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  1. Article ; Online: HSPiP, Computational, and Thermodynamic Model-Based Optimized Solvents for Subcutaneous Delivery of Tolterodine Tartrate and GastroPlus-Based In Vivo Prediction in Humans: Part I.

    Malik, Abdul / Khan, Tasneem / Siddique, Mohd Usman Mohd / Faruk, Abdul / Sood, Ashwani Kumar / Bhat, Zahid Rafiq

    AAPS PharmSciTech

    2024  Volume 25, Issue 5, Page(s) 93

    Abstract: Tolterodine tartrate (TOTA) is associated with adverse effect, high hepatic access, varied bioavailability, slight aqueous solubility, and short half-life after oral delivery. Hansen solubility parameters (HSP, HSPiP program), experimental solubility (T = ...

    Abstract Tolterodine tartrate (TOTA) is associated with adverse effect, high hepatic access, varied bioavailability, slight aqueous solubility, and short half-life after oral delivery. Hansen solubility parameters (HSP, HSPiP program), experimental solubility (T = 298.2 to 318.2 K and p = 0.1 MPa), computational (van't Hoff and Apelblat models), and thermodynamic models were used to the select solvent(s). HSPiP predicted PEG400 as the most suitable co-solvent based on HSP values (δ
    MeSH term(s) Solubility ; Humans ; Tolterodine Tartrate/administration & dosage ; Tolterodine Tartrate/chemistry ; Tolterodine Tartrate/pharmacokinetics ; Solvents/chemistry ; Thermodynamics ; Polyethylene Glycols/chemistry ; Biological Availability ; Chemistry, Pharmaceutical/methods ; Injections, Subcutaneous ; Drug Delivery Systems/methods
    Chemical Substances Tolterodine Tartrate (5T619TQR3R) ; Solvents ; Polyethylene Glycols (3WJQ0SDW1A) ; polyethylene glycol 400 (B697894SGQ)
    Language English
    Publishing date 2024-05-01
    Publishing country United States
    Document type Journal Article
    ZDB-ID 2052070-0
    ISSN 1530-9932 ; 1530-9932
    ISSN (online) 1530-9932
    ISSN 1530-9932
    DOI 10.1208/s12249-024-02800-2
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Target validation and structure-based virtual screening to Discover potential lead molecules against the oncogenic NSD1 histone methyltransferase.

    Bhat, Zahid Rafiq / Gahlawat, Anuj / Kumar, Navneet / Sharma, Nisha / Garg, Prabha / Tikoo, Kulbhushan

    In silico pharmacology

    2023  Volume 11, Issue 1, Page(s) 21

    Language English
    Publishing date 2023-08-11
    Publishing country Germany
    Document type Journal Article
    ZDB-ID 2702993-1
    ISSN 2193-9616
    ISSN 2193-9616
    DOI 10.1007/s40203-023-00158-0
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: MicroRNA-941 regulates the proliferation of breast cancer cells by altering histone H3 Ser 10 phosphorylation.

    Surapaneni, Sunil Kumar / Bhat, Zahid Rafiq / Tikoo, Kulbhushan

    Scientific reports

    2020  Volume 10, Issue 1, Page(s) 17954

    Abstract: Breast cancer including triple negative breast cancer (TNBC) represents an important clinical challenge, as these tumours often develop resistance to conventional chemotherapeutics. MicroRNAs play a crucial role in cell-cycle regulation, differentiation, ...

    Abstract Breast cancer including triple negative breast cancer (TNBC) represents an important clinical challenge, as these tumours often develop resistance to conventional chemotherapeutics. MicroRNAs play a crucial role in cell-cycle regulation, differentiation, apoptosis, and migration. Herein, we performed Affymetrix Gene Chip miRNA 4.0 microarray and observed differential regulation of miRNAs (75 upregulated and 199 downregulated) in metastatic MDA-MB-231 cells as compared to immortalized human non-tumorigenic breast epithelial (MCF-10A) cells. MicroRNA-941 was significantly upregulated in MDA-MB-231 cells (almost nine-fold increase) in comparison to MCF-10A cells. Transfection of MiRNA-941 inhibitor significantly decreased the proliferation and migration of MDA-MB-231 cells by altering the expressions of p21, Cyclin D1, PP2B-B1, E-cadherin and MMP-13. Interestingly, we provide first evidence that inhibiting miR-941 prevents cell proliferation and phosphorylation of histone H3 at Ser10 residue. Xenograft model of breast cancer was developed by subcutaneous injection of MDA-MB-231 cells into the mammary fat pad of female athymic nude mice (Crl:NU-Foxn1nu). The tumours were allowed to grow to around 60 mm
    MeSH term(s) Animals ; Breast Neoplasms/drug therapy ; Breast Neoplasms/genetics ; Breast Neoplasms/metabolism ; Breast Neoplasms/pathology ; Cell Movement/genetics ; Cell Proliferation/genetics ; Disease Models, Animal ; Female ; Gene Expression Regulation, Neoplastic/genetics ; Histones/genetics ; Histones/metabolism ; Humans ; MCF-7 Cells ; Mice, Nude ; MicroRNAs/antagonists & inhibitors ; MicroRNAs/genetics ; MicroRNAs/metabolism ; MicroRNAs/physiology ; Molecular Targeted Therapy ; Phosphorylation/genetics ; Tumor Cells, Cultured
    Chemical Substances Histones ; MIRN941 microRNA, human ; MicroRNAs
    Language English
    Publishing date 2020-10-21
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-020-74847-7
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Role of autophagy and histone deacetylases in diabetic nephropathy: Current status and future perspectives.

    Khan, Sabbir / Bhat, Zahid Rafiq / Jena, Gopabandhu

    Genes & diseases

    2016  Volume 3, Issue 3, Page(s) 211–219

    Abstract: The prevalence of diabetes and its complications is increasing at an alarming rate in both developed and deve1oping nations. The emerging evidences highlighted that both genetic and epigenetic mechanisms including histone modifications play a significant ...

    Abstract The prevalence of diabetes and its complications is increasing at an alarming rate in both developed and deve1oping nations. The emerging evidences highlighted that both genetic and epigenetic mechanisms including histone modifications play a significant role in the pathogenesis of diabetic nephropathy (DN). Histone deacetylases (HDACs) and acetylation are involved in the regulation of autophagy as well as pathogenesis of DN. Both HDACs and histone acetyltransferases (HATs) play a key role in chromatin remodeling and affect the transcription of various genes involved in the cellular homeostasis, apoptosis, immunity and angiogenesis. Further, HDAC inhibitors are exert the renoprotective effects in DN and other diabetic complications. Thus, the cellular acetylation plays a crucial role in the regulation of autophagy and can be explored as a new therapeutic target for the treatment of DN. This review aimed to delineate the role of HDACs and associated molecular signaling/pathways in the regulation of autophagy with an emphasis on promising targets for the treatment of DN.
    Language English
    Publishing date 2016-04-23
    Publishing country China
    Document type Journal Article ; Review
    ZDB-ID 2821806-1
    ISSN 2352-3042 ; 2352-3042
    ISSN (online) 2352-3042
    ISSN 2352-3042
    DOI 10.1016/j.gendis.2016.04.003
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: In Vivo Anticancer Evaluation of 6b, a Non-Covalent Imidazo[1,2-

    Bhat, Zahid Rafiq / Kumar, Manvendra / Sharma, Nisha / Yadav, Umesh Prasad / Singh, Tashvinder / Joshi, Gaurav / Pujala, Brahmam / Raja, Mohd / Chatterjee, Joydeep / Tikoo, Kulbhushan / Singh, Sandeep / Kumar, Raj

    Molecules (Basel, Switzerland)

    2022  Volume 27, Issue 17

    Abstract: Tyrosine kinase inhibitors are validated therapeutic agents against EGFR-mutated non-small cell lung cancer (NSCLC). However, the associated critical side effects of these agents are inevitable, demanding more specific and efficient targeting agents. ... ...

    Abstract Tyrosine kinase inhibitors are validated therapeutic agents against EGFR-mutated non-small cell lung cancer (NSCLC). However, the associated critical side effects of these agents are inevitable, demanding more specific and efficient targeting agents. Recently, we have developed and reported a non-covalent imidazo[1,2-
    MeSH term(s) Animals ; Carcinoma, Non-Small-Cell Lung/metabolism ; Cell Line, Tumor ; Cell Proliferation ; Drug Resistance, Neoplasm ; ErbB Receptors/metabolism ; Heterografts ; Humans ; Lung Neoplasms/metabolism ; Mice ; Mice, Nude ; Mutation ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Quinazolines/pharmacology ; Quinoxalines/pharmacology ; Quinoxalines/therapeutic use ; Xenograft Model Antitumor Assays
    Chemical Substances Protein Kinase Inhibitors ; Quinazolines ; Quinoxalines ; ErbB Receptors (EC 2.7.10.1)
    Language English
    Publishing date 2022-08-28
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules27175540
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.MO 81: Show issues

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  6. Article ; Online: Design and Synthesis of Non-Covalent Imidazo[1,2-

    Kumar, Manvendra / Joshi, Gaurav / Arora, Sahil / Singh, Tashvinder / Biswas, Sajal / Sharma, Nisha / Bhat, Zahid Rafiq / Tikoo, Kulbhushan / Singh, Sandeep / Kumar, Raj

    Molecules (Basel, Switzerland)

    2021  Volume 26, Issue 5

    Abstract: A series of 30 non-covalent imidazo[1,2- ...

    Abstract A series of 30 non-covalent imidazo[1,2-
    MeSH term(s) A549 Cells ; Antineoplastic Agents/pharmacology ; Carcinoma, Non-Small-Cell Lung/metabolism ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Drug Resistance, Neoplasm/drug effects ; Drug Screening Assays, Antitumor ; ErbB Receptors/antagonists & inhibitors ; ErbB Receptors/metabolism ; Erlotinib Hydrochloride/pharmacology ; Gefitinib/pharmacology ; Humans ; Imidazoles/chemistry ; Imidazoles/pharmacology ; Inhibitory Concentration 50 ; Lung Neoplasms/metabolism ; Molecular Docking Simulation ; Mutation/drug effects ; Protein Kinase Inhibitors/pharmacology ; Quinoxalines/chemistry ; Quinoxalines/pharmacology ; Structure-Activity Relationship
    Chemical Substances Antineoplastic Agents ; Imidazoles ; Protein Kinase Inhibitors ; Quinoxalines ; Erlotinib Hydrochloride (DA87705X9K) ; EGFR protein, human (EC 2.7.10.1) ; ErbB Receptors (EC 2.7.10.1) ; Gefitinib (S65743JHBS)
    Language English
    Publishing date 2021-03-09
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 1413402-0
    ISSN 1420-3049 ; 1431-5165 ; 1420-3049
    ISSN (online) 1420-3049
    ISSN 1431-5165 ; 1420-3049
    DOI 10.3390/molecules26051490
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.MO 81: Show issues

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  7. Article ; Online: Synthesis and evaluation of new 1,2,4-oxadiazole based trans- acrylic acid derivatives as potential PPAR-alpha/gamma dual agonist.

    Kaur, Paranjeet / Bhat, Zahid Rafiq / Bhat, Sana / Kumar, Rakesh / Kumar, Rajan / Tikoo, Kulbhushan / Gupta, Jeena / Khurana, Navneet / Kaur, Jaskiran / Khatik, Gopal L

    Bioorganic chemistry

    2020  Volume 100, Page(s) 103867

    Abstract: Diabetes is a ubiquitously a metabolic disorder and life-threatening disease. Peroxisome proliferator-activated receptors (PPARs) belong to the class of nuclear receptors which acts as transcription factors to regulate lipid and glucose metabolism. PPAR ... ...

    Abstract Diabetes is a ubiquitously a metabolic disorder and life-threatening disease. Peroxisome proliferator-activated receptors (PPARs) belong to the class of nuclear receptors which acts as transcription factors to regulate lipid and glucose metabolism. PPAR alpha/gamma dual agonists tend to corroborate the functions of both thiazolidinediones and fibrates and they hold substantial promise for ameliorating the type 2 diabetic treatments and providing potential therapeutic diabetic interventions. New 1,2,4-oxadiazole based trans- acrylic acid derivatives compounds possessing aryl/methylene linker in between pharmacophore head and lipophilic tail for dual PPAR-alpha/gamma agonists are studied. AutoDock Vina used for potential PPAR alpha/gamma dual agonists and 6 compounds 9a, 9g, 9 m, 9n, 9o, and 9r were identified comparable to PPAR gamma agonist Pioglitazone on the basis of their affinity scores and further their in-silico toxicity and in-silico ADME properties. The selected compounds showed better-calculated lipophilicity (iLogP) was found to be 0.92 to 3.19. Compound 9n and 9a were found to be most potent on both PPAR alpha and gamma receptors with EC
    MeSH term(s) Animals ; Blood Glucose/analysis ; Blood Glucose/metabolism ; Diabetes Mellitus, Type 2/blood ; Diabetes Mellitus, Type 2/drug therapy ; Diabetes Mellitus, Type 2/metabolism ; Drug Design ; Female ; Humans ; Hypoglycemic Agents/chemistry ; Hypoglycemic Agents/pharmacology ; Hypoglycemic Agents/therapeutic use ; Molecular Docking Simulation ; Oxadiazoles/chemistry ; Oxadiazoles/pharmacology ; Oxadiazoles/therapeutic use ; PPAR alpha/agonists ; PPAR alpha/metabolism ; PPAR gamma/agonists ; PPAR gamma/metabolism ; Rats, Sprague-Dawley
    Chemical Substances Blood Glucose ; Hypoglycemic Agents ; Oxadiazoles ; PPAR alpha ; PPAR gamma
    Language English
    Publishing date 2020-04-21
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 120080-x
    ISSN 1090-2120 ; 0045-2068
    ISSN (online) 1090-2120
    ISSN 0045-2068
    DOI 10.1016/j.bioorg.2020.103867
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 4207: Show issues Location:
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    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
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