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  1. Article ; Online: Channeling Nicotinamide Phosphoribosyltransferase (NAMPT) to Address Life and Death.

    Velma, Ganga Reddy / Krider, Isabella S / Alves, Erick T M / Courey, Jenna M / Laham, Megan S / Thatcher, Gregory R J

    Journal of medicinal chemistry

    2024  Volume 67, Issue 8, Page(s) 5999–6026

    Abstract: Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the rate-limiting step in ... ...

    Abstract Nicotinamide phosphoribosyltransferase (NAMPT) catalyzes the rate-limiting step in NAD
    MeSH term(s) Nicotinamide Phosphoribosyltransferase/metabolism ; Nicotinamide Phosphoribosyltransferase/antagonists & inhibitors ; Humans ; Enzyme Inhibitors/pharmacology ; Enzyme Inhibitors/chemistry ; Animals ; Neoplasms/drug therapy ; NAD/metabolism ; Allosteric Regulation/drug effects ; Cell Death/drug effects ; Antineoplastic Agents/pharmacology ; Antineoplastic Agents/chemistry ; Cytokines/metabolism
    Chemical Substances Nicotinamide Phosphoribosyltransferase (EC 2.4.2.12) ; Enzyme Inhibitors ; NAD (0U46U6E8UK) ; Antineoplastic Agents ; nicotinamide phosphoribosyltransferase, human (EC 2.4.2.12) ; Cytokines
    Language English
    Publishing date 2024-04-05
    Publishing country United States
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c02112
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: Nicotinamide Phosphoribosyltransferase Positive Allosteric Modulators Attenuate Neuronal Oxidative Stress.

    Gordon-Blake, Jesse / Ratia, Kiira / Weidig, Victoria / Velma, Ganga Reddy / Ackerman-Berrier, Martha / Penton, Christopher / Musku, Soumya Reddy / Alves, Erick T M / Driver, Tom / Tai, Leon / Thatcher, Gregory R J

    ACS medicinal chemistry letters

    2024  Volume 15, Issue 2, Page(s) 205–214

    Abstract: Evidence supports boosting nicotinamide adenine dinucleotide ( ... ...

    Abstract Evidence supports boosting nicotinamide adenine dinucleotide (NAD
    Language English
    Publishing date 2024-01-24
    Publishing country United States
    Document type Journal Article
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.3c00391
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Synthesis, Optimization, and Structure-Activity Relationships of Nicotinamide Phosphoribosyltransferase (NAMPT) Positive Allosteric Modulators (N-PAMs).

    Shen, Zhengnan / Ratia, Kiira / Krider, Isabella / Ackerman-Berrier, Martha / Penton, Christopher / Musku, Soumya Reddy / Gordon-Blake, Jesse M / Laham, Megan S / Christie, Nicholas / Ma, Nina / Fu, Jiqiang / Xiong, Rui / Courey, Jenna M / Velma, Ganga Reddy / Thatcher, Gregory R J

    Journal of medicinal chemistry

    2023  Volume 66, Issue 24, Page(s) 16704–16727

    Abstract: Depletion of nicotinamide adenine dinucleotide ( ... ...

    Abstract Depletion of nicotinamide adenine dinucleotide (NAD
    MeSH term(s) Nicotinamide Phosphoribosyltransferase/chemistry ; Nicotinamide Phosphoribosyltransferase/metabolism ; NAD/metabolism ; Niacinamide/pharmacology ; Cell Line, Tumor ; Cytokines/metabolism ; Structure-Activity Relationship
    Chemical Substances Nicotinamide Phosphoribosyltransferase (EC 2.4.2.12) ; NAD (0U46U6E8UK) ; Niacinamide (25X51I8RD4) ; Cytokines
    Language English
    Publishing date 2023-12-14
    Publishing country United States
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c01406
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Mechanism of Allosteric Modulation of Nicotinamide Phosphoribosyltransferase to Elevate Cellular NAD

    Ratia, Kiira M / Shen, Zhengnan / Gordon-Blake, Jesse / Lee, Hyun / Laham, Megan S / Krider, Isabella S / Christie, Nicholas / Ackerman-Berrier, Martha / Penton, Christopher / Knowles, Natalie G / Musku, Soumya Reddy / Fu, Jiqiang / Velma, Ganga Reddy / Xiong, Rui / Thatcher, Gregory R J

    Biochemistry

    2023  Volume 62, Issue 4, Page(s) 923–933

    Abstract: In aging and disease, cellular nicotinamide adenine dinucleotide ( ... ...

    Abstract In aging and disease, cellular nicotinamide adenine dinucleotide (NAD
    MeSH term(s) Humans ; Cytokines/metabolism ; Longevity ; NAD/metabolism ; Niacinamide/pharmacology ; Niacinamide/metabolism ; Nicotinamide Phosphoribosyltransferase/chemistry ; Nicotinamide Phosphoribosyltransferase/metabolism ; Allosteric Site
    Chemical Substances Cytokines ; NAD (0U46U6E8UK) ; Niacinamide (25X51I8RD4) ; Nicotinamide Phosphoribosyltransferase (EC 2.4.2.12)
    Language English
    Publishing date 2023-02-06
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Research Support, N.I.H., Extramural ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 1108-3
    ISSN 1520-4995 ; 0006-2960
    ISSN (online) 1520-4995
    ISSN 0006-2960
    DOI 10.1021/acs.biochem.2c00655
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: Identification and characterization of forced degradation products of vortioxetine by LC/MS/MS and NMR.

    Ragi, Nagarjuna Chary / Velma, Ganga Reddy / Pallerla, Pavan Kumar / Siddiqua, Sana / Alugonda, Veeresham / Rachamalla, Hari Krishna Reddy / Pabbaraja, Srihari / Sripadi, Prabhakar

    Journal of pharmaceutical and biomedical analysis

    2020  Volume 188, Page(s) 113442

    Abstract: Vortioxetine (VTX) is a novel multimodal antidepressant drug that affects the serotoninergic and noradrenergic systems. In this work, the forced degradation of VTX was studied according to (ICH) Q1A (R2) guidelines. The study revealed that VTX was stable ...

    Abstract Vortioxetine (VTX) is a novel multimodal antidepressant drug that affects the serotoninergic and noradrenergic systems. In this work, the forced degradation of VTX was studied according to (ICH) Q1A (R2) guidelines. The study revealed that VTX was stable under thermal stress conditions and hydrolytic stress conditions i.e., acidic, basic and neutral conditions. In contrast, six degradation products (DPs) were formed under photolytic and oxidative stress conditions. The DPs were identified and characterized by high-resolution LC/MS and LC/MS/MS. The structures of major DPs were further confirmed by the synthesis and characterization by
    MeSH term(s) Chromatography, High Pressure Liquid ; Drug Stability ; Hydrolysis ; Oxidation-Reduction ; Photolysis ; Spectrometry, Mass, Electrospray Ionization ; Tandem Mass Spectrometry ; Vortioxetine
    Chemical Substances Vortioxetine (3O2K1S3WQV)
    Language English
    Publishing date 2020-06-27
    Publishing country England
    Document type Journal Article
    ZDB-ID 604917-5
    ISSN 1873-264X ; 0731-7085
    ISSN (online) 1873-264X
    ISSN 0731-7085
    DOI 10.1016/j.jpba.2020.113442
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Dinuclear orthometallated gold(I)-gold(III) anticancer complexes with potent in vivo activity through an ROS-dependent mechanism.

    Mirzadeh, Nedaossadat / Telukutla, Srinivasa Reddy / Luwor, Rodney / Privér, Steven / Velma, Ganga Reddy / Jakku, Ranjith Kumar / Andrew N, Stephens / Plebanski, Magdalena / Christian, Hartinger / Bhargava, Suresh

    Metallomics : integrated biometal science

    2021  Volume 13, Issue 7

    Abstract: Increasingly explored over the last decade, gold complexes have shown great promise in the field of cancer therapeutics. A major obstacle to their clinical progression has been their lack of in vivo stability, particularly for gold(III) complexes, which ... ...

    Abstract Increasingly explored over the last decade, gold complexes have shown great promise in the field of cancer therapeutics. A major obstacle to their clinical progression has been their lack of in vivo stability, particularly for gold(III) complexes, which often undergo a facile reduction in the presence of biomolecules such as glutathione. Herein, we report a new class of promising anticancer gold(I)-gold(III) complexes with the general formula [XAuI(μ-2-C6F4PPh2)(κ2-2-C6F4PPh2)AuIIIX] [X = Cl (1), Br (2), NO3 (3)] which feature two gold atoms in different oxidation states (I and III) in a single molecule. Interestingly, gold(I)-gold(III) complexes (1-3) are stable against glutathione reduction under physiological-like conditions. In addition, complexes 1-3 exhibit significant cytotoxicity (276-fold greater than cisplatin) toward the tested cancer cells compared to the noncancerous cells. Moreover, the gold(I)-gold(III) complexes do not interact with DNA-like cisplatin but target cellular thioredoxin reductase, an enzyme linked to the development of cisplatin drug resistance. Complexes 1-3 also showed potential to inhibit cancer and endothelial cell migration, as well as tube formation during angiogenesis. In vivo studies in a murine HeLa xenograft model further showed the gold compounds may inhibit tumor growth on par clinically used cisplatin, supporting the significant potential this new compound class has for further development as cancer therapeutic.
    MeSH term(s) Animals ; Antineoplastic Agents/chemistry ; Antineoplastic Agents/pharmacology ; Apoptosis ; Cell Cycle ; Cell Proliferation ; Cisplatin/pharmacology ; Coordination Complexes/chemistry ; Coordination Complexes/pharmacology ; Female ; Gold/chemistry ; Humans ; Mice ; Mice, Inbred BALB C ; Mice, Nude ; Reactive Oxygen Species/metabolism ; Tumor Cells, Cultured ; Uterine Cervical Neoplasms/drug therapy ; Uterine Cervical Neoplasms/pathology ; Xenograft Model Antitumor Assays
    Chemical Substances Antineoplastic Agents ; Coordination Complexes ; Reactive Oxygen Species ; Gold (7440-57-5) ; Cisplatin (Q20Q21Q62J)
    Language English
    Publishing date 2021-06-23
    Publishing country England
    Document type Journal Article
    ZDB-ID 2474317-3
    ISSN 1756-591X ; 1756-5901
    ISSN (online) 1756-591X
    ISSN 1756-5901
    DOI 10.1093/mtomcs/mfab039
    Database MEDical Literature Analysis and Retrieval System OnLINE

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