Article
Biochemistry & Molecular Biology
Siddhant Bhoir, Oluwatobi Ogundepo, Xiuping Yu, Runhua Shi, Arrigo De Benedetti
Summary: This study discovers that enhancing the therapeutic effect of cisplatin (CPT) on androgen-insensitive prostate cancer cells can be achieved by inhibiting TLK1 protein. TLK1, through phosphorylation of RAD54L and RAD54B proteins, participates in homologous recombination repair (HRR) and interferes with the HRR process, thus increasing sensitivity to CPT.
Article
Immunology
Xue-Feng Li, Cigdem Selli, Han-Lin Zhou, Jian Cao, Shuiqing Wu, Ruo-Yu Ma, Ye Lu, Cheng-Bin Zhang, Bijie Xun, Alyson D. Lam, Xiao-Cong Pang, Anu Fernando, Zeda Zhang, Asier Unciti-Broceta, Neil O. Carragher, Prakash Ramachandran, Neil C. Henderson, Ling-Ling Sun, Hai-Yan Hu, Gui-Bo Li, Charles Sawyers, Bin-Zhi Qian
Summary: This study identified macrophages as the major component of the metastatic microenvironment in bone-metastatic prostate cancer. Macrophages were found to play a critical role in enzalutamide resistance through the induction of a wound-healing-like response and activation of the cytokine activin A- fibronectin-integrin alpha 5-tyrosine kinase Src signaling cascade. Depletion of macrophages or inhibition of Src significantly inhibited resistant growth, suggesting a potential therapeutic approach for treating metastatic prostate cancer.
JOURNAL OF EXPERIMENTAL MEDICINE
(2023)
Article
Pharmacology & Pharmacy
Pethaiah Gunasekaran, Ho Jin Han, Jung Hoon Choi, Eun Kyoung Ryu, Nam Yeong Park, Geul Bang, Yeo Kyung La, Sunghyun Park, Kyubin Hwang, Hak Nam Kim, Mi-Hyun Kim, Young Ho Jeon, Nak-Kyun Soung, Jeong Kyu Bang
Summary: The small molecule ADG-2e has shown significant anticancer potency by inhibiting cell proliferation and inducing cancer cell death possibly through a mechanism of cell damage. In mouse xenograft models, ADG-2e demonstrated potential in inhibiting cancer cell proliferation.
Review
Oncology
Yu-Shui Ma, Ji-Bin Liu, Xiao-Li Yang, Rui Xin, Yi Shi, Dan-Dan Zhang, Hui-Min Wang, Pei-Yao Wang, Qin-Lu Lin, Wen Li, Da Fu
Summary: Chemotherapy is a main treatment for cancer, advancing from cytotoxic to precise treatment strategies and targeting drugs for specific genes. Research into cancer cells' molecular mechanisms has led to accelerated development of related drugs through technologies like cancer genome sequencing.
AMERICAN JOURNAL OF CANCER RESEARCH
(2021)
Review
Biochemistry & Molecular Biology
Siddhant Bhoir, Arrigo De Benedetti
Summary: Androgen deprivation therapy (ADT) is the main treatment for prostate cancer, but it can lead to resistance and poor prognosis. Our research identified TLK1 as a crucial factor in PCa cell adaptation to ADT and its inhibition could prevent PCa progression and metastasis. Targeting TLK1 could be a promising approach in treating prostate cancer.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Cell Biology
Bingbing Dai, Jithesh J. Augustine, Ya'an Kang, David Roife, Xinqun Li, Jenying Deng, Lin Tan, Leona A. Rusling, John N. Weinstein, Philip L. Lorenzi, Michael P. Kim, Jason B. Fleming
Summary: This study identified a novel compound NSLC01 that selectively targets NRF2-activated pancreatic cancer cells, inducing significant anticancer effects, especially in cells with high NRF2 activation. NSLC01 induces apoptosis in cancer cells by inhibiting protein translation and suppressing de novo synthesis of amino acids, leading to synthetic lethal effects in NRF2-activated pancreatic cancers.
CELL DEATH & DISEASE
(2021)
Article
Oncology
Yishu Wang, Jianxiu Yu
Summary: Protein modification with SUMOs has dual roles in prostate cancer tumorigenesis and development, with deregulated SUMOylation affecting the balance between tumorigenic potential and anticancer effects. SUMOylation on the androgen receptor and oncoproteins plays a role in this pathological process in PCa.
Article
Immunology
Yue Zheng, Yin-Yin Xue, Ya-Qin Zhao, Ye Chen, Zhi-Ping Li
Summary: This case report suggests that despite low HER2 expression in patients with metastatic primary urethral carcinoma, they can still benefit from the combination of Disitamab Vedotin and PD-1 inhibitor, achieving persistent partial remission.
FRONTIERS IN IMMUNOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Sreeja Sreekumar, Dong Zhou, Cedric Mpoy, Elsa Schenk, Jalen Scott, Jeffrey M. Arbeit, Jinbin Xu, Buck E. Rogers
Summary: This study identified PARP-1 as an attractive target for therapeutic strategies in advanced prostate cancer. Synthesized radio-brominated Auger emitting inhibitor, [Br-77]Br-WC-DZ, induced DNA damage, cell cycle arrest, and cytotoxicity in prostate cancer cells. The findings provide a strong rationale for future clinical investigation.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Huahui Zeng, Duanjie Xu, Yagang Song, Shuo Tian, Jingyi Qiao, Zhanzhan Li, Lingzhou Zhao, Hui Shi, Yueyue Zhou, Shuo Li, Ying Luo, Jiashi Li, Mingsan Miao, Xiangxiang Wu
Summary: The researchers synthesized and evaluated nine prodrugs, among which SS-12 showed the most promising efficacy against breast cancer, with improved bioavailability and longer retention time compared to stachydrine.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Oncology
Philip Vitorino, Chen-Hua Chuang, Alexandre Iannello, Xi Zhao, Wade Anderson, Ronald Ferrando, Zhaomei Zhang, Shravanthi Madhavan, Holger Karsunky, Laura R. Saunders
Summary: Combining sub-efficacious doses of Rova-T with anti-PD1 enhances anti-tumor activity and sustains anti-tumor immunity in SCLC patients. The combination treatment activates immune response, increases CD8 T cells, and results in prolonged anti-tumor effects.
TRANSLATIONAL ONCOLOGY
(2021)
Review
Endocrinology & Metabolism
David Standing, Prasad Dandawate, Shrikant Anant
Summary: Prolactin (PRL) is a peptide hormone secreted by the anterior pituitary gland, and its receptor PRLR plays a role in various cancers. PRL binding to PRLR leads to downstream signaling that promotes cancer progression. The PRLR signaling pathway is an attractive target for drug development in cancer treatment.
FRONTIERS IN ENDOCRINOLOGY
(2023)
Article
Multidisciplinary Sciences
Lin Lei, Lijuan Yu, Weixiao Fan, Xiaoke Hao
Summary: This study reveals the significant role of small extracellular vesicles (sEVs) in the androgen-independent transformation of prostate cancer. By transferring the key sEVs molecule Let-7a-5p and activating the androgen receptor (AR) and PI3K/Akt signaling pathways, sEVs regulate the process. This finding provides new perspectives for targeted treatment approaches for AIPC patients.
Article
Biochemistry & Molecular Biology
Min Chen, Linxuan Cai, Yu Xiang, Ling Zhong, Jianyou Shi
Summary: Non-radioactive PSMA-targeted SMDCs have great therapeutic potential for mCRPC as a form of targeted therapy. Several non-radioactive PSMA-targeted SMDCs that have been developed show favorable properties in both in vitro and in vivo evaluations, demonstrating better results than unmodified cytotoxic drugs.
BIOORGANIC CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Juan Miao, Honggen Yuan, Jingwei Rao, Jiahui Zou, Kelu Yang, Guiqing Peng, Shengbo Cao, Huanchun Chen, Yunfeng Song
Summary: A compound with high and specific inhibitory effects on ZIKV NS2B-NS3 protease has been identified in this study. The compound showed antiviral effects and protection in cell and mouse models, making it a potential therapeutic agent.
ANTIVIRAL RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Yoshinobu Saitoh, Costansia Bureta, Hiromi Sasaki, Satoshi Nagano, Shingo Maeda, Tatsuhiko Furukawa, Noboru Taniguchi, Takao Setoguchi
MOLECULAR CARCINOGENESIS
(2019)
Article
Oncology
Muhammad Kamil, Yoshinari Shinsato, Nayuta Higa, Takuro Hirano, Masashi Idogawa, Tomoko Takajo, Kentaro Minami, Michiko Shimokawa, Masatatsu Yamamoto, Kohichi Kawahara, Hajime Yonezawa, Hirofumi Hirano, Tatsuhiko Furukawa, Koji Yoshimoto, Kazunori Arita
BRITISH JOURNAL OF CANCER
(2019)
Article
Biotechnology & Applied Microbiology
Jingsong Cao, Ding An, Mikel Galduroz, Jenny Zhuo, Shi Liang, Marianne Eybye, Andrea Frassetto, Eishi Kuroda, Aki Funahashi, Jordan Santana, Cosmin Mihai, Kerry E. Benenato, E. Sathyajith Kumarasinghe, Staci Sabnis, Timothy Salerno, Kimberly Coughlan, Edward J. Miracco, Becca Levy, Gilles Besin, Joshua Schultz, Christine Lukacs, Lin Guey, Patrick Finn, Tatsuhiko Furukawa, Paloma H. Giangrande, Takeyori Saheki, Paolo G. V. Martini
Article
Pharmacology & Pharmacy
Tsuyoshi Aoyama, Yoshihiko Shibayama, Tatsuhiko Furukawa, Mitsuru Sugawara, Yoh Takekuma
BIOLOGICAL & PHARMACEUTICAL BULLETIN
(2019)
Article
Oncology
Takuto Kawahata, Kohichi Kawahara, Michiko Shimokawa, Akie Sakiyama, Takehiro Shiraishi, Kentaro Minami, Masatatsu Yamamoto, Yoshinari Shinsato, Kazunari Arima, Toshiyuki Hamada, Tatsuhiko Furukawa
Article
Oncology
Takuro Hirano, Yoshinari Shinsato, Kan Tanabe, Nayuta Higa, Muhammad Kamil, Kohichi Kawahara, Masatatsu Yamamoto, Kentaro Minami, Michiko Shimokawa, Takaaki Arigami, Shigehiro Yanagita, Daisuke Matushita, Yoshikazu Uenosono, Sumiya Ishigami, Yuko Kijima, Kosei Maemura, Ikumi Kitazono, Akihide Tanimoto, Tatsuhiko Furukawa, Shoji Natsugoe
Article
Chemistry, Analytical
Takahiro Kogaki, Ikumi Ohshio, Hasumi Ura, Souta Iyama, Kaori Kitae, Toshiya Morie, Shintarou Fujii, Shohei Sato, Toshiyuki Nagata, Aya Harada Takeda, Masaya Aoki, Kazuhiro Ueda, Kentaro Minami, Masatatsu Yamamoto, Kohichi Kawahara, Tatsuhiko Furukawa, Masami Sato, Yuko Ueda, Kentaro Jingushi, Zenzaburo Tozuka, Daisuke Saigusa, Hiroaki Hase, Kazutake Tsujikawa
Summary: A highly sensitive and quantitative method was developed using UHPLC-UniSpray-MS/MS to measure modified nucleosides, successfully detecting differences in levels of nucleosides between cancerous and noncancerous tissues in various biological samples.
JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS
(2021)
Article
Multidisciplinary Sciences
Kentaro Jingushi, Masaya Aoki, Kazuhiro Ueda, Takahiro Kogaki, Masaya Tanimoto, Yuya Monoe, Masayuki Ando, Takuya Matsumoto, Kentaro Minami, Yuko Ueda, Kaori Kitae, Hiroaki Hase, Toshiyuki Nagata, Aya Harada-Takeda, Masatatsu Yamamoto, Kohichi Kawahara, Kazuhiro Tabata, Tatsuhiko Furukawa, Masami Sato, Kazutake Tsujikawa
Summary: The study reveals that high expression of ALKBH4 is associated with the progression of non-small-cell lung cancer, and knockdown of ALKBH4 can inhibit cancer cell proliferation and affect cell cycle and E2F1 expression. Patients with high ALKBH4 expression have a poor prognosis, indicating that ALKBH4 plays a crucial tumour-promoting role in NSCLC.
SCIENTIFIC REPORTS
(2021)
Article
Oncology
Tsunayuki Otsuka, Kazuhiro Ueda, Tatsuhiko Furukawa, Chihaya Koriyama, Ituro Inoue, Masami Sato
Summary: The frequency of EGFR mutations in lung adenocarcinoma patients depends on their mitochondrial lineage, indicating a potential role of maternal ancestry in influencing EGFR mutations in this population, especially in non-smokers.
ANTICANCER RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Toshiyuki Nagata, Kentaro Minami, Masatatsu Yamamoto, Tsubasa Hiraki, Masashi Idogawa, Katsumi Fujimoto, Shun Kageyama, Kazuhiro Tabata, Kohichi Kawahara, Kazuhiro Ueda, Ryuji Ikeda, Yukio Kato, Masaaki Komatsu, Akihide Tanimoto, Tatsuhiko Furukawa, Masami Sato
Summary: The study shows that BHLHE41 expression in normal lung tissues is higher than in lung adenocarcinoma tissues, and is associated with better overall survival in patients. In non-small cell lung cancer, BHLHE41 expression helps prevent malignant progression of early lung tumors.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Oncology
Masaya Aoki, Kazuhiro Ueda, Go Kamimura, Yoshiyuki Iwamoto, Mizuki Ikehata, Keisuke Tabata, Yuri Sakagami, Shoichiro Morizono, Takuya Tokunaga, Tadashi Umehara, Aya Harada-Takeda, Koki Maeda, Toshiyuki Nagata, Kota Kariatsumari, Tatsuhiko Furukawa, Kazutake Tsujikawa, Masami Sato
Summary: The expression of ALKBH4 is associated with histological type and prognosis in non-small cell lung cancer, and may serve as a useful predictor for postoperative outcomes in lung adenocarcinoma patients.
TRANSLATIONAL CANCER RESEARCH
(2022)
Review
Biochemistry & Molecular Biology
Tatsuhiko Furukawa, Kentaro Mimami, Toshiyuki Nagata, Masatasu Yamamoto, Masami Sato, Akihide Tanimoto
Summary: The circadian rhythm-related genes BHLHE40/DEC1 and BHLHE41/DEC2 have diverse functions in different cellular and tissue contexts. BHLHE41/DEC2 can act as both a cancer-suppressor and an oncogene during cancer development. Studies on the effects of BHLHE41/DEC2 on differentiation have been conducted using Bhlhe41/Dec2 knockout mice and/or in vitro differentiation models, as well as through genetic analysis of tumor cells, in vitro analysis of cancer cell lines, and immunohistochemical studies of clinical samples. We summarize these studies, discuss several issues, and highlight the need for further research to resolve contradictory findings.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Dentistry, Oral Surgery & Medicine
Noriho Shinagawa, Kentaro Minami, Takayuki Ishida, Hiroshi Hijioka, Masatatsu Yamamoto, Kohichi Kawahara, Tatsuhiko Furukawa, Norifumi Nakamura
Summary: Combining hydroxyurea (HU) and/or tranilast (TRL) with gemcitabine (GEM) enhances the toxic effect in gemcitabine-resistant cells induced by RRM1, potentially by reducing the ratio of RRM1/RRM2. These compounds have different effects on the mRNA and protein expression of RRM1 and RRM2.
ORAL SCIENCE INTERNATIONAL
(2021)
Article
Oncology
Hiroaki Hase, Masaya Aoki, Kentaro Matsumoto, Shuichi Nakai, Toshiyuki Nagata, Aya Takeda, Kazuhiro Ueda, Kentaro Minami, Kaori Kitae, Kentaro Jingushi, Yuko Ueda, Masatatsu Yamamoto, Tatsuhiko Furukawa, Masami Sato, Kazutake Tsujikawa
Summary: It was found that Ct-SLCO1B3 acts as a tumour-promoting factor in NSCLC by regulating EMT-related genes, leading to upregulation of anchorage-independent cell growth and cell migration.
Article
Multidisciplinary Sciences
Takeyori Saheki, Mitsuaki Moriyama, Eishi Kuroda, Aki Funahashi, Izumi Yasuda, Yoshiko Setogawa, Qinghua Gao, Miharu Ushikai, Sumie Furuie, Ken-ichi Yamamura, Katsura Takano, Yoichi Nakamura, Kazuhiro Eto, Takashi Kadowaki, David S. Sinasac, Tatsuhiko Furukawa, Masahisa Horiuchi, Yen How Tai
SCIENTIFIC REPORTS
(2019)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
