Review
Medicine, Research & Experimental
Tapan Behl, Amit Gupta, Aayush Sehgal, Ali Albarrati, Mohammed Albratty, Abdulkarim M. Meraya, Asim Najmi, Saurabh Bhatia, Simona Bungau
Summary: Type 2 diabetes is a widely spread metabolic disorder with limitations in conventional therapies. Protein tyrosine phosphatase is a promising therapeutic target, and various inhibitors have shown effectiveness in managing diabetes.
BIOMEDICINE & PHARMACOTHERAPY
(2022)
Article
Biochemistry & Molecular Biology
Sonia Rocha, Mariana Lucas, Vera L. M. Silva, Pedro M. O. Gomes, Artur M. S. Silva, Alberto N. Araujo, Natalia Aniceto, Rita C. Guedes, M. Luisa Corvo, Eduarda Fernandes, Marisa Freitas
Summary: This study evaluated a library of 22 pyrazole compounds against human PTP1B activity, identifying two potent inhibitors and highlighting the importance of additional benzene rings in enhancing PTP1B inhibition. The most active compounds showed selectivity over TCPTP and molecular docking analyses revealed key residue contacts. This study represents a significant step in the design of novel PTP1B inhibitors.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Review
Oncology
Pei-Jie Chen, Yun-Tian Zhang
Summary: Tyrosine phosphorylation is a reversible process regulated by protein tyrosine kinases and phosphatases. Abnormalities in these proteins, such as PTP1B, can contribute to the development of diseases including cancer. Recent studies have shown that PTP1B plays an important role in cancer initiation and progression, making it a potential target for cancer therapies. This review focuses on the functions and pharmacological effects of PTP1B in different types of cancer.
CURRENT CANCER DRUG TARGETS
(2022)
Article
Chemistry, Physical
Suresh Thareja, Sant Kumar Verma, Akhlesh Kumar Jain, Manoj Kumar, Tilak Raj Bhardwaj
Summary: In order to discover protein tyrosine phosphatase 1B (PTP1B) inhibitors, we designed novel biphenyl thiazolidinedione conjugates (8a-n) that met the criteria of drug-likeness. One of the derivatives, N-methyl benzoic acid derivative (8j), showed strong binding interactions with PTP1B and exhibited selectivity over other PTPs. The synthesized analogues (8a-n) demonstrated moderate to good PTP1B inhibitory activity and showed time-dependent in vivo efficacy.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Bo Jiang, Jiao Luo, Shuju Guo, Lijun Wang
Summary: In this study, molecules containing 2,4-thiazolidinedione and hydantoin were designed, synthesized and evaluated for PTP1B inhibitory potency. Compound 5a was identified as a potent PTP1B inhibitor with selectivity over TCPTP, leading to improvements in blood glucose levels, insulin sensitivity, liver glycogen storage, and pancreatic islet structure in diabetic mice. These results suggest that compound 5a could be a promising lead compound for new antidiabetic drug discovery.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Ming-Fo Hsu, Yoshihiro Ito, Jai Prakash Singh, Shu-Fang Hsu, Alan Wells, Kuang-Yu Jen, Tzu-Ching Meng, Fawaz G. Haj
Summary: This study identified alpha-actinin4 as a novel substrate of PTP1B in podocytes and demonstrated their interaction in regulating podocyte function. Targeting PTP1B and alpha-actinin4 could be a potential therapeutic approach for podocyte injury.
BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH
(2024)
Article
Biochemistry & Molecular Biology
Sukhbir Singh, Ajmer Singh Grewal, Rupanshi Grover, Neelam Sharma, Bhawna Chopra, Ashwani Kumar Dhingra, Sandeep Arora, Sonika Redhu, Viney Lather
Summary: This review provides an overview of type 2 diabetes, the role of PTP1B in metabolic disorders, and recent developments in PTP1B inhibitors. Extensive literature search reveals various molecules that inhibit PTP1B, but only a few have entered clinical trials and were later withdrawn due to their unsatisfactory effectiveness and adverse effects. Developing potent, selective, and safe PTP1B inhibitors remains crucial.
BIOORGANIC CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Mohd Saeed, Ambreen Shoaib, Munazzah Tasleem, Nadiyah M. Alabdallah, Md Jahoor Alam, Zeina El Asmar, Qazi Mohammad Sajid Jamal, Fevzi Bardakci, Saad S. Alqahtani, Irfan Ahmad Ansari, Riadh Badraoui
Summary: Diabetes mellitus is a major global public health issue, requiring the search for safe and effective drugs. Shikonin may serve as an anti-diabetic agent, showing competitive inhibitory effects on PTP1B, and has the potential to be a source for the production of preventive and therapeutic agents.
Review
Biochemistry & Molecular Biology
Maryam Teimouri, Hossein Hosseini, Zahra ArabSadeghabadi, Reyhaneh Babaei-Khorzoughi, Sattar Gorgani-Firuzjaee, Reza Meshkani
Summary: This article highlights the importance of PTP1B in type 2 diabetes mellitus and its potential as a target for therapeutic interventions. PTP1B negatively regulates the insulin receptor signaling pathway, leading to insulin resistance. PTP1B inhibitors have shown promise in improving insulin receptor sensitivity and may be effective in treating insulin resistance-related diseases.
JOURNAL OF PHYSIOLOGY AND BIOCHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Kira V. V. Derkach, Maxim A. A. Gureev, Anastasia A. A. Babushkina, Vladimir N. N. Mikhaylov, Irina O. O. Zakharova, Andrey A. A. Bakhtyukov, Viktor N. N. Sorokoumov, Alexander S. S. Novikov, Mikhail Krasavin, Alexander O. O. Shpakov, Irina A. A. Balova
Summary: This article describes the identification of dual inhibitors of protein phosphotyrosine phosphatase 1B (PTP1B)/T-cell protein phosphotyrosine phosphatase (TC-PTP) based on the 3-(hydroxymethyl)-4-oxo-1,4-dihydrocinnoline scaffold. The compounds were evaluated for their effects on obesity-related parameters and gene expressions. The results indicate the potential of these compounds as dual inhibitors for the treatment of metabolic disorders.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Multidisciplinary
Jinmin Miao, Jiajun Dong, Yiming Miao, Yunpeng Bai, Zihan Qu, Brenson A. Jassim, Bo Huang, Quyen Nguyen, Yuan Ma, Allison A. Murray, Jinyue Li, Philip S. Low, Zhong-Yin Zhang
Summary: In this study, researchers discovered the first highly potent and selective TC-PTP degrader called TP1L, which can induce degradation of TC-PTP and enhance T-cell signaling and tumor killing efficacy.
Article
Plant Sciences
Xiao Zhou, Lin Lin Wang, Wen Jing Tang, Biao Tang
Summary: The study demonstrated that AST IV effectively improved insulin resistance in HepG2 cells and reduced triglyceride accumulation in OA-treated HepG2 cells by inhibiting PTP1B.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Patricia Sanchez-Alonso, Mercedes Griera, Javier Garcia-Marin, Manuel Rodriguez-Puyol, Ramon Alajarin, Juan J. Vaquero, Diego Rodriguez-Puyol
Summary: Novel compounds targeting PTP1B as potential therapeutics for diabetes and other diseases have been synthesized, showing inhibitory activity against the enzyme and potential insulin mimetic effects in cells.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Review
Biochemistry & Molecular Biology
Kaushik Roychoudhury, Rashmi S. Hegde
Summary: This review focuses on the haloacid dehalogenase (HAD) class of protein phosphatases, particularly the unique group of enzymes known as the eyes absent (EYA) family. EYA proteins are structurally and mechanistically classified as HAD enzymes, but they function as protein tyrosine phosphatases (PTPs) and do not use a Cysteine residue as a nucleophile in their dephosphorylation reaction. The article provides an overview of HAD phosphatase structure-function, describes the unique features of the EYA family and their tyrosine phosphatase activity, summarizes the known substrates and cellular functions of EYA proteins, and speculates about the evolutionary origins of the EYA family of proteins.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Miriam Diaz-Rojas, Huzefa Raja, Martin Gonzalez-Andrade, Jose Rivera-Chavez, Manuel Rangel-Grimaldo, Isabel Rivero-Cruz, Rachel Mata
Summary: Three undescribed compounds, named alboluteins A-C, were isolated from solid rice-based cultures of Malbranchea albolutea. These compounds showed inhibitory activity against PTP1B, with albolutein C behaving as a noncompetitive inhibitor. Docking and molecular dynamic studies indicated that the compounds prefer to bind at the allosteric site of the enzyme, providing insights into their mechanism of action.
Article
Biochemistry & Molecular Biology
Laxmi Banjare, Yogesh Singh, Sant Kumar Verma, Atul Kumar Singh, Pradeep Kumar, Shashank Kumar, Akhlesh Kumar Jain, Suresh Thareja
Summary: This study investigated a series of biphenyl bearing molecules with a wide range of aromatase inhibitory activity using a multifaceted approach including 3D-QSAR analysis, molecular docking, molecular dynamic simulations, and pharmacophore mapping. The results showed that the force field-based 3D-QSAR model was the best in terms of fitness, and the generated pharmacophoric features were able to explain the variation in biological activity. The findings offer guidance for designing potent biphenyl derivatives as aromatase inhibitors.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Chemistry, Multidisciplinary
Honey Goel, Vinni Kalra, Sant Kumar Verma, Sunil Kumar Dubey, Ashok Kumar Tiwary
Summary: The brain, a complex and delicate organ, presents challenges in treating central nervous system disorders mainly due to the blood-brain barrier. Current approaches for CNS disorders face limitations, and intranasal delivery may provide a new way to overcome these challenges.
JOURNAL OF CONTROLLED RELEASE
(2022)
Review
Environmental Sciences
Saptarshy Sarkar, Sukhbir Singh Gill, Ghanshyam Das Gupta, Sant Kumar Verma
Summary: Water is essential for human use, but the presence of toxicants in water caused by urbanization, industrialization, chemical use, and human ignorance poses a threat to both ecosystems and human health. This article discusses the determination techniques for water pollutants and remediation techniques to control toxicants.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2022)
Article
Biochemistry & Molecular Biology
Yogesh Singh, Shalini Jaswal, Satwinder Singh, Sant Kumar Verma, Suresh Thareja
Summary: The study used molecular docking and 3D-QSAR analysis to identify lead structures for dual aromatase-steroid sulfatase inhibitors (DASIs) and revealed their specific interactions with aromatase and steroid sulfatase. These findings can be used for drug candidate optimization in the treatment of hormone-dependent breast cancer.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2022)
Article
Chemistry, Physical
Suresh Thareja, Sant Kumar Verma, Akhlesh Kumar Jain, Manoj Kumar, Tilak Raj Bhardwaj
Summary: In order to discover protein tyrosine phosphatase 1B (PTP1B) inhibitors, we designed novel biphenyl thiazolidinedione conjugates (8a-n) that met the criteria of drug-likeness. One of the derivatives, N-methyl benzoic acid derivative (8j), showed strong binding interactions with PTP1B and exhibited selectivity over other PTPs. The synthesized analogues (8a-n) demonstrated moderate to good PTP1B inhibitory activity and showed time-dependent in vivo efficacy.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Ankush Kharyal, Sanjeev Ranjan, Shalini Jaswal, Darakhshan Parveen, Ghanshyam Das Gupta, Suresh Thareja, Sant Kumar Verma
Summary: Diabetes-associated complications are a major global health concern, and aldose reductase inhibitors have been proposed as a viable strategy for dealing with these complications. This review provides a comprehensive insight into the development and medicinal chemistry of 2,4-thiazolidinedione (TZD) and rhodanine derivatives as aldose reductase inhibitors. The review discusses the synthetic strategies, structure-activity relationships (SAR), and binding mode of various compounds, with a focus on optimizing/designing potent target-specific inhibitors for the treatment of diabetic complications.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Analytical
Sitanshu Mondal, Vivek Asati, Sant Kumar Verma, Ghanshyam Das Gupta, Balak Das Kurmi, Preeti Patel
Summary: A trustworthy high-performance liquid chromatography approach was developed using quality by design for simultaneous measurement of cefepime and sulbactam. Chromatographic settings that ensure quality peaks and component separation within a manageable run time were determined. Critical quality attributes were evaluated to establish an analytical design space and control strategy. The independent parameters in the mathematical models were acetonitrile volume, trimethylamine volume, and flow rate. The ideal conditions were found to be the mobile phase of acetonitrile:high-performance liquid chromatography water:triethylamine at a ratio of 50.0:50:0.15 (v/v/v), pH 6.0 adjusted with orthophosphoric acid, and a flow rate of 1.1 ml/min. The developed method provided appropriate baseline separation of both drugs within approximately 10 minutes with high percent recoveries and low relative standard deviations.
SEPARATION SCIENCE PLUS
(2023)
Review
Chemistry, Medicinal
Shivanshu Pandey, Sitanshu Mondal, Kumari Kajal, Balak Das Kurmi, Sant Kumar Verma, Preeti Patel
Summary: Despite advancements in cancer research and therapy, breast cancer remains a complex health crisis for women and a top priority in biomedical research. It is a highly heterogeneous disease and the leading cause of death among women worldwide. The incidence and mortality rates of breast cancer have been gradually increasing. Common treatment options include chemotherapy, endocrine therapy, immunotherapy, radiotherapy, and surgery. The article reviews different targets associated with breast cancer and summarizes the progress in research on synthesized inhibitors as anti-breast cancer agents from 2015 to 2021. It aims to provide insights for designing novel compounds for breast cancer therapy.
ARCHIV DER PHARMAZIE
(2023)
Review
Chemistry, Physical
Priya, Shalini Jaswal, Ghanshyam Das Gupta, Sant Kumar Verma
Summary: Aurora kinase family plays a critical role in cell division and the cell cycle, and overexpression of AURKA and AURKB has been linked to the development of various carcinomas. The synthesis and development of Aurora Kinase inhibitors offer new opportunities for anticancer therapy.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Editorial Material
Pharmacology & Pharmacy
Arshdeep Chopra, Yogindra Kumari, Sant Kumar Verma, Rohit Bhatia
CURRENT PHARMACEUTICAL ANALYSIS
(2023)
Article
Biochemistry & Molecular Biology
Priyadarshi Gautam, Priya Bisht, Anupam Gautam, Ghanshyam Das Gupta, Rajveer Singh, Sant Kumar Verma
Summary: This study uses structure-guided alignment-dependent 3D-QSAR to investigate compounds with thiazolidine-2,4-dione scaffold as potential aldose reductase inhibitors. Compound 65 exhibits higher stability and binding energy, indicating better activity against aldose reductase. These findings provide valuable insights for rational compound design with improved aldose reductase activity.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Biochemistry & Molecular Biology
Anushka Sharma, Rahul Dubey, Ritu Bhupal, Preeti Patel, Sant Kumar Verma, Savas Kaya, Vivek Asati
Summary: Diabetes Mellitus (DM) is a common global disease caused by high glucose consumption. Inhibiting enzymes such as α-amylase and α-glucosidase is an effective therapeutic approach for the development of antidiabetic drugs. Medicinally privileged triazole structures, specifically 1,2,3-triazol and 1,2,4-triazoles, fused with other heterocyclic rings, have shown promising antidiabetic activity. This review summarizes the structure-activity relationship, enzyme inhibitory activity, and patents filed of these scaffolds as alpha-amylase and alpha-glucosidase inhibitors.
MOLECULAR DIVERSITY
(2023)
Review
Biochemistry & Molecular Biology
Megha Goswami, Priya, Shalini Jaswal, Ghanshyam Das Gupta, Sant Kumar Verma
Summary: Phytosterols, including stigmasterol, are bioactive substances found in plant foods. Stigmasterol has various biological effects such as antioxidant, anticancer, and lipid-lowering effects, making it a potential supplement for related illnesses. However, further clinical studies are needed before it can be used therapeutically.
Review
Environmental Sciences
Sukhbir Singh Gill, Tanish Goyal, Megha Goswami, Preeti Patel, Ghanshyam Das Gupta, Sant Kumar Verma
Summary: Carbonaceous materials, including carbon nanotubes, fullerene, graphene, graphene oxide, carbon nanofiber nanospheres, and activated carbon, have effective adsorption and photocatalytic properties, making them ideal for removing emerging and persistent inorganic/organic contaminants, heavy metals, and radionucleotides from the environment. This review provides comprehensive insights into the mechanisms, efficiencies, applications, advantages, and shortcomings of using carbonaceous materials for the remediation of environmental toxicants. Opportunities and challenges associated with carbon materials are discussed, offering future perspectives in the field.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)
Review
Environmental Sciences
Tanish Goyal, Sukhwinder Singh, Ghanshyam Das Gupta, Sant Kumar Verma
Summary: The contamination of ecosystems by microplastics has become a global concern, as their presence has been found in the atmosphere, food items, and soil ecosystems. They are abundant in various environments, including seawater, beach sand, drinking water, agricultural soils, wastewater treatment plant effluent, and the atmosphere. This review highlights the potential sources of microplastics, their effects on human health, and the need for guidelines and specifications for controlling their presence in the environment.
ENVIRONMENTAL SCIENCE AND POLLUTION RESEARCH
(2023)