Review
Biochemistry & Molecular Biology
Xiao-Jing Pang, Xiu-Juan Liu, Yuan Liu, Wen-Bo Liu, Yin-Ru Li, Guang-Xi Yu, Xin-Yi Tian, Yan-Bing Zhang, Jian Song, Cheng-Yun Jin, Sai-Yang Zhang
Summary: FAK, a nonreceptor intracellular tyrosine kinase, is overexpressed in many human cancer cell lines, promoting tumor growth by controlling various cellular functions. Targeting FAK with small molecule inhibitors is considered a promising cancer therapy, with several FAK inhibitors undergoing clinical trials in different phases. Additionally, the development of novel FAK inhibitors, including FAK degraders through PROTAC technology, provides potential for new anticancer agents.
Article
Medicine, Research & Experimental
Yueheng Qi, Ye Li, Yu Fang, Hang Gao, Bingchao Qiang, Shuxia Wang, Huabei Zhang
Summary: A series of 2,4-diaminopyrimidine derivatives labeled with F-18 were found to have potential as PET tumor imaging agents, with Q6 showing good inhibition of FAK activity and biodistribution in S180-bearing mice.
MOLECULAR PHARMACEUTICS
(2021)
Review
Oncology
Ximin Tan, Yuheng Yan, Bin Song, Shuangli Zhu, Qi Mei, Kongming Wu
Summary: Focal adhesion kinase (FAK) plays a crucial role in cellular functions and tumor microenvironment. Increased FAK expression and activity are strongly associated with unfavorable clinical outcomes and metastatic characteristics in cancer. Modulating FAK activity has potential as an effective approach in cancer therapy.
EXPERIMENTAL HEMATOLOGY & ONCOLOGY
(2023)
Article
Chemistry, Organic
Haitao Tian, Wenxuan Xue, Jingtao Wu, Ziguang Yang, Hongcheng Lu, Conghui Tang
Summary: A novel and highly-efficient N-heterocycle assembly methodology has been developed using a cobalt-N,N-bidentate complex as a catalyst. The cobalt complex, which is phosphine-free and easily-prepared, enables the synthesis of various N-heterocycles from readily available alcohols and amines through acceptorless dehydrogenation. The generality and practicability of this catalytic system are demonstrated by obtaining all N-heterocycles under nearly identical reaction conditions.
ORGANIC CHEMISTRY FRONTIERS
(2022)
Article
Oncology
Yumeng Zhang, Shu Liu, Shu Zhou, Dandan Yu, Junjie Gu, Qin Qin, Yu Cheng, Xinchen Sun
Summary: Oesophageal cancer is highly invasive and prone to recurrence and metastasis, with a low five-year survival rate, making the development of new therapeutic interventions crucial. Focal adhesion kinase (FAK) plays a key role in survival, proliferation, and migration of cancer cells, making it a potential therapeutic target for oesophageal cancer. The combination of FAK inhibitors with other treatments is expected to improve patient survival.
Review
Cell Biology
Johanne Le Coq, Ivan Acebron, Barbara Rodrigo Martin, Pilar Lopez Navajas, Daniel Lietha
Summary: In this review, the authors discuss the role of focal adhesion kinase (FAK) in cell-matrix adhesion and migration. They highlight the known structural features of FAK and the challenges in understanding its integration in the focal adhesion complex and the structural changes during focal adhesion maturation.
JOURNAL OF CELL SCIENCE
(2022)
Article
Engineering, Biomedical
Jefferson O. Abaricia, Arth H. Shah, Rene Olivares-Navarrete
Summary: Recent studies have shown that neutrophils regulate NET formation in response to physical and mechanical cues from biomaterials through integrin/FAK signaling pathways. Neutrophils on higher stiffness substrates exhibit increased NET formation and pro-inflammatory cytokine secretion, with fibronectin being the most potent inducer of NET formation in a stiffness-dependent manner. Inhibition of FAK activity abolishes the stiffness-dependent increase in NET formation and pro-inflammatory molecule secretion.
Article
Fisheries
Junjie Wan, Xuelin Zhao, Jiqing Liu, Kaiyu Chen, Chenghua Li
Summary: In this study, a novel SFK homologue (AjSrc) was identified in Apostichopus japonicus, which mediated Vibrio splendidus-induced coelomocytes' phagocytosis via interacting with focal adhesion kinase (AjFAK) and co-phosphorylation. This study enriched the mechanism of phagocytosis in echinoderm and provided a new theoretical foundation for disease control of sea cucumber.
FISH & SHELLFISH IMMUNOLOGY
(2022)
Review
Chemistry, Multidisciplinary
Adarsh Kumar, Kuber Kumar Bhagat, Ankit Kumar Singh, Harshwardhan Singh, Tanuja Angre, Amita Verma, Habibullah Khalilullah, Mariusz Jaremko, Abdul-Hamid Emwas, Pradeep Kumar
Summary: This study focuses on pyrido[2,3-d]pyrimidine derivatives as anticancer agents, which have emerged as a promising scaffold in medicinal chemistry with a broad spectrum of activities. The study covers the inhibition mechanisms, structure-activity relationship, and signaling pathways of these derivatives against various cancer targets. The review provides a comprehensive medicinal and pharmacological profile of pyrido[2,3-d]pyrimidines and offers insights for designing new selective, effective, and safe anticancer agents.
Article
Microbiology
Leny Jose, Jessica Gonzalez, Emma Kessinger, Elliot J. Androphy, Marsha Desmet
Summary: This study reveals that focal adhesion kinase (FAK) can control the replication of human papillomavirus (HPV) genome through its interaction and phosphorylation of the E2 protein, thus preventing over-replication of the viral genome.
Article
Oncology
Mulu Geletu, Hanad Adan, Maximillian Niit, Rozanne Arulanandam, Esther Carefoot, Victoria Hoskin, Diana Sina, Bruce Elliott, Patrick Gunning, Leda Raptis
Summary: Cell-to-cell adhesion mediated by cadherins activates Stat3, while adhesion to the ECM activates FAK, Src, RTKs, PI3k/Akt, and Ras/Erk pathways. Cell density affects FAK and Akt activity, with FAK playing an important role in Akt activation.
EXPERIMENTAL CELL RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Jingnan Huang, Natalie J. Jooss, Delia Fernandez, Albert Sickmann, Angel Garcia, Kanin Wichapong, Ingrid Dijkgraaf, Johan W. M. Heemskerk
Summary: This study reveals a shear-dependent signaling axis of PTK2, integrin alpha IIb beta 3, and CIB1 in collagen- and GPVI-dependent thrombus formation, which is modulated by GPR56.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Cell Biology
Jinling Dong, Haiyan Zhou, Yongjie Li, Rong Li, Ni Chen, Youkun Zheng, Xin Deng, Mao Luo, Jianbo Wu, Liqun Wang
Summary: The study demonstrated that rhMG53 inhibits angiogenesis by regulating the FAK/Src/Akt/ERK1/2 signaling pathways, impacting endothelial cell function and postnatal mouse retinal neovascularization.
JOURNAL OF CELLULAR AND MOLECULAR MEDICINE
(2021)
Review
Pharmacology & Pharmacy
Patricia A. Quispe, Martin J. Lavecchia, Ignacio E. Leon
Summary: In this article, we review the strategies used to inhibit FAK activity in solid tumors and provide an overview of the preclinical and clinical studies on FAK inhibitors.
DRUG DISCOVERY TODAY
(2022)
Article
Biochemistry & Molecular Biology
Lalit Kumar Sharma, Mi Kyung Yun, Chitra Subramanian, Rajendra Tangallapally, Suzanne Jackowski, Charles O. Rock, Stephen W. White, Richard E. Lee
Summary: Optimization and synthesis of a new series of PANK inhibitors led to the discovery of potent drug-like molecules with excellent inhibitory effects and well-defined structure-activity relationships, offering potential targets for treating neurological and metabolic disorders.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
