Article
Medicine, Research & Experimental
Ho Jin Lee, Hye-Young Min, Young-Sik Yong, Jihyae Ann, Cong Truong Nguyen, Minh Thanh La, Seung Yeob Hyun, Huong Thuy Le, Hyewon Kim, Hyukjin Kwon, Gibeom Nam, Hyun-Ju Park, Jeewoo Lee, Ho-Young Lee
Summary: This study revealed that Hsp90 inhibitors that block the N-terminal ATP-binding pocket activate STAT3, leading to the transcriptional upregulation of Wnt ligands and promoting cell survival in NSCLC. NCT-80 effectively reduced NSCLC cell viability, migration, and CSC-like phenotypes, and inhibited the growth of patient-derived xenograft tumors.
Article
Gastroenterology & Hepatology
Li Wang, Qihui Zhu, Jitao David Zhang, Yaling Zhang, Xiaoju Ni, Kunlun Xiang, Jiaxi Jiang, Baocun Li, Youjun Yu, Hui Hu, Meifang Zhang, Waikwong Wu, Jing Zeng, Zhipeng Yan, Jieyu Dai, Kai Sun, Xin Zhang, Dongdong Chen, Song Feng, Lisa Sach-Peltason, John A. T. Young, Lu Gao
Summary: A small-molecule cccDNA inhibitor has been discovered that reduces the levels of HBV cccDNA. This provides a potential new approach for the complete cure of patients chronically infected with HBV.
JOURNAL OF HEPATOLOGY
(2023)
Article
Oncology
Rony Mshaik, John Simonet, Aleksandra Georgievski, Layla Jamal, Shaliha Bechoua, Paola Ballerini, Pierre-Simon Bellaye, Zandile Mlamla, Jean-Paul Pais de Barros, Audrey Geissler, Pierre-Jean Francin, Francois Girodon, Carmen Garrido, Ronan Quere
Summary: T-cell and B-cell acute lymphoblastic leukemias are aggressive hematological malignancies that require novel targeted therapies to improve patient outcomes. Research has shown that HSP90 plays a key role in the growth of ALL cells.
BLOOD CANCER JOURNAL
(2021)
Article
Chemistry, Medicinal
Robin A. Fairhurst, Pascal Furet, Patricia Imbach-Weese, Frederic Stauffer, Heinrich Rueeger, Clive McCarthy, Sebastien Ripoche, Susanne Oswald, Bertrand Arnaud, Aline Jary, Michel Maira, Christian Schnell, Daniel A. Guthy, Markus Wartmann, Michael Kiffe, Sandrine Desrayaud, Francesca Blasco, Toni Widmer, Frank Seiler, Sascha Gutmann, Mark Knapp, Giorgio Caravatti
Summary: Balanced pan-class I phosphoinositide 3-kinase inhibition is a promising approach for cancer treatment, offering the potential to treat various tumor types and enhance efficacy with a single inhibitor. This study identified a best-in-class phosphoinositide 3-kinase inhibitor, 40 (NVP-CLR457), by optimizing its properties, including eliminating off-target activity and balancing the inhibition profile.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Hongchao Zheng, Jichen Zhao, Bing Li, Weihe Zhang, Michael A. Stashko, Katherine A. Minson, Madeline G. Huey, Yubai Zhou, Henry Shelton Earp, Dmitri Kireev, Douglas K. Graham, Deborah DeRyckere, Stephen Frye, Xiaodong Wang
Summary: Inhibition of MER receptor tyrosine kinase (MERTK) contributes to tumor cell killing and stimulation of the immune response. UNC5293 is a highly selective MERTK inhibitor with potent and selective inhibition in cell-based assays, excellent mouse PK properties, and activity in leukemia cells in a murine model.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Xin Xie, Nan Zhang, Xiang Li, He Huang, Cheng Peng, Wei Huang, Leonard J. Foster, Gu He, Bo Han
Summary: Hsp90 is a crucial molecular chaperone that plays a critical role in biological pathways and cellular operations. It is closely linked to cancer and has been studied as a potential drug target. Combining Hsp90 inhibitors with other tumor inhibitors has shown synergistic antitumor effects, making the development of Hsp90 dual-target inhibitors a promising strategy in cancer treatment.
BIOORGANIC CHEMISTRY
(2023)
Article
Multidisciplinary Sciences
Tadatoshi Sato, Christian D. Castro Andrade, Sung-Hee Yoon, Yingshe Zhao, William J. Greenlee, Patricia C. Weber, Usha Viswanathan, John Kulp, Daniel J. Brooks, Marie B. Demay, Mary L. Bouxsein, Bruce Mitlak, Beate Lanske, Marc N. Wein
Summary: This study identifies SIK2/SIK3 as potential drug targets for treating osteoporosis and successfully develops an orally available SIK2/SIK3 inhibitor. The inhibitor stimulates bone formation and increases bone density without apparent toxicity. These findings provide a new approach for the pharmacological treatment of osteoporosis.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Biochemistry & Molecular Biology
Kazuki Miura, Manjusha Joshi, Taiki Morita, Hiroyuki Nakamura
Summary: This study developed an efficient method for synthesizing bicyclo[3.3.1]nonane, and found that its derivatives can inhibit gene transcription and cell growth. The compounds also showed different mechanism of action compared to conventional HSP90 inhibitors.
BIOORGANIC & MEDICINAL CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Pengxing He, Jing Jing, Linna Du, Xuyang Zhang, Yufei Ren, Han Yang, Bin Yu, Hongmin Liu
Summary: YS-363 is a novel EGFR inhibitor that demonstrates potent reversible inhibition and excellent activities against cell proliferation, migration, cell cycle and apoptosis. It is a promising selective inhibitor that can potentially be developed as a more effective anti-lung cancer agent targeting EGFR.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Pharmacology & Pharmacy
Ruby Maharjan, Laxman Subedi, Rudra Pangeni, Saurav Kumar Jha, Seo Hee Kang, Kwan-Young Chang, Youngro Byun, Jeong Uk Choi, Jin Woo Park
Summary: In this study, oral administration of PMX/DL-CD improved the oral bioavailability of PMX and demonstrated enhanced antitumor effects in mice models.
Article
Pharmacology & Pharmacy
Pang-Yen Liu, Hsin-Hsueh Shen, Ching-Wen Kung, Shu-Ying Chen, Chia-Hsien Lu, Yen-Mei Lee
Summary: Sepsis is a life-threatening organ dysfunction syndrome caused by bacterial infections, characterized by systemic inflammatory responses and elevated oxidative stress leading to multiple organ dysfunction and disseminated intravascular coagulation. Heat shock protein 70 (HSP70) plays a protective role in cellular homeostasis, while HSP 90 inhibitors have been reported to have anti-inflammatory effects through the induction of HSP70.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Neil K. Viswanathan, Michael E. Chirgwin, Julia Gibbs, Brianna N. Kalaj, Sierra Durham, Jennifer Tran, Maximillian Gomez, Horacio Lazaro, Ming Chen, Christopher R. Mansfield, Emily R. Derbyshire, Scott Eagon
Summary: A series of & beta;-carbolines based on harmine were synthesized and tested for antimalarial activity and toxicity. Some of these compounds showed promising bioactivity, offering a new therapeutic option with a unique mode of action compared to current clinical treatments.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Martin A. . Lowe, Alvaro Cardenas, Jean-Pierre Valentin, Zhaoning Zhu, Jan Abendroth, Jose L. Castro, Reiner Class, Annie Delaunois, Renaud Fleurance, Helga Gerets, Vitalina Gryshkova, Lloyd King, Donald D. Lorimer, Malcolm MacCoss, Julian H. Rowley, Marie-Luce Rosseels, Leandro Royer, Richard D. Taylor, Melanie Wong, Oliver Zaccheo, Vishal P. Chavan, Gokul A. . Ghule, Bapusaheb K. Tapkir, Jeremy N. Burrows, Maelle Duffey, Matthias Rottmann, Sergio Wittlin, Inigo Angulo-Barturen, Maria Belen Jimenez-Diaz, Josefine Striepen, Kate J. Fairhurst, Tomas Yeo, David A. . Fidock, Alan F. Cowman, Paola Favuzza, Benigno Crespo-Fernandez, Francisco Javier Gamo, Daniel E. Goldberg, Dominique Soldati-Favre, Benoit Laleu, Teresa de Haro
Summary: This study optimized Plasmepsin X (PMX) and identified potent PMX inhibitors with potential efficacy in treating malaria.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Wataru Kawahata, Tokiko Asami, Takao Kiyoi, Takayuki Irie, Shigeki Kashimoto, Hatsuo Furuichi, Masaaki Sawa
Summary: The study identified a series of novel noncovalent BTK inhibitors, among which 13f (AS-1763) as a next-generation noncovalent BTK inhibitor, showed good oral availability, potency, and selectivity, with significant efficacy in in vivo tumor xenograft models, and has advanced to phase 1 clinical trials.
JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Physical
Zhenfu Wen, Fengyu Liu, Guoxin Liu, Qinyan Sun, Yuhuan Zhang, Mehdi Muhammad, Yongqian Xu, Hongjuan Li, Shiguo Sun
Summary: This study explores a treatment strategy combining photothermal therapy and chemotherapy to promote apoptosis in cancer cells by inhibiting the overexpression of Hsp-90 and survivin.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2021)
Article
Oncology
Andrew J. Massey, Peter Stephens, Rebecca Rawlinson, Lauren McGurk, Ruth Plummer, Nicola J. Curtin
MOLECULAR ONCOLOGY
(2016)
Article
Oncology
Andrew J. Massey, Stephen Stokes, Helen Browne, Nicolas Foloppe, Andrea Fiumana, Simon Scrace, Mandy Fallowfield, Simon Bedford, Paul Webb, Lisa Baker, Mark Christie, Martin J. Drysdale, Mike Wood
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Oncology
Andrew J. Massey
Article
Oncology
Joanne Wayne, Teresa Brooks, Andrew J. Massey
Article
Multidisciplinary Sciences
Andrew J. Massey
SCIENTIFIC REPORTS
(2016)
Article
Chemistry, Medicinal
Paul A. Brough, Lisa Baker, Simon Bedford, Kirsten Brown, Seema Chavda, Victoria Chell, Jalanie D'Alessandro, Nicholas G. M. Davies, Ben Davis, Loic Le Strat, Alba T. Macias, Daniel Maddox, Patrick C. Mahon, Andrew J. Massey, Natalia Matassova, Sean McKenna, Johannes W. G. Meissner, Jonathan D. Moore, James B. Murray, Christopher J. Northfield, Charles Parry, Rachel Parsons, Stephen D. Roughley, Terry Shaw, Heather Simmonite, Stephen Stokes, Allan Surgenor, Emma Stefaniak, Alan Robertson, Yikang Wang, Paul Webb, Neil Whitehead, Mike Wood
JOURNAL OF MEDICINAL CHEMISTRY
(2017)
Article
Biochemical Research Methods
Clara C. Geneste, Andrew J. Massey
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Multidisciplinary Sciences
Andrew J. Massey
Article
Oncology
Rebecca Rawlinson, Andrew J. Massey
Article
Oncology
Christopher Bryant, Rebecca Rawlinson, Andrew J. Massey
Article
Biochemistry & Molecular Biology
Christopher Bryant, Kirsten Scriven, Andrew J. Massey
Article
Oncology
Hana Tabusa, Teresa Brooks, Andrew J. Massey
MOLECULAR CANCER RESEARCH
(2013)
Article
Multidisciplinary Sciences
Andrew J. Massey
Article
Multidisciplinary Sciences
Andrew J. Massey
SCIENTIFIC REPORTS
(2017)
Meeting Abstract
Chemistry, Multidisciplinary
Alba T. Macias, Christopher J. Graham, Lisa Baker, Teresa Brooks, Victoria Chell, Katherine Lawlor, Andrew J. Massey, Natalia Matassova, Jon D. Moore, James B. Murray, Stuart Ray, Alan Robertson, Stephen D. Roughley, Alasdair M. Scott, Terry Shaw, Heather Simmonite, Julia Smith, Anna Staniszewska, Allan E. Surgenor, Claire Walmsley, Joanne Wayne, Paul Webb
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY
(2014)