Article
Biochemistry & Molecular Biology
Hyun Ji Kim, Jung Woo Park, Sangjae Seo, Kwang-Hwi Cho, Mohammed M. Alanazi, Eun-Kyoung Bang, Gyochang Keum, Ashraf K. El-Damasy
Summary: The development of resistance to targeted therapy in cancer is a major challenge in cancer treatment. This study aimed to identify new anticancer candidates, especially those targeting oncogenic mutants. Through structural modifications, a series of tailored quinoline-based arylamides were synthesized and evaluated for their inhibitory potency against B-RAF and C-RAF kinases. Compound 17b emerged as the most potent and exhibited significant inhibitory activity against resistant B-RAF mutants. Molecular docking and molecular dynamics studies provided insights into the binding mode of 17b. Additionally, all target compounds showed superior anticancer activity compared to the lead compound in cell lines. Compound 17b demonstrated highly potent antiproliferative activity against melanoma cell lines. Therefore, 17b has the potential to be a valuable candidate for anticancer chemotherapy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Coralie Dorard, Claire Madry, Olivier Buhard, Stefanie Toifl, Sebastian Didusch, Toky Ratovomanana, Quentin Letourneur, Helmut Dolznig, Mathew J. Garnett, Alex Duval, Manuela Baccarini
Summary: This study shows that RAF1 plays a crucial role in the proliferation of colorectal cancer and is independent of KRAS mutation status. RAF1 ablation decreases proliferation and STAT3 phosphorylation, indicating that RAF1 could be a therapeutic target for colorectal cancer.
Article
Biochemistry & Molecular Biology
Francesca Sanguedolce, Ugo Giovanni Falagario, Magda Zanelli, Andrea Palicelli, Maurizio Zizzo, Stefano Ascani, Simona Tortorella, Vito Mancini, Angelo Cormio, Giuseppe Carrieri, Luigi Cormio
Summary: Molecular subtyping of bladder cancer using immunohistochemical markers can help stratify patient risk. This study investigated the correlation between molecular subtypes and conventional prognostic variables in muscle-invasive bladder cancer and found a significant association between the pattern of muscularis propria invasion and molecular subtypes.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Oncology
Joanna Lee, Tasnia Ahmed, Andrea Maurichi, Lorenzo Di Guardo, Anna M. Stagno, Lydia Warburton, Amelia. M. Taylor, Elisabeth Livingstone, Saba Rehman, Adnan Khattak, Katharina C. Kahler, Vito Vanella, Victoria Atkinson, Michael Millward, Dirk Schadendorf, Douglas B. Johnson, Paolo A. Ascierto, Axel Hauschild, Serigne N. Lo, Georgina V. Long, Alexander M. Menzies, Matteo S. Carlino
Summary: For patients with advanced melanoma, there is a risk of recurrence after discontinuation of targeted therapy, but retreatment with targeted therapy shows a high response rate.
EUROPEAN JOURNAL OF CANCER
(2023)
Article
Medicine, General & Internal
Hyo Yeong Ahn, Chang Hun Lee, Min Ki Lee, Jung Seop Eom, Yeon Joo Jeong, Yeong Dae Kim, Jeong Su Cho, Jonggeun Lee, So Jeong Lee, Dong Hoon Shin, Ahrong Kim
Summary: This study aimed to explore the BRAF mutational status in resected non-small cell lung cancer (NSCLC) patients in the Korean population. The findings revealed a low incidence (1.3%) of the BRAF V600 mutation, with 0.8% of patients showing BRAF V600E mutations. Patients with lung adenocarcinoma and micropapillary components should be prioritized for BRAF mutation testing.
MEDICINA-LITHUANIA
(2023)
Article
Oncology
Kevin Yao, Emily Zhou, Chao Cheng
Summary: In this study, a B-Raf signature score was defined using RNA-seq data, which could predict B-Raf mutation status and other aberrations. Patients dichotomized by the median B-Raf score showed more significant stratification compared to other metrics. High B-Raf score also predicted higher sensitivity to B-Raf inhibitors and drugs targeting other relevant oncogenic pathways.
Article
Multidisciplinary Sciences
M. Govindammal, S. Kannan, P. Srinivasan, M. Prasath
Summary: Quercitrin is an anti-lung cancer agent derived from nuts and beverages. Its optimized structure and anti-cancer activity have been studied using computational methods. Molecular docking and molecular dynamics simulations demonstrate the stability and activity of Quercitrin.
Article
Biochemistry & Molecular Biology
Yuki Teramoto, Guiyang Jiang, Takuro Goto, Taichi Mizushima, Yujiro Nagata, George J. Netto, Hiroshi Miyamoto
Summary: In bladder cancer cells, GULP1 is regulated by AR signaling and influences sensitivity to cisplatin. Knockdown of GULP1 results in increased resistance to cisplatin treatment, reduced apoptosis, and increased G2/M phases. Additionally, GULP1 expression levels correlate with response to neoadjuvant chemotherapy in muscle-invasive bladder cancer patients.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Cell Biology
Avinashnarayan Venkatanarayan, Jason Liang, Ivana Yen, Frances Shanahan, Benjamin Haley, Lilian Phu, Erik Verschueren, Trent B. Hinkle, David Kan, Ehud Segal, Jason E. Long, Tony Lima, Nicholas P. D. Liau, Jawahar Sudhamsu, Jason Li, Christiaan Klijn, Robert Piskol, Melissa R. Junttila, Andrey S. Shaw, Mark Merchant, Matthew T. Chang, Donald S. Kirkpatrick, Shiva Malek
Summary: CRAF is necessary for the growth of KRAS mutant tumors and its dimerization plays a vital role. Lack of CRAF leads to sustained ERK activation and cell cycle arrest, and the CRAF-loss phenotype can be rescued by inhibiting MEK or ERK.
Review
Biochemistry & Molecular Biology
Francesca Sanguedolce, Magda Zanelli, Andrea Palicelli, Stefano Ascani, Maurizio Zizzo, Giorgia Cocco, Lars Bjornebo, Anna Lantz, Matteo Landriscina, Vincenza Conteduca, Ugo Giovanni Falagario, Luigi Cormio, Giuseppe Carrieri
Summary: A consensus classification has been developed for molecular stratification of bladder cancer (BC), which includes a six-cluster scheme. Immunohistochemistry (IHC) has been explored as a potential method for risk stratification and has shown promising results in different clinical settings.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Biochemistry & Molecular Biology
Francesca Sanguedolce, Magda Zanelli, Andrea Palicelli, Alessandra Bisagni, Maurizio Zizzo, Stefano Ascani, Maria Carmela Pedicillo, Angelo Cormio, Ugo Giovanni Falagario, Giuseppe Carrieri, Luigi Cormio
Summary: Bladder cancer is a heterogeneous disease with molecular, morphological, and clinical variations. HER2 is an oncogene involved in the development of bladder cancer. Assessing HER2 overexpression through immunohistochemistry can be useful in correctly identifying different types of bladder lesions, providing prognostic information, and improving BC molecular subtyping. Additionally, HER2 has potential as a therapeutic target in the development of novel target therapies.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Francesca Sanguedolce, Magda Zanelli, Andrea Palicelli, Stefano Ascani, Maurizio Zizzo, Giorgia Cocco, Lars Bjornebo, Anna Lantz, Ugo Giovanni Falagario, Luigi Cormio, Giuseppe Carrieri
Summary: Bladder cancer is a heterogeneous disease with varied clinical and pathological features, leading to different treatment responses. Molecular classification schemes play a crucial role in assessing prognosis and predicting outcomes, while immunohistochemistry has been explored as a surrogate method for stratifying bladder cancer.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Multidisciplinary Sciences
Eunyoung Park, Shaun Rawson, Anna Schmoker, Byeong-Won Kim, Sehee Oh, Kangkang Song, Hyesung Jeon, Michael J. Eck
Summary: RAF kinases are autoinhibited in cytosol and activated by recruitment to plasma membrane by GTP-bound RAS. This study presents cryoEM structures of a membrane-free KRAS/BRAF/MEK/14-3-3 complex, capturing a pre-activation intermediate with BRAF still in an autoinhibited state. The structures illustrate the separability of binding and activation of BRAF by RAS, suggesting a potential therapeutic strategy to stabilize the pre-activation intermediate instead of blocking KRAS binding.
NATURE COMMUNICATIONS
(2023)
Article
Medicine, General & Internal
Fee-Wai Chin, Huzlinda Hussin, De-Ming Chau, Teng-Aik Ong, Rosna Yunus, Azad Hassan Abdul Razack, Khatijah Yusoff, Soon-Choy Chan, Abhi Veerakumarasivam
Summary: This study aimed to analyze the protein expression of HOXA13 and HOXB13 genes in Malaysian bladder cancer patients and characterize their features. The results showed that high expression of HOXA13 was significantly associated with non-muscle invasive bladder cancer, lower tumor grade, higher number of lymph node metastases, and recurrence risk. In contrast, low expression of HOXB13 was significantly associated with muscle-invasive bladder cancer, higher tumor stage, tumor grade, and metastatic risk. The expression of HOXA13 and HOXB13 proteins were closely associated with bladder tumorigenesis, suggesting their potential as biomarkers in bladder cancer.
Article
Chemistry, Multidisciplinary
Charles W. Morgan, Ian L. Dale, Andrew P. Thomas, James Hunt, Jason W. Chin
Summary: In this study, bio-orthogonal ligand tethering (BOLT) was used to selectively target inhibitors to CRAF, showing that selective CRAF inhibition promotes paradoxical activation. This suggests that BOLT may be used to triage potential targets for drug discovery before any target-selective small molecules are known.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2021)
Article
Immunology
Konstantia E. Tasioudi, Stratigoula Sakellariou, Georgia Levidou, Dimitrios Theodorou, Nikolaos V. Michalopoulos, Efstratios Patsouris, Penelope Korkolopoulou, Angelica A. Saetta
Article
Oncology
Stratigoula Sakellariou, Paraskevi Fragkou, Georgia Levidou, Antonios N. Gargalionis, Christina Piperi, Georgia Dalagiorgou, Christos Adamopoulos, Angelica Saetta, George Agrogiannis, Irini Theohari, Stavros Sougioultzis, Panagiota Tsioli, Ioannis Karavokyros, Nikolaos Tsavaris, Ioannis D. Kostakis, Adamantia Zizi-Serbetzoglou, Gerasimos P. Vandoros, Efstratios Patsouris, Penelope Korkolopoulou
Article
Oncology
Maria L. Karadima, Angelica A. Saetta, Ilenia Chatziandreou, Andreas C. Lazaris, Efstratios Patsouris, Nikolaos Tsavaris
PATHOLOGY & ONCOLOGY RESEARCH
(2016)
Article
Pathology
Aggeliki Tserga, Ilenia Chatziandreou, Nicolaos V. Michalopoulos, Efstratios Patsouris, Angelica A. Saetta
Article
Urology & Nephrology
Michalis Liontos, Eleni-Andriana Trigka, Penelope Korkolopoulou, Kimon Tzannis, Giorgos Lainakis, Konstantinos Koutsoukos, Efthymios Kostouros, Maria Lykka, Christos N. Papandreou, Vassilis Karavasilis, Christos Christodoulou, Athanasios Papatsoris, Andreas Skolarikos, Ioannis Varkarakis, Ioannis Adamakis, Christos Alamanis, Konstantinos Stravodimos, Dionysios Mitropoulos, Charalambos Deliveliotis, Constantinos A. Constantinidis, Angelica Saetta, Efstratios Patsouris, Meletios I. Dimopoulos, Aristotelis Bamias
WORLD JOURNAL OF UROLOGY
(2017)
Article
Multidisciplinary Sciences
Eleftheria Lakiotaki, Georgia Levidou, Maria K. Angelopoulou, Christos Adamopoulos, Gerassimos Pangalis, George Rassidakis, Theodoros Vassilakopoulos, Gabriella Gainaru, Pagona Flevari, Sotirios Sachanas, Angelica A. Saetta, Athanasia Sepsa, Maria Moschogiannis, Christina Kalpadakis, Nikolaos Tsesmetzis, Vassilios Milionis, Ilenia Chatziandreou, Irene Thymara, Panayiotis Panayiotidis, Maria Dimopoulou, Eleni Plata, Konstantinos Konstantopoulos, Efstratios Patsouris, Christina Piperi, Penelope Korkolopoulou
SCIENTIFIC REPORTS
(2016)
Article
Pathology
Spyridon Tsikalakis, Ilenia Chatziandreou, Nikolaos Michalopoulos, Georgios E. Theodoropoulos, Stratigoula Sakellariou, Penelope Korkolopoulou, Efstratios Patsouris, Angelica A. Saetta
PATHOLOGY RESEARCH AND PRACTICE
(2018)
Article
Cell & Tissue Engineering
Konstantinos G. Apostolou, Ioannis G. Papanikolaou, Charalampos Katselis, Themistoklis Feretis, Dimitrios Kletsas, Manousos M. Konstadoulakis, Maria Lymperi, Angelica A. Saetta, Spiros Tsikalakis, George Agrogiannis, Efstratios Patsouris, George C. Zografos, Apostolos E. Papalois
STEM CELLS INTERNATIONAL
(2018)
Article
Multidisciplinary Sciences
Sofia Fragkioudaki, Adrianos Nezos, Vassilis L. Souliotis, Ilenia Chatziandreou, Angelica A. Saetta, Nikolaos Drakoulis, Athanasios G. Tzioufas, Michael Voulgarelis, Petros P. Sfikakis, Michael Koutsilieris, Mary K. Crow, Haralampos M. Moutsopoulos, Clio P. Mavragani
SCIENTIFIC REPORTS
(2017)
Article
Oncology
Evangelos Koustas, Panagiotis Sarantis, Stamatios Theoharis, Angelica A. Saetta, Ilenia Chatziandreou, Georgia Kyriakopoulou, Ioanna Giannopoulou, Maria Michelli, Dimitrios Schizas, Athanasios G. Papavassiliou, Michalis V. Karamouzis
AMERICAN JOURNAL OF CLINICAL ONCOLOGY-CANCER CLINICAL TRIALS
(2019)
Article
Oncology
Patroklos Katafygiotis, Stratigoula Sakellariou, Ilenia Chatziandreou, Ioanna Giannopoulou, Irene Thymara, Angelica A. Saetta, Penelope Korkolopoulou
ANTICANCER RESEARCH
(2019)
Article
Pathology
Eleni A. Karatrasoglou, Ilenia Chatziandreou, Stratigoula Sakellariou, Konstantinos Stamopoulos, Nikolaos Kavantzas, Andreas C. Lazaris, Penelope Korkolopoulou, Angelica A. Saetta
Article
Pathology
Maria Michelli, Alexandros Zougros, Ilenia Chatziandreou, Nikolaos Michalopoulos, Andreas C. Lazaris, Angelica A. Saetta
PATHOLOGY RESEARCH AND PRACTICE
(2020)
Article
Cell Biology
Galinos Fanourakis, Angelica A. Saetta, Andreas C. Lazaris, Maria Miaouli, Gerassimos E. Voutsinas, Efstratios Patsouris, Sofia Tseleni-Balafouta
Review
Oncology
Emmanouil Dimonitsas, Aliki Liakea, Stratigoula Sakellariou, Irene Thymara, Andreas Giannopoulos, Alexandros Stratigos, Efthymia Soura, Angelica Saetta, Penelope Korkolopoulou
ANNALS OF TRANSLATIONAL MEDICINE
(2018)