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Article ; Online: The Journey of Thiazolidinediones as Modulators of PPARs for the Management of Diabetes: A Current Perspective.

Ahsan, Waquar

2019 Volume 25, Issue 23, Page(s) 2540–2554

Abstract: Peroxisome Proliferator-Activated Receptors (PPARs) also known as glitazone receptors are a family of receptors that regulate the expression of genes and have an essential role in carbohydrate, lipid and protein metabolism apart from other functions. ... ...

Abstract	Peroxisome Proliferator-Activated Receptors (PPARs) also known as glitazone receptors are a family of receptors that regulate the expression of genes and have an essential role in carbohydrate, lipid and protein metabolism apart from other functions. PPARs come in 3 sub-types: PPAR-α, PPAR-β/δ and PPAR-γ - with PPAR-γ having 2 isoforms - γ1 and γ2. Upon activation, the PPARs regulate the transcription of various genes involved in lipid and glucose metabolism, adipocyte differentiation, increasing insulin sensitivity, prevention of oxidative stress and to a certain extent, modulation of immune responses via macrophages that have been implicated in the pathogenesis of insulin resistance. Hence, PPARs are an attractive molecular target for designing new anti-diabetic drugs. This has led to a boost in the research efforts directed towards designing of PPAR ligands - particularly ones that can selectively and specifically activate one or more of the PPAR subtypes. Though, PPAR- γ full agonists such as Thiazolidinediones (TZDs) are well established agents for dyslipidemia and type 2 diabetes mellitus (T2D), the side effect profile associated with TZDs has potentiated an imminent need to come up with newer agents that act through this pathway. Several newer derivatives having TZD scaffold have been designed using structure based drug designing technique and computational tools and tested for their PPAR binding affinity and efficacy in combating T2D and some have shown promising activities. This review would focus on the role of PPARs in the management of T2D; recently reported TZD derivatives which acted as agonists of PPAR- γ and its subtypes and are potentially useful in the new drug discovery for the disease.
MeSH term(s)	Diabetes Mellitus, Type 2/drug therapy ; Humans ; Hypoglycemic Agents/therapeutic use ; Insulin Resistance ; PPAR gamma/antagonists & inhibitors ; Thiazolidinediones/therapeutic use
Chemical Substances	Hypoglycemic Agents ; PPAR gamma ; Thiazolidinediones
Language	English
Publishing date	2019-07-22
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	1304236-1
ISSN	1873-4286 ; 1381-6128
ISSN (online)	1873-4286
ISSN	1381-6128
DOI	10.2174/1381612825666190716094852
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Article ; Online: Development of erlotinib-loaded nanotransferosomal gel for the topical treatment of ductal carcinoma

Mangla, Bharti / Mittal, Priya / Kumar, Pankaj / Javed, Shamama / Ahsan, Waquar / Aggarwal, Geeta

Nanomedicine (London, England)

2024 Volume 19, Issue 10, Page(s) 855–874

Abstract: Aims: ...

Abstract	Aims:
MeSH term(s)	Humans ; Female ; Erlotinib Hydrochloride/therapeutic use ; Carcinoma, Intraductal, Noninfiltrating ; Cell Line, Tumor ; Liposomes ; Breast Neoplasms/drug therapy
Chemical Substances	Erlotinib Hydrochloride (DA87705X9K) ; Liposomes
Language	English
Publishing date	2024-03-05
Publishing country	England
Document type	Journal Article
ZDB-ID	2277839-1
ISSN	1748-6963 ; 1743-5889
ISSN (online)	1748-6963
ISSN	1743-5889
DOI	10.2217/nnm-2023-0260
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Article ; Online: Targeting PD-1/PD-L-1 immune checkpoint inhibition for cancer immunotherapy: success and challenges.

Javed, Sadique A / Najmi, Asim / Ahsan, Waquar / Zoghebi, Khalid

Frontiers in immunology

2024 Volume 15, Page(s) 1383456

Abstract: The programmed death-1 receptor (PD-1) acts as a T-cell brake, and its interaction with ligand-1 (PD-L-1) interferes with signal transduction of the T-cell receptor. This leads to suppression of T-cell survival, proliferation, and activity in the tumor ... ...

Abstract	The programmed death-1 receptor (PD-1) acts as a T-cell brake, and its interaction with ligand-1 (PD-L-1) interferes with signal transduction of the T-cell receptor. This leads to suppression of T-cell survival, proliferation, and activity in the tumor microenvironment resulting in compromised anticancer immunity. PD-1/PD-L-1 interaction blockade shown remarkable clinical success in various cancer immunotherapies. To date, most PD-1/PD-L-1 blockers approved for clinical use are monoclonal antibodies (mAbs); however, their therapeutic use are limited owing to poor clinical responses in a proportion of patients. mAbs also displayed low tumor penetration, steep production costs, and incidences of immune-related side effects. This strongly indicates the importance of developing novel inhibitors as cancer immunotherapeutic agents. Recently, advancements in the small molecule-based inhibitors (SMIs) that directly block the PD-1/PD-L-1 axis gained attention from the scientific community involved in cancer research. SMIs demonstrated certain advantages over mAbs, including longer half-lives, low cost, greater cell penetration, and possibility of oral administration. Currently, several SMIs are in development pipeline as potential therapeutics for cancer immunotherapy. To develop new SMIs, a wide range of structural scaffolds have been explored with excellent outcomes; biphenyl-based scaffolds are most studied. In this review, we analyzed the development of mAbs and SMIs targeting PD-1/PD-L-1 axis for cancer treatment. Altogether, the present review delves into the problems related to mAbs use and a detailed discussion on the development and current status of SMIs. This article may provide a comprehensive guide to medicinal chemists regarding the potential structural scaffolds required for PD-1/PD-L-1 interaction inhibition.
MeSH term(s)	Humans ; Neoplasms/immunology ; Neoplasms/therapy ; Neoplasms/drug therapy ; Programmed Cell Death 1 Receptor/antagonists & inhibitors ; Programmed Cell Death 1 Receptor/immunology ; Immune Checkpoint Inhibitors/therapeutic use ; Immune Checkpoint Inhibitors/pharmacology ; Immunotherapy/methods ; B7-H1 Antigen/antagonists & inhibitors ; B7-H1 Antigen/immunology ; Animals ; Tumor Microenvironment/drug effects ; Tumor Microenvironment/immunology ; Antibodies, Monoclonal/therapeutic use
Chemical Substances	Programmed Cell Death 1 Receptor ; Immune Checkpoint Inhibitors ; B7-H1 Antigen ; PDCD1 protein, human ; CD274 protein, human ; Antibodies, Monoclonal
Language	English
Publishing date	2024-04-10
Publishing country	Switzerland
Document type	Journal Article ; Review ; Research Support, Non-U.S. Gov't
ZDB-ID	2606827-8
ISSN	1664-3224 ; 1664-3224
ISSN (online)	1664-3224
ISSN	1664-3224
DOI	10.3389/fimmu.2024.1383456
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Article ; Online: Amelioration of the therapeutic potential of gefitinib against breast cancer using nanostructured lipid carriers.

Kumar, Pankaj / Mangla, Bharti / Javed, Shamama / Ahsan, Waquar / Aggarwal, Geeta

Nanomedicine (London, England)

2023 Volume 18, Issue 18, Page(s) 1139–1160

Abstract: Aim: ...

Abstract	Aim:
MeSH term(s)	Humans ; Female ; Drug Carriers/therapeutic use ; Breast Neoplasms/drug therapy ; Gefitinib/therapeutic use ; Nanostructures ; Lipids ; Particle Size
Chemical Substances	Drug Carriers ; Gefitinib (S65743JHBS) ; Lipids
Language	English
Publishing date	2023-09-04
Publishing country	England
Document type	Journal Article
ZDB-ID	2277839-1
ISSN	1748-6963 ; 1743-5889
ISSN (online)	1748-6963
ISSN	1743-5889
DOI	10.2217/nnm-2023-0107
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Article: Potential effect of luteolin, epiafzelechin, and albigenin on rats under cadmium-induced inflammatory insult:

Shahzadi, Andleeb / Tariq, Nusrat / Sonmez, Haktan / Waquar, Sulayman / Zahid, Ayesha / Javed, Muhammad Ahsan / Ashraf, Muhammad Yasin / Malik, Arif / Ozturk, Munir

Frontiers in chemistry

2023 Volume 11, Page(s) 1036478

Abstract: Introduction: ...

Abstract	Introduction:
Language	English
Publishing date	2023-03-01
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2711776-5
ISSN	2296-2646
ISSN	2296-2646
DOI	10.3389/fchem.2023.1036478
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Article ; Online: Bromelain: a review of its mechanisms, pharmacological effects and potential applications.

Kumar, Virender / Mangla, Bharti / Javed, Shamama / Ahsan, Waquar / Kumar, Pankaj / Garg, Vandana / Dureja, Harish

Food & function

2023 Volume 14, Issue 18, Page(s) 8101–8128

Abstract: The utilization of plant-derived supplements for disease prevention and treatment has long been recognized because of their remarkable potential. ...

Abstract	The utilization of plant-derived supplements for disease prevention and treatment has long been recognized because of their remarkable potential.
MeSH term(s)	Humans ; Bromelains/pharmacology ; Bromelains/therapeutic use ; Apoptosis ; Arthritis, Rheumatoid ; Asthma ; Biological Availability
Chemical Substances	Bromelains (9001-00-7)
Language	English
Publishing date	2023-09-19
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	2612033-1
ISSN	2042-650X ; 2042-6496
ISSN (online)	2042-650X
ISSN	2042-6496
DOI	10.1039/d3fo01060k
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Article ; Online: Multivariate Statistical 2D QSAR Analysis of Indenoisoquinoline-based Topoisomerase- I Inhibitors as Anti-lung Cancer Agents.

Singh, Supriya / Mangla, Bharti / Javed, Shamama / Kumar, Pankaj / Ahsan, Waquar

Anti-cancer agents in medicinal chemistry

2023 Volume 23, Issue 20, Page(s) 2237–2247

Abstract: Background: Indenoisoquinoline-based compounds have shown promise as topoisomerase-I inhibitors, presenting an attractive avenue for rational anticancer drug design. However, a detailed QSAR study on these derivatives has not been performed till date.!## ...

Abstract	Background: Indenoisoquinoline-based compounds have shown promise as topoisomerase-I inhibitors, presenting an attractive avenue for rational anticancer drug design. However, a detailed QSAR study on these derivatives has not been performed till date. Objective: This study aimed to identify crucial molecular features and structural requirements for potent topoisomerase- 1 inhibition. Methods: A comprehensive two-dimensional (2D) QSAR analysis was performed on a series of 49 indenoisoquinoline derivatives using TSAR3.3 software. A robust QSAR model based on a training set of 33 compounds was developed achieving favorable statistical values: r Results: The optimized QSAR model revealed the importance of specific descriptors, including molecular volume, Verloop B2, and Weiner topological index, providing essential insights into effective topoisomerase-1 inhibition. We also obtained a robust partial least-square (PLS) analysis model with high predictive ability (r Conclusion: The present 2D QSAR analysis offered valuable molecular insights into indenoisoquinoline-based topoisomerase- I inhibitors, supporting their potential as anti-lung cancer agents. These findings contribute to the rational design of more effective derivatives, advancing the development of targeted therapies for lung cancer treatment.
MeSH term(s)	Humans ; Quantitative Structure-Activity Relationship ; Antineoplastic Agents/pharmacology ; Neural Networks, Computer ; Neoplasms
Chemical Substances	Antineoplastic Agents
Language	English
Publishing date	2023-10-09
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	2217610-X
ISSN	1875-5992 ; 1871-5206
ISSN (online)	1875-5992
ISSN	1871-5206
DOI	10.2174/0118715206262897230924011648
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Article ; Online: From propolis to nanopropolis: An exemplary journey and a paradigm shift of a resinous substance produced by bees.

Javed, Shamama / Mangla, Bharti / Ahsan, Waquar

Phytotherapy research : PTR

2022 Volume 36, Issue 5, Page(s) 2016–2041

Abstract: Propolis, a natural resinous mixture produced by honey bees is poised with diverse biological activities. Owing to the presence of flavonoids, phenolic acids, terpenes, and sesquiterpenes, propolis has garnered versatile applications in pharmaceutical ... ...

Abstract	Propolis, a natural resinous mixture produced by honey bees is poised with diverse biological activities. Owing to the presence of flavonoids, phenolic acids, terpenes, and sesquiterpenes, propolis has garnered versatile applications in pharmaceutical industry. The biopharmaceutical issues associated with propolis often beset its use as being too hydrophobic in nature; it is not absorbed in the body well. To combat the problem, various nanotechnological approaches for the development of novel drug delivery systems are generally applied to improve its bioavailability. This paradigm shift and transition of conventional propolis to nanopropolis are evident from the literature wherein a multitude of studies are available on nanopropolis with improved bioavailability profile. These approaches include preparation of gold nanoparticles, silver nanoparticles, magnetic nanoparticles, liposomes, liquid crystalline formulations, solid lipid nanoparticles, mesoporous silica nanoparticles, etc. Nanopropolis has further been explored to assess the potential benefits of propolis for the development of futuristic useful products such as sunscreens, creams, mouthwashes, toothpastes, and nutritional supplements with improved solubility, bioavailability, and penetration profiles. However, more high-quality clinical studies assessing the effects of propolis either alone or in combination with synthetic drugs as well as natural products are warranted and its safety needs to be firmly established.
MeSH term(s)	Animals ; Gold ; Liposomes ; Metal Nanoparticles ; Nanoparticles ; Propolis/pharmacology ; Silver
Chemical Substances	Lipid Nanoparticles ; Liposomes ; Silver (3M4G523W1G) ; Gold (7440-57-5) ; Propolis (9009-62-5)
Language	English
Publishing date	2022-03-08
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	639136-9
ISSN	1099-1573 ; 0951-418X
ISSN (online)	1099-1573
ISSN	0951-418X
DOI	10.1002/ptr.7435
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Article: Design-of-Experiments (DoE)-Assisted Fabrication of Quercetin-Loaded Nanoemulgel and Its Evaluation against Human Skin Cancer Cell Lines.

Chitkara, Aman / Mangla, Bharti / Kumar, Pankaj / Javed, Shamama / Ahsan, Waquar / Popli, Harvinder

Pharmaceutics

2022 Volume 14, Issue 11

Abstract: Background: ...

Abstract	Background:
Language	English
Publishing date	2022-11-19
Publishing country	Switzerland
Document type	Journal Article
ZDB-ID	2527217-2
ISSN	1999-4923
ISSN	1999-4923
DOI	10.3390/pharmaceutics14112517
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Article ; Online: Recent Advances in the Treatment Strategies of Friedreich's Ataxia: A Review of Potential Drug Candidates and their Underlying Mechanisms.

Saini, Aman Kumar / Anil, Neha / Vijay, Ardra N / Mangla, Bharti / Javed, Shamama / Kumar, Pankaj / Ahsan, Waquar

Current pharmaceutical design

2024

Abstract: Background: Friedreich's ataxia (FRDA) is a rare hereditary neurodegenerative disorder characterized by progressive ataxia, cardiomyopathy, and diabetes. The disease is caused by a deficiency of frataxin, a mitochondrial protein involved in iron-sulfur ... ...

Abstract	Background: Friedreich's ataxia (FRDA) is a rare hereditary neurodegenerative disorder characterized by progressive ataxia, cardiomyopathy, and diabetes. The disease is caused by a deficiency of frataxin, a mitochondrial protein involved in iron-sulfur cluster synthesis and iron metabolism. Objective: This review aims to summarize recent advances in the development of treatment strategies for FRDA, with a focus on potential drug candidates and their mechanisms of action. Methods: A comprehensive literature search was conducted using various authentic scientific databases to identify studies published in the last decade that investigated potential treatment strategies for FRDA. The search terms used included "Friedreich's ataxia," "treatment," "drug candidates," and "mechanisms of action." Results: To date, only one drug got approval from US-FDA in the year 2023; however, significant developments were achieved in FRDA-related research focusing on diverse therapeutic interventions that could potentially alleviate the symptoms of this disease. Several promising drug candidates have been identified for the treatment of FRDA, which target various aspects of frataxin deficiency and aim to restore frataxin levels, reduce oxidative stress, and improve mitochondrial function. Clinical trials have shown varying degrees of success, with some drugs demonstrating significant improvements in neurological function and quality of life in FRDA patients. Conclusion: While there has been significant progress in the development of treatment strategies for FRDA, further research is needed to optimize these approaches and identify the most effective and safe treatment options for patients. The integration of multiple therapeutic strategies may be necessary to achieve the best outcomes in FRDA management.
Language	English
Publishing date	2024-04-17
Publishing country	United Arab Emirates
Document type	Journal Article
ZDB-ID	1304236-1
ISSN	1873-4286 ; 1381-6128
ISSN (online)	1873-4286
ISSN	1381-6128
DOI	10.2174/0113816128288707240404051856
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