest and apoptosis in human prostate cancer cells.

    abstract::The relation between the consumption of cruciferous vegetables and reduced prostate cancer occurrence has been documented, although the responsible phytochemicals are unknown. The effects of sulforaphane (SFN) which occurs as the precursor glucosinolate in broccoli and other cruciferous vegetables, and its metabolite ...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Chiao JW,Chung FL,Kancherla R,Ahmed T,Mittelman A,Conaway CC

    更新日期:2002-03-01 00:00:00

  • Kinase inhibitor screening identifies CDK4 as a potential therapeutic target for melanoma.

    abstract::Despite recent advances in targeted therapies and immunotherapies metastatic melanoma remains only rarely curable. The objective of the present study was to identify novel therapeutic targets for metastatic melanoma. A library of 160 well-characterised and potent protein kinase inhibitors was screened in the BRAF muta...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Mahgoub T,Eustace AJ,Collins DM,Walsh N,O'Donovan N,Crown J

    更新日期:2015-09-01 00:00:00

  • Adherens junctions associated protein 1 serves as a predictor of recurrence of squamous cell carcinoma of the esophagus.

    abstract::Esophageal squamous cell carcinoma (ESCC), the most common esophageal cancer in East Asia, is among the six cancers with the highest fatality rates worldwide. Unfortunately, multidisciplinary treatment strategies have not achieved satisfactory outcomes. Therefore, novel insights into the molecular biology of ESCC are ...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Tanaka H,Kanda M,Koike M,Iwata N,Shimizu D,Ezaka K,Sueoka S,Tanaka Y,Takami H,Hashimoto R,Tanaka C,Yamada S,Fujii T,Nakayama G,Sugimoto H,Fujiwara M,Kodera Y

    更新日期:2015-11-01 00:00:00

  • Bioinformatic analysis of chemokine (C-C motif) ligand 21 and SPARC-like protein 1 revealing their associations with drug resistance in ovarian cancer.

    abstract::Chemokine (C-C motif) ligand 21 (CCL21) and SPARC-like protein 1 (SPARCL1/MAST9/hevin/SC-1) are associated with various biological behavior in the development of cancers. Although the expression of CCL21 and SPARCL1 is downregulated in many solid tumors, their roles in ovarian cancer and their associations with drug r...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Yin F,Liu X,Li D,Wang Q,Zhang W,Li L

    更新日期:2013-04-01 00:00:00

  • Transcriptome analysis of hepatitis B virus-associated small hepatocellular carcinoma by serial analysis of gene expression.

    abstract::Serial analysis of gene expression (SAGE) is a sequence-based tool that enables quantitative study of comprehensive gene expression profiles. In this study, we generated a SAGE library of hepatitis B virus (HBV)-associated small hepatocellular carcinoma (HCC) and compared it with libraries of normal liver and other or...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Kim JW,Lee SH,Park YS,Jeong SH,Kim N,Lee DH,Lee HS

    更新日期:2009-07-01 00:00:00

  • Pathways regulating the expression of the immunomodulatory protein glycodelin in non‑small cell lung cancer.

    abstract::Glycodelin [gene name, progesterone associated endometrial protein (PAEP)] was initially described as an immune system modulator in reproduction. Today, it is also known to be expressed in several types of cancer, including non‑small cell lung cancer (NSCLC). In this cancer type, the feasibility of its usage as a foll...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Weber R,Meister M,Muley T,Thomas M,Sültmann H,Warth A,Winter H,Herth FJF,Schneider MA

    更新日期:2019-02-01 00:00:00

  • microRNA expression profile in undifferentiated gastric cancer.

    abstract::Prognosis of patients with undifferentiated gastric cancer is generally poor. The expression of various microRNAs (miRNAs) has not been comprehensively investigated in undifferentiated gastric cancer. Total RNA was extracted from the specimens of 42 undifferentiated gastric cancer tissues and paired normal gastric tis...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Katada T,Ishiguro H,Kuwabara Y,Kimura M,Mitui A,Mori Y,Ogawa R,Harata K,Fujii Y

    更新日期:2009-02-01 00:00:00

  • Overcoming the classical multidrug resistance phenotype by adenoviral delivery of anti-MDR1 short hairpin RNAs and ribozymes.

    abstract::Simultaneous resistance of cancer cells to multiple cytotoxic drugs, multidrug resistance (MDR), is the major limitation to the successful chemotherapeutic treatment of disseminated neoplasms. The 'classical' MDR phenotype is conferred by MDR1/P-glycoprotein (MDR1/P-gp) that is expressed in almost 50% of human cancers...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Kaszubiak A,Holm PS,Lage H

    更新日期:2007-08-01 00:00:00

  • Metformin increases sensitivity of osteosarcoma stem cells to cisplatin by inhibiting expression of PKM2.

    abstract::Multiple drug resistance is reported to be a major obstacle in treatment of osteosarcoma (OS). Research has demonstrated that small subsets of cells called cancer stem cells (CSCs) are responsible for multiple drug resistance. CSCs are potential targets for reversing chemoresistance. In the present study, we compared ...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Shang D,Wu J,Guo L,Xu Y,Liu L,Lu J

    更新日期:2017-05-01 00:00:00

  • Amplification of telomeric DNA directly correlates with metastatic potential of human and murine cancers of various histological origin.

    abstract::Telomeres, repeated DNA sequences (T2AG3)n that guard the ends of chromosomes, serve as a checkpoint for cell-cycle progression and regulate cell senescence and apoptosis. Loss of the telomeric repeats promotes genomic instability, which is the hallmark of most cancer cells. Whether this loss differs among tumor cells...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Multani AS,Ozen M,Sen S,Mandal AK,Price JE,Fan D,Radinsky R,Ali-Osman F,Von Eschenbach AC,Fidler IJ,Pathak S

    更新日期:1999-09-01 00:00:00

  • Phase II study of induction chemotherapy followed by concomitant chemoradiotherapy in advanced head and neck cancer: clinical outcome, toxicity and organ/function preservation.

    abstract::The purpose of the study was to assess response rate, clinical outcome, organ/function preservation and toxicity in head and neck cancer patients treated with induction chemotherapy followed by concomitant chemoradiotherapy and, when necessary, limited surgery. The study design was a phase II non-randomized trial in h...

    journal_title:International journal of oncology

    pub_type: 临床试验,杂志文章


    authors: Mantovani G,Maccio A,Massa E,Mulas C,Mudu MC,Massidda S,Massa D,Murgia V,Ferreli L,Succu G,Astara G,Proto E,Tore G,Mura M,Maxia G

    更新日期:2000-06-01 00:00:00

  • Treatment of hepatocellular carcinoma and the exacerbation of liver function.

    abstract::We performed interventional treatments on 50 patients with hepatocellular carcinoma (HCC) and analyzed the relationship between these treatments and the exacerbation of liver function after treatment. The different treatments included transcatheter arterial embolization (TAE), percutaneous ethanol injection therapy (P...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Okano H,Shiraki K,Inoue H,Deguchi M,Sugimoto K,Sakai T,Ohmori S,Murata K,Nakano T,Yamakado K,Takeda K

    更新日期:2001-12-01 00:00:00

  • Histone deacetylase inhibitor scriptaid induces cell cycle arrest and epigenetic change in colon cancer cells.

    abstract::Histone deacetylase inhibitors (HDACIs) are involved in cell growth, apoptosis and differentiation. This study aimed to investigate the effects of HDACI scriptaid on histone modification, demethylation, cell growth, cell cycle and apoptosis in the RKO colorectal cancer cell line and screening for scriptaid-induced gen...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Lee EJ,Lee BB,Kim SJ,Park YD,Park J,Kim DH

    更新日期:2008-10-01 00:00:00

  • Expression of prostaglandin E2 receptors in oral squamous cell carcinomas and growth inhibitory effects of an EP3 selective antagonist, ONO-AE3-240.

    abstract::Prostaglandin E2 (PGE2) can stimulate tumor progression by both direct and indirect mechanisms. However, its influence on cell proliferation is still unclear. The present study characterized expression of subtypes of PGE2 receptors in oral squamous cell carcinomas, while also investigating the effects of EP3 and EP4 s...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Hoshikawa H,Goto R,Mori T,Mitani T,Mori N

    更新日期:2009-03-01 00:00:00

  • Multidrug resistance mediated by overexpression of P-glycoprotein in human osteosarcoma in vivo.

    abstract::We examined the expression levels of P-glycoprotein (P-Gp)/the human multidrug resistance gene (MDR1) and in vivo chemosensitivity in the 7 osteosarcoma xenografts. Three of seven (43%) osteosarcoma xenografts expressed MDR1 by reverse transcriptase-polymerase chain reaction (RT-PCR). The OSS-516R xenograft selected w...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Suto R,Abe Y,Nakamura M,Ohnishi Y,Yoshimura M,Lee YH,Imanishi T,Yamazaki H,Kijima H,Tokunaga T,Oshika Y,Hiraoka N,Tamaoki N,Fukuda H,Ueyama Y

    更新日期:1998-02-01 00:00:00

  • Oligoclonal expansion of cd8+ T-lymphocytes in cultured peripheral lymphocytes derived from asymptomatic HTLV-I carriers.

    abstract::Peripheral blood mononulear cells (PBMC) derived from 10 asymptomatic human T lymphotropic virus type I (HTLV-I) carriers were cultured for a short term (10-14 days) in the absence of exogenous antigens. In 5 carriers, when compared with 5 HTLV-I non-carriers an apparent increase in the proportion of CD8+ DR+ cells wa...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Yang H,Furukawa K,Shinzato O,Kamihira S,Moji K,Takemoto T,Shiku H

    更新日期:1994-08-01 00:00:00

  • Enhancement of the effect of 5-aminolevulinic acid-based photodynamic therapy by simultaneous hyperthermia.

    abstract::In the present study, we have investigated a combination of photodynamic therapy (PDT) using 5-aminolevulinic acid (ALA) and simultaneous hyperthermia (HT) on osteosarcoma (HOSM-1) cells, squamous cell carcinoma (KB) cells and fibroblasts (HF), including an assessment of the differences in the sensitivity of these cel...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Yanase S,Nomura J,Matsumura Y,Nagai K,Kinoshita M,Nakanishi H,Ohnishi Y,Tokuda T,Tagawa T

    更新日期:2005-07-01 00:00:00

  • Transcriptomic study of dormant gastrointestinal cancer stem cells.

    abstract::We previously discovered the coexistence of dormant and proliferating cancer stem cells (CSCs) in gastrointestinal cancer, which leads to chemoradiation resistance. CD13-/CD90+ proliferating liver CSCs are sensitive to chemotherapy, and CD13+/CD90- dormant CSCs have a limited prolif...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Nishikawa S,Dewi DL,Ishii H,Konno M,Haraguchi N,Kano Y,Fukusumi T,Ohta K,Noguchi Y,Ozaki M,Sakai D,Satoh T,Doki Y,Mori M

    更新日期:2012-09-01 00:00:00

  • Interleukin-4 inhibits lak and initial phase til activity via interleukin-2 receptor.

    abstract::In the present study, we analyzed the proliferation and cytotoxic activities of LAK cells and initial phase TILs by stimulation with IL-4. IL-4 obviously inhibited the DNA synthesis of LAK cells and initial phase TILs at the concentration of 250 pg/ml and 25 pg/ml, respectively. Furthermore, IL-4 (25 ng/ml for LAK cel...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Tsunoda T,Tanimura H,Yamaue H,Iwahashi M,Tani M,Tamai M,Noguchi K,Mizobata S,Arii K

    更新日期:1995-11-01 00:00:00

  • Selective uveal melanoma inhibition with calcium channel blockade.

    abstract::Uveal malignant melanoma (UMM), the most common primary adult intraocular tumor with a marked metastatic potential, is genetically unique and has unfortunately had few treatment breakthroughs. In this study, we subjected a UMM cell line to high‑throughput library screening with 1,018 FDA‑approved compounds to identify...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Shaughnessy M,Lamuraglia G,Klebanov N,Ji Z,Rajadurai A,Kumar R,Flaherty K,Tsao H

    更新日期:2019-11-01 00:00:00

  • Tetramethypyrazine inhibits renal cell carcinoma cells through inhibition of NKG2D signaling pathways.

    abstract::Tetramethypyrazine (TMP), one of the active compounds extracted from the traditional Chinese medicinal herb (Chuanxiong), has been verified as an anticancer compound against several types of cancer. However, understanding of the molecular mechanisms have not been fully elucidated. In the present study, the anticancer ...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Luan Y,Liu J,Liu X,Xue X,Kong F,Sun C,Wang J,Liu L,Jia H

    更新日期:2016-10-01 00:00:00

  • Establishment and characterization of a novel cell line (cc‑006cpm8) of moderately/poorly differentiated colorectal adenocarcinoma derived from a primary tumor of a patient.

    abstract::In the present study, the cc‑006cpm8 novel colon cell line was established from a sample of right colorectal adenocarcinoma obtained from a woman with liver metastasis. It was possible to culture this cell line for ≥100 passages in vitro with vigorous growth. Morphologically, the cells grew as several layers with tigh...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Chu X,Xue Y,Huo X,Wei J,Chen Y,Han R,Chen H,Su X,Zhang H,Gong Y,Chen J

    更新日期:2019-07-01 00:00:00

  • Establishment of combined immuno-chemotherapy with systemically administered gemcitabine and intra-portal administration of interleukin-2 in murine models of liver metastases of pancreatic cancer.

    abstract::Despite attempts to use multiple drug combinations that include gemcitabine (GEM), there is very little evidence that these combination regimens are superior to the single use of this agent. We therefore investigated the suppressive effect of the combination of systemically administered GEM and locally administered in...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Ito Y,Aiura K,Ueda M,Kitajima M,Kitagawa Y

    更新日期:2008-07-01 00:00:00

  • Epidermal growth factor-stimulated human cervical cancer cell growth is associated with EGFR and cyclin D1 activation, independent of COX-2 expression levels.

    abstract::Cervical cancer constitutes the second most common cancer in women. It is evident from earlier studies that epidermal growth factor (EGF) is a mitogen, in that it mimics the function of estrogen by mediating cross-talk with other oncoproteins. Although epidermal growth factor recept...

    journal_title:International journal of oncology

    pub_type: 杂志文章,收录出版


    authors: Narayanan R,Kim HN,Narayanan NK,Nargi D,Narayanan B

    更新日期:2012-01-01 00:00:00

  • A murine model of hepatitis B-associated hepatocellular carcinoma generated by adeno-associated virus-mediated gene delivery.

    abstract::A relevant animal model is critical for investigating the pathogenic mechanisms underlying hepatitis B virus (HBV)-induced hepatocellular carcinoma (HCC). Mice are not naturally infected by HBV, presumably due to the lack of HBV receptors on mouse hepatocytes. To bypass this entry step of HBV infection, we report gene...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Huang YH,Fang CC,Tsuneyama K,Chou HY,Pan WY,Shih YM,Wu PY,Chen Y,Leung PS,Gershwin ME,Tao MH

    更新日期:2011-12-01 00:00:00

  • Narrow band imaging hysteroscopy: a comparative study using randomized video images.

    abstract::Narrow band imaging (NBI) has been used in the gastrointestinal endoscopy field as a novel endoscopic imaging technique and has contributed to improved qualitative diagnosis and detection of lesions. However, there are only a few studies of use of NBI in the gynecology field. We applied NBI in flexible hysteroscopy at...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Kisu I,Banno K,Kobayashi Y,Ono A,Masuda K,Ueki A,Nomura H,Hirasawa A,Abe T,Kouyama K,Susumu N,Aoki D

    更新日期:2011-11-01 00:00:00

  • Translational implication of Kallmann syndrome-1 gene expression in hepatocellular carcinoma.

    abstract::Accumulation of epigenetic alterations causes inactivation of tumor suppressors and contributes to the initiation and progression of hepatocellular carcinoma (HCC). Identification of methylated genes is necessary to improve our understanding of the pathogenesis of HCC and develop novel biomarkers and therapeutic targe...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Tanaka Y,Kanda M,Sugimoto H,Shimizu D,Sueoka S,Takami H,Ezaka K,Hashimoto R,Okamura Y,Iwata N,Tanaka C,Yamada S,Fujii T,Nakayama G,Koike M,Nomoto S,Fujiwara M,Kodera Y

    更新日期:2015-01-01 00:00:00

  • Analysis of cytokine gene expression in squamous cell carcinoma of the head and neck.

    abstract::Cytokine production in squamous cell carcinoma (SCC) of the head and neck may directly influence the clinical behavior of this aggressive neoplasm since cytokines act as autocrine/paracrine growth factors, as well as immunomodulators. In the present study, the cytokine profiles of 16 SCCs of the head and neck and matc...

    journal_title:International journal of oncology

    pub_type: 杂志文章


    authors: Sabourin C,Wang Q,Mallery S,Nicholson R,Gopalakrishnan R,Lang J,Schuller D,Stoner G

    更新日期:1996-01-01 00:00:00