Article
Pharmacology & Pharmacy
Eva Fuchs, David Alexander Christian Messerer, Georg Karpel-Massler, Michael Fauler, Thomas Zimmer, Bettina Jungwirth, Karl Josef Foehr
Summary: In addition to its classical anti-cancer activity, the tumor therapeutic drug TIC10 may enhance its anti-tumor properties by blocking voltage-gated sodium channels.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Yichao Wan, Guoqing Fang, Hongjuan Chen, Xu Deng, Zilong Tang
Summary: This review summarizes recent advances of sulfonamide derivatives as potential anti-cancer agents, focusing on their applications on anti-cancer targets and corresponding structure-activity relationships.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Yichao Wan, Jiabing Long, Han Gao, Zilong Tang
Summary: Cancer is the second leading health killer in human society, and there is an urgent need to develop new anticancer agents with high activity and low toxicity due to multi-drug resistance and side effects. 2-Aminothiazole, as an important scaffold with potential anti-cancer activity, plays a crucial role in the discovery of anti-cancer agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Oncology
Antonio Federico, Michele Fratello, Giovanni Scala, Lena Mobus, Alisa Pavel, Giusy del Giudice, Michele Ceccarelli, Valerio Costa, Alfredo Ciccodicola, Vittorio Fortino, Angela Serra, Dario Greco
Summary: The study found that current treatments for complex diseases have high toxicity and often lead to drug resistance, highlighting the need for novel and more specific pharmacological therapies. The authors developed an integrated network pharmacology framework combining mechanistic and chemocentric approaches to predict potential drug combinations for cancer therapy. The results show paclitaxel as a suitable drug for combination therapy in many cancer types and identified several non-cancer-related genes as potential candidates for cancer pharmacological treatment.
Review
Medicine, Research & Experimental
Yau-Tuen Chan, Yuanjun Lu, Junyu Wu, Cheng Zhang, Hor-Yue Tan, Zhao-xiang Bian, Ning Wang, Yibin Feng
Summary: CRISPR-Cas9 is a powerful gene editing tool that allows high-precision genetic engineering of the genomes of all organisms. The latest advancements include genome library screening, which can detect survival-essential and drug resistance genes. This technology has various applications in anti-cancer drug discovery.
Review
Chemistry, Medicinal
Guoqing Fang, Hongjuan Chen, Zhiyun Cheng, Zilong Tang, Yichao Wan
Summary: Heterocycles, especially azaindole derivatives, have become important sources of kinase inhibitors for drug design, due to their ability to form hydrogen bonds in ATP-binding sites. This review focuses on the recent development of azaindole derivatives as potential kinase inhibitors, targeting various kinases such as AAK1, ALK, AXL, Cdc7, CDKs, DYRK1A, FGFR4, PI3K, and PIM kinases. The structure-activity relationships and binding modes of these derivatives are also elucidated. This review provides insights for medicinal chemists in the rational design of more potent kinase inhibitors with the azaindole scaffold.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Cell Biology
Hong Dai, Razack Abdullah, Xiaoqiu Wu, Fangfei Li, Yuan Ma, Aiping Lu, Ge Zhang
Summary: Pancreatic cancer is a lethal cancer with limited effectiveness of current chemotherapy. Nucleic acid-based targeting therapies have shown promising progress in the treatment of pancreatic cancer, offering potential as a future treatment direction.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2022)
Article
Medicine, Research & Experimental
Federica Laudisi, Teresa Pacifico, Claudia Maresca, Anderson Luiz-Ferreira, Sara Antonelli, Angela Ortenzi, Alfredo Colantoni, Antonio Di Grazia, Eleonora Franze, Marco Colella, Davide Di Fusco, Giuseppe S. Sica, Ivan Monteleone, Giovanni Monteleone, Carmine Stolfi
Summary: Colorectal cancer is a major cause of cancer-related death, and current treatments are not effective against advanced disease. Researchers have found that the anthelmintic drug rafoxanide can enhance the sensitivity of colorectal cancer cells to TRAIL, a targeted therapy. This discovery suggests that rafoxanide could be a potential treatment option for overcoming TRAIL resistance in colorectal cancer.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Review
Pharmacology & Pharmacy
Raef Shams, Yoshihiro Ito, Hideyuki Miyatake
Summary: mTOR is a protein kinase involved in cell growth and proliferation, which can be assembled into mTORC1 and mTORC2 complexes with different functions. In cancer cells, mTOR is hyperactivated to adapt to stress conditions, leading to efforts in developing compounds to inhibit mTOR and disrupt cancer cell metabolism.
PHARMACOLOGY & THERAPEUTICS
(2022)
Article
Oncology
Venkateshwar Madka, Arielle De La Cruz, Gopal Pathuri, Janani Panneerselvam, Yuting Zhang, Nicole Stratton, Sean Hacking, Niklas K. Finnberg, Howard P. Safran, Shizuko Sei, Elizabeth R. Glaze, Robert Shoemaker, Jennifer Fox, Alexander G. Raufi, Wafik S. El-Deiry, Chinthalapally Rao
Summary: The small molecule ONC201/TIC10 has shown great potential for preventing colorectal cancer (CRC). In a preclinical model representing high-risk familial adenomatous polyposis (FAP) patients, ONC201 demonstrated a strong suppressive effect on the development of intestinal tumors in male and female mice.
AMERICAN JOURNAL OF CANCER RESEARCH
(2022)
Article
Biotechnology & Applied Microbiology
Shigao Huang, Cheng Jiang, Muhammad Jameel Mughal, Guanyu Wang, Fuqiang Xing
Summary: An efficient in vivo drug screening platform based on FRET technique was established. Cancer cell lines expressing FRET-based caspase-3 sensor were validated in zebrafish embryos and nude mice models, showing effectiveness in detecting drug-induced cell death. The platform has the potential to improve drug screening efficiency through in vivo imaging.
FRONTIERS IN BIOENGINEERING AND BIOTECHNOLOGY
(2022)
Article
Immunology
Li Wang, Michael A. Crackower, Hao Wu
Summary: Inflammasome proteins are important drug targets for many diseases, but their drug discovery has been difficult due to challenges in solving high-resolution structures. Recent advances in the structural biology of NLRP3 and NLRP1 offer hope for structure-based drug design.
JOURNAL OF EXPERIMENTAL MEDICINE
(2022)
Article
Chemistry, Medicinal
Angela Takacs, Zsofia Szasz, Marton Kalabay, Peter Barany, Antal Csampai, Hargita Hegyesi, Orsolya Lang, Eszter Lajko, Laszlo Kohidai
Summary: The study demonstrated the synergistic effect of BOZ and TIC10 in tumor cells, resulting in reduced dosage, improved efficacy, and decreased side effects. The combination treatment led to increased apoptosis and enhanced expression of death receptor 5 (DR5) on the cell surface.
Article
Biochemistry & Molecular Biology
Zhenjiang Zhang, Sagar B. Patel, Michael R. King
Summary: A novel type of nanomaterial, MILs, was prepared to sensitize cancer cells to TRAIL and increase the water solubility of PL. MILs successfully loaded micelles inside the liposomal core and achieved sustained release of PL. The potent synergistic apoptotic effect in cancer cells by PL MILs in combination with liposomal TRAIL was also demonstrated.
Review
Biochemistry & Molecular Biology
Ravian L. van Ineveld, Esmee J. van Vliet, Ellen J. Wehrens, Maria Alieva, Anne C. Rios
Summary: This article introduces the importance and potential applications of 3D imaging in cancer research. 3D imaging provides more accurate information about the cellular composition and structure of cancer, and offers new strategies and methods for cancer treatment and patient diagnosis.
Article
Biochemistry & Molecular Biology
John R. Frost, Nicholas T. Jacob, Louis J. Papa, Andrew E. Owens, Rudi Fasan
ACS CHEMICAL BIOLOGY
(2015)
Article
Chemistry, Medicinal
Bin Zhou, Lisa M. Eubanks, Nicholas T. Jacob, Beverly Ellis, Amanda J. Roberts, Kim D. Janda
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2016)
Article
Chemistry, Medicinal
Nicholas T. Jacob, Jonathan W. Lockner, Joel E. Schlosburg, Beverly A. Ellis, Lisa M. Eubanks, Kim D. Janda
JOURNAL OF MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Organic
Kensaku Anraku, Shun Sato, Nicholas T. Jacob, Lisa M. Eubanks, Beverly A. Ellis, Kim D. Janda
ORGANIC & BIOMOLECULAR CHEMISTRY
(2017)
Article
Biochemistry & Molecular Biology
Nicholas T. Jacob, Pedro O. Miranda, Ryan J. Shirey, Ritika Gautam, Bin Zhou, M. Elena de Orbe Izquierdo, Mark S. Hixon, Jonathan R. Hart, Lynn Ueno, Peter K. Vogt, Kim D. Janda
BIOORGANIC & MEDICINAL CHEMISTRY
(2018)
Article
Chemistry, Medicinal
Pedro O. Miranda, Beatrice Cubitt, Nicholas T. Jacob, Kim D. Janda, Juan C. de la Torre
ACS INFECTIOUS DISEASES
(2018)
Article
Biochemistry & Molecular Biology
John R. Frost, Francesca Vitali, Nicholas T. Jacob, Micah D. Brown, Rudi Fasan
Article
Chemistry, Multidisciplinary
NIcholas T. Jacob, Kensaku Anraku, Atsushi Kimishima, Bin Zhou, Karen C. Collins, Jonathan W. Lockner, Beverley A. Ellis, Kim D. Janda
CHEMICAL COMMUNICATIONS
(2017)