Academic literature on the topic 'HIV fusion inhibitor'

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Journal articles on the topic "HIV fusion inhibitor"

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Tremblay, Cécile L., Françoise Giguel, Christopher Kollmann, et al. "Anti-Human Immunodeficiency Virus Interactions of SCH-C (SCH 351125), a CCR5 Antagonist, with Other Antiretroviral Agents In Vitro." Antimicrobial Agents and Chemotherapy 46, no. 5 (2002): 1336–39. http://dx.doi.org/10.1128/aac.46.5.1336-1339.2002.

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ABSTRACT SCH-C (SCH 351125) is a small-molecule antagonist of the human immunodeficiency virus type 1(HIV-1) coreceptor CCR5. It has in vitro activity against R5 viruses with 50% inhibitory concentrations ranging from 1.0 to 30.9 nM. We have studied anti-HIV-1 interactions of SCH-C with other antiretroviral agents in vitro. Synergistic interactions were seen with nucleoside reverse transcriptase inhibitors (zidovudine and lamivudine), nonnucleoside reverse transcriptase inhibitors (efavirenz), and protease inhibitors (indinavir) at all inhibitory concentrations evaluated. We have also studied
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Xu, Wei, Zhe Cong, Qianyu Duan, et al. "A Protein-Based, Long-Acting HIV-1 Fusion Inhibitor with an Improved Pharmacokinetic Profile." Pharmaceuticals 15, no. 4 (2022): 424. http://dx.doi.org/10.3390/ph15040424.

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Recently, a series of highly effective peptide- or protein-based HIV fusion inhibitors have been identified. However, due to their short half-life, their clinical application is limited. Therefore, the development of long-acting HIV fusion inhibitors is urgently needed. Here, we designed and constructed a protein-based, long-acting HIV fusion inhibitor, termed FLT (FN3-L35-T1144), consisting of a monobody, FN3, which contains an albumin-binding domain (ABD), a 35-mer linker (L35), and a peptide-based HIV fusion inhibitor, T1144. We found that FLT bound, via its FN3 component, with human serum
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Descalzi-Montoya, Dante, Jihong Dai, Sukhwinder Singh, and Patricia Fitzgerald-Bocarsly. "Human plasmacytoid dendritic cells and myeloid Dendritic cells fuse with chronically HIV-infected T cells (168.23)." Journal of Immunology 188, no. 1_Supplement (2012): 168.23. http://dx.doi.org/10.4049/jimmunol.188.supp.168.23.

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Abstract Our laboratory has previously shown that plasmacytoid dendritic cells (pDC) fuse with chronically-HIV infected H9 T cells and also with acutely infected CD4+ primary T cells; a process mediated by virus/CD4 and CXCR4 interactions. In the present study, using the Amnis ImageStream, we observed that fusions can also form between chronically-HIV infected H9 T cells and myeloid dendritic cells (mDC). MDC showed a tendency to form more fusions than pDC. Although the fusion of mDC with HIV-infected H9 T cells was prevented by the CXCR4 inhibitor AMD3100, it was not affected by the CCR5 inhi
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Balzarini, J., and E. De Clercq. "The Thiocarboxanilides UC-10 and UC-781 Have an Additive Inhibitory Effect against Human Immunodeficiency Virus Type 1 Reverse Transcriptase and Replication in Cell Culture When Combined with other Antiretroviral Drugs." Antiviral Chemistry and Chemotherapy 8, no. 3 (1997): 197–204. http://dx.doi.org/10.1177/095632029700800303.

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The thiocarboxanilides represent a structural class of potent and selective human immunodeficiency virus type 1 (HIV-1)-specific reverse transcriptase (RT) inhibitors. Combinations of the clinical candidate thiocarboxanilides UC-10 (oxime ether derivative) and UC-781 (pentenyloxy ether derivative) with a variety of nucleoside RT inhibitors (NRTIs) and non-nucleoside RT inhibitors (NNRTIs), two HIV protease inhibitors and one fusion/uncoating inhibitor were evaluated for their inhibitory effects on HIV-1 RT activity and HIV-1 replication in CEM cell cultures. The inhibitory activity of the NNRT
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BAO, JU, JIN F. LIU, XIAO HE, and JOHN Z. H. ZHANG. "COMPUTATIONAL STUDY OF HIV-1 gp41 NHR TRIMER: INHIBITION MECHANISMS OF N-SUBSTITUTED PYRROLE DERIVATIVES AND FRAGMENT-BASED VIRTUAL SCREENING." Journal of Theoretical and Computational Chemistry 12, no. 08 (2013): 1341001. http://dx.doi.org/10.1142/s0219633613410010.

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Fusion of HIV-1 viral and host cellular membranes is an important step for HIV infection. The HIV-1 envelope glycoprotein mediating the membrane fusion consists of subunits gp120 and gp41 whereas gp120 recognizes the cell-surface receptors and gp41 promotes viral-cell membrane fusion. The trimeric helical complex composed of heterodimer of N-terminal and C-terminal extraviral segments has been used for the gp41 function study, and the trimeric N-terminal teptad repeat (NHR) is considered as an antiviral drug target for developing HIV-1 membrane fusion inhibitors. By using computational solvent
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Su, Yang, Huihiui Chong, Shengwen Xiong, Yuanyuan Qiao, Zonglin Qiu, and Yuxian He. "Genetic Pathway of HIV-1 Resistance to Novel Fusion Inhibitors Targeting the Gp41 Pocket." Journal of Virology 89, no. 24 (2015): 12467–79. http://dx.doi.org/10.1128/jvi.01741-15.

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ABSTRACTThe peptide drug enfuvirtide (T20) is the only HIV-1 fusion inhibitor in clinical use, but it easily induces drug resistance, calling for new strategies for developing effective drugs. On the basis of the M-T hook structure, we recently developed highly potent short-peptide HIV-1 fusion inhibitors (MTSC22 and HP23), which mainly target the conserved gp41 pocket and possess high genetic barriers to resistance. Here, we focused on the selection and characterization of HIV-1 escape mutants of MTSC22, which revealed new resistance pathways and mechanisms. Two mutations (E49K and L57R) loca
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Naito, Takeshi, Kazuki Izumi, Eiichi Kodama та ін. "SC29EK, a Peptide Fusion Inhibitor with Enhanced α-Helicity, Inhibits Replication of Human Immunodeficiency Virus Type 1 Mutants Resistant to Enfuvirtide". Antimicrobial Agents and Chemotherapy 53, № 3 (2008): 1013–18. http://dx.doi.org/10.1128/aac.01211-08.

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ABSTRACT Peptides derived from the α-helical domains of human immunodeficiency virus (HIV) type 1 (HIV-1) gp41 inhibit HIV-1 fusion to the cell membrane. Enfuvirtide (T-20) is a peptide-based drug that targets the step of HIV fusion, and as such, it effectively suppresses the replication of HIV-1 strains that are either wild type or resistant to multiple reverse transcriptase and/or protease inhibitors. However, HIV-1 variants with T-20 resistance have emerged; therefore, the development of new and potent inhibitors is urgently needed. We have developed a novel HIV fusion inhibitor, SC34EK, wh
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Osborne, Newton G. "Enfuvirtide: The First HIV Fusion Inhibitor." Journal of Gynecologic Surgery 20, no. 3 (2004): 103–4. http://dx.doi.org/10.1089/gyn.2004.20.103.

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Lazzarin, Adriano. "Enfuvirtide: the first HIV fusion inhibitor." Expert Opinion on Pharmacotherapy 6, no. 3 (2005): 453–64. http://dx.doi.org/10.1517/14656566.6.3.453.

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Das, Debananda, Kenji Maeda, Yasuhiro Hayashi, et al. "Insights into the Mechanism of Inhibition of CXCR4: Identification of Piperidinylethanamine Analogs as Anti-HIV-1 Inhibitors." Antimicrobial Agents and Chemotherapy 59, no. 4 (2015): 1895–904. http://dx.doi.org/10.1128/aac.04654-14.

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ABSTRACTThe cellular entry of HIV-1 into CD4+T cells requires ordered interactions of HIV-1 envelope glycoprotein with C-X-C chemokine receptor type 4 (CXCR4) receptors. However, such interactions, which should be critical for rational structure-based discovery of new CXCR4 inhibitors, remain poorly understood. Here we first determined the effects of amino acid substitutions in CXCR4 on HIV-1NL4-3glycoprotein-elicited fusion events using site-directed mutagenesis-based fusion assays and identified 11 potentially key amino acid substitutions, including D97A and E288A, which caused >30% reduc
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Dissertations / Theses on the topic "HIV fusion inhibitor"

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Quinn, Killian. "The development of a new fusion inhibitor for the treatment of HIV." Thesis, Imperial College London, 2017. http://hdl.handle.net/10044/1/50677.

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Since the introduction of combination antiretroviral therapy (ART), there has been a dramatic improvement in the prognosis of people living with HIV. Indeed, data from numerous cohorts now show that for people commenced on ART at high CD4 counts and who are retained in care, life expectancy is similar to matched HIV-negative people. Consequently, the number of years an individual diagnosed with HIV can expect to be treated with ART is set to increase markedly. With the emergence of an older population, polypharmacy and drug-drug interactions are now more prominent clinical problems in the mana
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Fallarino, Lorena. "Anti HIV-1 gene therapy approach combining multiple siRNAs with the membrane-anchored fusion inhibitor C-peptide maC46." Doctoral thesis, Università degli studi di Padova, 2018. http://hdl.handle.net/11577/3426674.

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The development of highly active anti-retroviral therapy (HAART) has considerably improved life expectancy of HIV-1 positive patients by transforming this infection, which once was lethal, into a manageable chronic illness. Although a significant suppression of viral replication under undetectable level is guaranteed following a constant therapeutic adherence, this therapy fails to completely eliminate the infection due to the persistence of HIV-1 into reservoirs, which represent therefore the main obstacle to a definite cure. Furthermore, a lifelong adherence to treatment is associated with d
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Martins, do Canto António Manuel teixeira. "Estudo teórico da estrutura e dinâmica de péptidos inibidores da fusão do HIV em água e membranas biológicas." Doctoral thesis, Instituto de Formação Avançada, Universidade de Évora, 2013. http://hdl.handle.net/10174/10012.

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A acção dos péptidos inibidores de fusão (FI) do HIV, T-20 e T-1249, foi analisada nesta tese por uma abordagem in silico através da técnica de dinâmica molecular (MD). Foi estudada tanto a estrutura como a dinâmica destes FI em três situações diferentes: em solução (com o intuito de tentar mimetizar a situação do péptido no plasma sanguíneo) e a interagir com modelos de membranas de 1-palmitoil-2-oleil-fosfatidilcolina (POPC) (na fase líquido desordenado - Ld) e membranas de POPC / colesterol (1:1) (POPC / Chol) (na fase líquido ordenado – Lo). Com isto tentámos perceber se haveria diferenças
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Silva, Fabio Eduardo Santos da. "Avaliação da resistência genotípica ao Enfuvirtida em pacientes submetidos ao HAART. Fenotipagem virtual das cepas de HIV1 isoladas de trinta e dois pacientes que apresentaram resistência aos antirretrovirais." Universidade de São Paulo, 2009. http://www.teses.usp.br/teses/disponiveis/9/9136/tde-19112009-132144/.

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Introdução: estudos com Enfuvirtida (ENF) mostraram que mutações na HR1 da gp41 levam à resistência primária de cepas em pacientes sem tratamento prévio com inibidores de fusão (Derdeyn et al., 2000; Rimsky et. al., 1998; Sista et. al., 2002). Outros, que o uso contínuo de HAART leva à falha virológica (Shafer et. al., 1998; Shafer & Vuitton, 1999). Para a melhor escolha terapêutica recomenda-se usar a Genotipagem do HIV1 (Ministério da Saúde, 2008b; Perez-Elias et. al., 2003; Shafer et. al., 2001). Objetivos: avaliar o perfil de resistência do HIV1 ao ENF pelo sequenciamento da HR1 da gp41 em
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Chinnadurai, Raghavan. "HIV-1 resistance to fusion inhibitors." [S.l. : s.n.], 2007. http://nbn-resolving.de/urn:nbn:de:bsz:289-vts-58600.

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Cherry, Elana. "Trans-dominant negative inhibition of human immunodeficiency virus type 1 replication by expression of protease-reverse transcriptase fusion proteins." Thesis, National Library of Canada = Bibliothèque nationale du Canada, 1999. http://www.collectionscanada.ca/obj/s4/f2/dsk1/tape7/PQDD_0019/NQ50069.pdf.

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Suntoke, Tara R. "HIV entry : a biophysical and mutational analysis of gp41-mediated membrane fusion and its inhibition." Thesis, Massachusetts Institute of Technology, 2005. http://hdl.handle.net/1721.1/31181.

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Thesis (Ph. D.)--Massachusetts Institute of Technology, Dept. of Biology, 2005.<br>Includes bibliographical references.<br>The experiments described in this thesis were designed to elucidate the manner in which the HIV-1 envelope protein (Env) initiates infection of host cells, and to develop inhibitors of viral entry. Env comprises two non-covalently attached subunits, gpl20 and gp41, that associate as a trimer on the virion surface. Once gp 120 contacts the target cell, gp41 undergoes extensive conformational changes to mediate fusion of viral and cellular membranes. First, a short hydrophob
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Huhmann, Susanne [Verfasser]. "Stabilization of peptides by site-specific incorporation of fluorinated amino acids: Model studies and the development of fluorinated, peptide-based HIV-1 fusion inhibitors / Susanne Huhmann." Berlin : Freie Universität Berlin, 2019. http://d-nb.info/1176632922/34.

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Baron, Alice. "Synthèse et Etude d'Analogues Peptidiques en tant qu'Inhibiteurs de Fusion du VIH." Thesis, Montpellier 2, 2010. http://www.theses.fr/2010MON20209/document.

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Depuis la découverte du Virus de l'Immunodéficience Humaine (VIH) au début des années 80, la recherche de nouvelles molécules anti-VIH demeure un challenge important pour la communauté scientifique. Les effets secondaires liés à l'usage d'inhibiteurs de la réplication virale, la découverte des récepteurs et la compréhension du mécanisme d'entrée du virus dans la cellule hôte ont encouragé la recherche sur de nouveaux inhibiteurs ciblant l'entrée virale. A ce jour, l'Enfuvirtide est le seul inhibiteur d'entrée approuvé en tant qu'inhibiteur de fusion. Bien que ce composé soit un antiviral puiss
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Chinnadurai, Raghavan [Verfasser]. "HIV-1 resistance to fusion inhibitors / presented by Raghavan Chinnadurai." 2006. http://d-nb.info/995860548/34.

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Books on the topic "HIV fusion inhibitor"

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ger, Hans Ja. Entry Inhibitoren: Neue Formen der HIV-Therapie. Springer Medizin, 2008.

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(Editor), Jacqueline D. Reeves, and Cynthia A. Derdeyn (Editor), eds. Entry Inhibitors in HIV Therapy (Milestones in Drug Therapy) (Milestones in Drug Therapy). Birkhäuser Basel, 2007.

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Book chapters on the topic "HIV fusion inhibitor"

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Zhang, Xiaobin, Hao Wu, and Fengshan Wang. "Sifuvirtide, A Novel HIV-1 Fusion Inhibitor." In Peptide Drug Discovery and Development. Wiley-VCH Verlag GmbH & Co. KGaA, 2011. http://dx.doi.org/10.1002/9783527636730.ch11.

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Oishi, Shinya, Saori Ito, Hiroki Nishikawa, et al. "Development of a Novel Fusion Inhibitor against T-20-resistant HIV-1." In Advances in Experimental Medicine and Biology. Springer New York, 2009. http://dx.doi.org/10.1007/978-0-387-73657-0_170.

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Ma, Xue Ting, Xiao Hui Sun, Jian Jun Tan, and Cun Xin Wang. "Development of Peptide Fusion Inhibitors Targeting HIV-1 gp41." In IFMBE Proceedings. Springer Berlin Heidelberg, 2013. http://dx.doi.org/10.1007/978-3-642-29305-4_583.

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Venner, Colin M., Annette N. Ratcliff, Mathieu Coutu, Andrés Finzi, and Eric J. Arts. "HIV-1 Entry and Fusion Inhibitors: Mechanisms and Resistance." In Antimicrobial Drug Resistance. Springer International Publishing, 2017. http://dx.doi.org/10.1007/978-3-319-46718-4_36.

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Smeulders, Liesbet, Lieve Bunkens, Inge Vereycken, et al. "A Homogeneous Time-Resolved Fluorescence Assay to Identify Inhibitors of HIV-1 Fusion." In Antiviral Methods and Protocols. Humana Press, 2013. http://dx.doi.org/10.1007/978-1-62703-484-5_2.

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Srinivas, Shamala K., Ranga V. Srinivas, Richard W. Compans, Y. V. Venkatachalapathi, Jere P. Segrest, and G. M. Anantharamaiah. "Amphipathic helical peptides derived from the C-terminus of the HIV glycoprotein interact with membranes and inhibit virus-induced cell fusion." In Peptides. Springer Netherlands, 1992. http://dx.doi.org/10.1007/978-94-011-2264-1_274.

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Cai, Lifeng, Weiguo Shi, and Keliang Liu. "Peptides and Peptidomimetics as Tools to Probe Protein-Protein Interactions – Disruption of HIV-1 gp41 Fusion Core and Fusion Inhibitor Design." In Biochemistry. InTech, 2012. http://dx.doi.org/10.5772/34034.

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Liang, Guodong, Yan Huang, Jinlin Wang, et al. "Peptide-Based Fusion Inhibitors Targeting 6-HB: Resistance to HIV-1 outside of Cells." In Antiretroviral Therapy - Latest Advances and Perspectives [Working Title]. IntechOpen, 2025. https://doi.org/10.5772/intechopen.1011082.

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Pathogenic viruses causing large outbreaks often contain Class I fusion proteins on their envelopes. These proteins facilitate virus-host cell membrane fusion through a common mechanism involving the N-terminal Heptad Repeat region forming a coiled-coil trimer and the C-terminal region folding back to form a six-helix bundle (6-HB). Fusion inhibitors, particularly peptide-based ones like Enfuvirtide and Albuvirtide, target the 6-HB to block membrane fusion and have been clinically approved. Researchers have always been committed to digging out more peptide-based fusion inhibitors lead candidat
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Bourgade Karine, Dupuis Gilles, Frost Eric H., and Fülöp Jr. Tamàs. "Anti-Viral Properties of Amyloid-&bgr; Peptides." In Advances in Alzheimer’s Disease. IOS Press, 2017. https://doi.org/10.3233/978-1-61499-706-1-221.

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Amyloid-&amp;bgr; (A&amp;bgr;) peptides generated by the amyloidogenic pathway of amyloid-&amp;bgr; protein precursor processing contribute significantly to neurodegeneration characteristic of Alzheimer's disease (AD). The involvement of A&amp;bgr; peptides in the etiology of AD remains a subject of debate. Data published in the last 6 years by three different groups have added a new twist by revealing that A&amp;bgr; peptides could act as antimicrobial peptides (AMP) in in vitro assays against some common and clinically relevant microorganisms,inhibit replication of seasonal and pandemic stra
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Conference papers on the topic "HIV fusion inhibitor"

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Zhang, Xiaohong, Yiyin Xia, Chuan-Fa Liu, and James P. Tam. "Efficient synthesis of three-helix bundle proteins using ligase-mediated trimerization of HIV-1 fusion inhibitor T20 on a dendrimer scaffold." In 37th European Peptide Symposium. The European Peptide Society, 2024. http://dx.doi.org/10.17952/37eps.2024.p2331.

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Jiang, Shibo, Lin Radigan, and Li Zhang. "Convenient cell fusion assay for rapid screening for HIV entry inhibitors." In BiOS 2000 The International Symposium on Biomedical Optics, edited by Patrick A. Limbach, John C. Owicki, Ramesh Raghavachari, and Weihong Tan. SPIE, 2000. http://dx.doi.org/10.1117/12.380514.

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Lustosa, Alysson Bastos, João Paulo Holanda Soares, Iago Mateus Rocha Leite, Rilciane Maria dos Reis Ribeiro, and Olívio Feitosa Costa Neto. "SECRETORY CARCINOMA BREAST IN A YOUNG MAN." In XXIV Congresso Brasileiro de Mastologia. Mastology, 2022. http://dx.doi.org/10.29289/259453942022v32s1075.

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Introduction: Secretory carcinoma of the breast is a rare disease, accounting for approximately 0.15% of breast cancer cases. This entity was first described in a child in 1966. However, one of the largest case series with SEER data, encompassing a total of 190 patients, showed that the median age at diagnosis was 56 years, and it can affect both sexes, being much more common in women. In this same series, 58% and 40% of patients were positive for estrogen and progesterone hormone receptors, respectively. Most cases (86.86%) were well to moderately differentiated tumors without lymph node invo
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