Review
Cell Biology
Morgane Lallier, Louise Marchandet, Brice Moukengue, Celine Charrier, Marc Baud'huin, Franck Verrecchia, Benjamin Ory, Francois Lamoureux
Summary: Osteosarcoma is the most common form of primary bone tumor affecting children and young adults, with a 5-year survival rate of 70%. Heat Shock Proteins play a significant role in cell proliferation, apoptosis inhibition, migration, and drug resistance in osteosarcoma. By studying HSP27, HSP60, HSP70, and HSP90, they can serve as potential clinical uses in osteosarcoma.
Review
Pharmacology & Pharmacy
Puhua Wu, Yan Zhou, Yizhen Guo, Shao-Lin Zhang, Kin Yip Tam
Summary: MCTs play a crucial role in lactate/proton efflux and may serve as a new target for anticancer therapies. While X-ray co-crystal structures of human MCTs with inhibitors are unavailable, homology models have aided in the design of new MCT inhibitors. Future directions include studying the structures and functions of MCT inhibitors and discovering more small-molecule inhibitors.
DRUG DISCOVERY TODAY
(2021)
Article
Cell & Tissue Engineering
Ju-Fang Liu, Po-Chun Chen, Thai-Yen Ling, Chun-Han Hou
Summary: This study demonstrates that heat shock induces the expression of HSPs in hPDMCs through the activation of ROS, p38 MAPK, Akt signaling, and HSF1, which plays a protective role.
STEM CELL RESEARCH & THERAPY
(2022)
Article
Chemistry, Inorganic & Nuclear
Alexander Kastner, Theresa Mendrina, Florian Bachmann, Walter Berger, Bernhard K. Keppler, Petra Heffeter, Christian R. Kowol
Summary: In this study, oxaliplatin(iv)-based complexes were developed as platinum(iv) prodrugs to release aspirin, which has shown antitumor activity against colon cancer. The newly synthesized complex demonstrated increased reduction stability compared to a cisplatin analog and exhibited desired prodrug properties in cell culture. A derivative with albumin-binding properties showed improved pharmacokinetics and tumor accumulation, leading to enhanced antitumor activity and overall survival in tumor-bearing mice.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Oncology
Sangah Lee, Jiyae Jung, Yu-Jin Lee, Seon-Kyu Kim, Jung-Ae Kim, Bo-Kyung Kim, Kyung Chan Park, Byoung-Mog Kwon, Dong Cho Han
Summary: The study identified HSF1 as a potential target protein to overcome EGFR-TKI resistance in NSCLC, demonstrating the efficacy of HSF1 inhibition in vitro and in vivo. This suggests a targetable HSF1 pathway to overcome multiple mechanisms of EGFR-TKI resistance.
Article
Chemistry, Medicinal
Zongbao Ding, Wei Pan, Yao Xiao, Binbin Cheng, Gang Huang, Jianjun Chen
Summary: DK1 is a novel DNA-PK inhibitor with great potential for further study. It has favorable drug-like properties and in vivo pharmacokinetics as an oral drug candidate. When used in combination with doxorubicin, DK1 shows synergistic antiproliferative activity against various cancer cell lines.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Magdalena Peruzynska, Aleksandra Borzyszkowska-Ledwig, Jacek G. Sosnicki, Lukasz Struk, Tomasz J. Idzik, Gabriela Maciejewska, Lukasz Skalski, Katarzyna Piotrowska, Pawel Lukasik, Marek Drozdzik, Mateusz Kurzawski
Summary: This study successfully obtained a mitotic-specific inhibitor with high antiproliferative activity and selectivity through structural modifications. By inhibiting tubulin polymerization in a dose-dependent manner, aberrant mitotic spindle formation was induced, leading to cell cycle arrest and apoptosis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Chiranjeev Sharma, Myeong A. Choi, Yoojin Song, Young Ho Seo
Summary: In this study, heterobifunctional small molecules were designed and synthesized, which combine HSF1 inhibitor and anticancer drug through E3 ligase-mediated proteolysis, selectively degrading cancerous proteins.
Review
Oncology
Shefali Shukla, Anantpreet K. Sood, Kartika Goyal, Ambika Singh, Vaidehi Sharma, Neha Guliya, Shikha Gulati, Sanjay Kumar
Summary: This review discusses the anticancer activity of chalcones and their potential mechanisms of action. Research has shown that chalcone analogs with specific functional groups have promising anticancer properties following various pathways.
ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Multidisciplinary
Ashraf A. Abbas, Kamal M. Dawood
Summary: The benzofuran moiety is a key component in numerous biologically active natural and synthetic heterocycles. These heterocycles exhibit unique therapeutic potential and are implicated in various clinical drugs. Recent studies have confirmed the exceptional inhibitory potency of benzofurans against human cancer cell lines compared to reference anticancer drugs. Several publications have focused on the anticancer properties of benzofuran-based heterocycles. This review comprehensively covers the latest developments in the anticancer activities of natural and synthetic benzofuran scaffolds from 2019 to 2022, highlighting their potential as promising candidates for anticancer agents.
Review
Biochemistry & Molecular Biology
Laila Rubab, Sumbal Afroz, Sajjad Ahmad, Saddam Hussain, Iram Nawaz, Ali Irfan, Fozia Batool, Katarzyna Kotwica-Mojzych, Mariusz Mojzych
Summary: Coumarin is an important pharmacophore with diverse biological activities. Coumarin sulfonamide compounds have shown great development potential as clinical drugs for various diseases. This review discusses the recent progress in the synthesis and medicinal chemistry of coumarin sulfonamide-based compounds, particularly in the field of oncology and carbonic anhydrase inhibitors.
Article
Biochemistry & Molecular Biology
Natalie Oberhuber, Hindole Ghosh, Bianca Nitzsche, Prasad Dandawate, Michael Hoepfner, Rainer Schobert, Bernhard Biersack
Summary: New N-alkylindole-substituted 2-(pyrid-3-yl)-acrylonitriles and their (p-cymene)Ru(II) piano-stool complexes were synthesized and found to exhibit potent antiproliferative activity in various cancer models. Some of the derivatives showed lower IC50 values than clinically relevant multikinase inhibitors gefitinib and sorafenib, indicating their potential as novel therapeutic agents for cancer treatment. The investigation of drug mechanism in HCT-116 p53-knockout colon cancer cells revealed that the derivatives induced apoptotic caspase-3/7 activity, ROS formation, and anti-angiogenic properties.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Julia Krzywik, Maral Aminpour, Jan Janczak, Ewa Maj, Mahshad Moshari, Witold Mozga, Joanna Wietrzyk, Jack A. Tuszynski, Adam Huczynski
Summary: Colchicine and its derivatives exhibit high cytotoxicity against cancer cells, with their mode of action believed to involve binding to the colchicine site at the molecular level.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Pharmacology & Pharmacy
Motahareh Mortazavi, Elaheh Raufi, Tahereh Damghani, Mehdi Khoshneviszadeh, Najmeh Edraki, Masoomeh Eskandari, Elisa Giovannetti, Godefridus J. Peters, Somayeh Pirhadi, Omidreza Firuzi
Summary: c-Met receptor tyrosine kinase is an important therapeutic target in pancreatic cancer. A virtual screening and experimental testing were conducted to identify potential c-Met inhibitors from a compound library. The most active compound, PhTH, demonstrated antiproliferative effects against PDAC cells, induced apoptosis, and inhibited c-Met activity. Molecular docking and simulation analysis confirmed the strong interactions between PhTH and c-Met kinase domain. These findings suggest the potential of PhTH and other compounds as c-Met inhibitors in the treatment of PDAC.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Moataz A. Shaldam, Hadia Almahli, Andrea Angeli, Rehab Mustafa Badi, Eman F. Khaleel, Abdelrahman I. Zain-Alabdeen, Zainab M. Elsayed, Eslam B. Elkaeed, Rofaida Salem, Claudiu T. Supuran, Wagdy M. Eldehna, Haytham O. Tawfik
Summary: New isatin-based sulphonamides were synthesized as potential dual VEGFR-2 and carbonic anhydrase inhibitors with anticancer activities. The most potent derivatives showed strong VEGFR-2 inhibitory effect but failed to inhibit relevant CA isoforms. Two derivatives were further tested for their impact on cell cycle disturbance and apoptotic potential. Molecular modelling analyses were conducted to assess the binding mode and stability of the target compounds.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Shrawan Kumar Mangawa, Chiranjeev Sharma, Ashawani Kumar Singh, Satish K. Awasthi
Review
Biochemistry & Molecular Biology
Chiranjeev Sharma, Satish Kumar Awasthi
CHEMICAL BIOLOGY & DRUG DESIGN
(2017)
Article
Chemistry, Multidisciplinary
Chiranjeev Sharma, Ashawani K. Singh, Jyothish Joy, Eluvathingal D. Jemmis, Satish K. Awasthi
Article
Chemistry, Organic
Chiranjeev Sharma, Jyothish Joy, Munirathinam Nethaji, Eluvathingal D. Jemmis, Satish Kumar Awasthi
ASIAN JOURNAL OF ORGANIC CHEMISTRY
(2016)
Article
Chemistry, Multidisciplinary
Chiranjeev Sharma, Kumkum Sharma, Jitendra Kumar Yadav, Alka Agarwal, Satish Kumar Awasthi
Article
Multidisciplinary Sciences
Myeong A. Choi, Sun You Park, Hye Yun Chae, Yoojin Song, Chiranjeev Sharma, Young Ho Seo
SCIENTIFIC REPORTS
(2019)
Article
Biochemistry & Molecular Biology
Chiranjeev Sharma, Yong Jin Oh, Byoungduck Park, Sooyeun Lee, Chul-Ho Jeong, Sangkil Lee, Ji Hae Seo, Young Ho Seo
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2019)
Article
Chemistry, Multidisciplinary
Priyanka Yadav, Bhawana Sharma, Chiranjeev Sharma, Preeti Singh, Satish K. Awasthi
Review
Chemistry, Medicinal
Chiranjeev Sharma, Youllee Kim, Dohee Ahn, Sang J. Chung
Summary: This review provides a comprehensive overview of the relevance of Protein tyrosine phosphatases (PTPs) to type 2 diabetes (T2D) and the potential challenges for PTP inhibitors to be next generation antidiabetics. It briefly discusses the structure and function of PTPs, and presents their importance and relevance in various human diseases, with a focus on diabetes. Various small molecule inhibitors targeting PTPs relevant to T2D have been explored, including natural products, synthetic compounds, and antisense nucleic acids.
ARCHIVES OF PHARMACAL RESEARCH
(2021)
Article
Chemistry, Medicinal
TaeJin Lee, Ju Hwan Kim, Se Jeong Kwon, Jin Woo Seo, Sun Hee Park, Jinyoung Kim, Jonghwa Jin, Ji Hye Hong, Hyo Jin Kang, Chiranjeev Sharma, Ji Hoon Choi, Sang J. Chung
Summary: In this study, a new method for antibody conjugation was developed, which achieved site-selective modification using an Fc-binding peptide equipped with a 5-norbornene-2-carboxylic acid thioester. The resulting antibody-drug conjugates showed remarkable anticancer activity.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Chiranjeev Sharma, Myeong A. Choi, Yoojin Song, Young Ho Seo
Summary: In this study, heterobifunctional small molecules were designed and synthesized, which combine HSF1 inhibitor and anticancer drug through E3 ligase-mediated proteolysis, selectively degrading cancerous proteins.
Article
Biochemistry & Molecular Biology
Dickson Donu, Chiranjeev Sharma, Yana Cen
Summary: Inhibition of nicotinamidase in Plasmodium falciparum could potentially lead to the development of new antimalarial drugs. Studies have shown that a recently discovered compound is able to inhibit both the enzyme activity and replication of the parasite in infected human red blood cells. This suggests that nicotinamide salvage through nicotinamidase plays a crucial role in maintaining NAD(+) homeostasis in P. falciparum.
Review
Nutrition & Dietetics
Chiranjeev Sharma, Dickson Donu, Yana Cen
Summary: Nicotinamide riboside (NR), as a potent NAD(+) enhancement agent, has shown promising results in protecting against various pathological conditions such as neurodegenerative diseases, diabetes, and hearing loss.
Article
Chemistry, Medicinal
Preeti Singh, Chiranjeev Sharma, Bhawana Sharma, Anupam Mishra, Drishti Agarwal, Deepika Kannan, Jana Held, Shailja Singh, Satish K. Awasthi
Summary: This study reports a rapid method for synthesizing N-sulfonylpiperidine dispiro-1,2,4,5-tetraoxane analogs for antimalarial research. The synthesized compounds were characterized and evaluated for their in vitro and in vivo antimalarial activities.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
