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  1. Article ; Online: Olgotrelvir, a dual inhibitor of SARS-CoV-2 M

    Mao, Long / Shaabani, Namir / Zhang, Xiaoying / Jin, Can / Xu, Wanhong / Argent, Christopher / Kushnareva, Yulia / Powers, Colin / Stegman, Karen / Liu, Jia / Xie, Hui / Xu, Changxu / Bao, Yimei / Xu, Lijun / Zhang, Yuren / Yang, Haigang / Qian, Shengdian / Hu, Yong / Shao, Jianping /
    Zhang, Can / Li, Tingting / Li, Yi / Liu, Na / Lin, Zhenhao / Wang, Shanbo / Wang, Chao / Shen, Wei / Lin, Yuanlong / Shu, Dan / Zhu, Zhenhong / Kotoi, Olivia / Kerwin, Lisa / Han, Qing / Chumakova, Ludmila / Teijaro, John / Royal, Mike / Brunswick, Mark / Allen, Robert / Ji, Henry / Lu, Hongzhou / Xu, Xiao

    Med (New York, N.Y.)

    2024  Volume 5, Issue 1, Page(s) 42–61.e23

    Abstract: ... antiviral targeting the SARS-CoV-2 main protease (M: Findings: Olgotrelvir is a highly bioavailable oral ... with SARS-CoV-2 M: Conclusions: Olgotrelvir is an oral inhibitor targeting M: Funding: Funded ...

    Abstract Background: Oral antiviral drugs with improved antiviral potency and safety are needed to address current challenges in clinical practice for treatment of COVID-19, including the risks of rebound, drug-drug interactions, and emerging resistance.
    Methods: Olgotrelvir (STI-1558) is designed as a next-generation antiviral targeting the SARS-CoV-2 main protease (M
    Findings: Olgotrelvir is a highly bioavailable oral prodrug that is converted in plasma to its active form, AC1115. The dual mechanism of action of olgotrelvir and AC1115 was confirmed by enzyme activity inhibition assays and co-crystal structures of AC1115 with SARS-CoV-2 M
    Conclusions: Olgotrelvir is an oral inhibitor targeting M
    Funding: Funded by Sorrento Therapeutics.
    MeSH term(s) Animals ; Humans ; Mice ; Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; Cathepsin L/antagonists & inhibitors ; COVID-19/prevention & control ; Disease Models, Animal ; Mice, Transgenic ; SARS-CoV-2 ; Coronavirus Protease Inhibitors/chemistry ; Coronavirus Protease Inhibitors/pharmacology ; Coronavirus 3C Proteases/antagonists & inhibitors ; COVID-19 Drug Treatment/methods
    Chemical Substances Antiviral Agents ; Cathepsin L (EC 3.4.22.15) ; STI-1558 ; Coronavirus Protease Inhibitors ; Coronavirus 3C Proteases (EC 3.4.22.28)
    Language English
    Publishing date 2024-01-04
    Publishing country United States
    Document type Journal Article
    ISSN 2666-6340
    ISSN (online) 2666-6340
    DOI 10.1016/j.medj.2023.12.004
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article ; Online: Olgotrelvir, a dual inhibitor of SARS-CoV-2 M

    Mao, Long / Shaabani, Namir / Zhang, Xiaoying / Jin, Can / Xu, Wanhong / Argent, Christopher / Kushnareva, Yulia / Powers, Colin / Stegman, Karen / Liu, Jia / Xie, Hui / Xu, Changxu / Bao, Yimei / Xu, Lijun / Zhang, Yuren / Yang, Haigang / Qian, Shengdian / Hu, Yong / Shao, Jianping /
    Zhang, Can / Li, Tingting / Li, Yi / Liu, Na / Lin, Zhenhao / Wang, Shanbo / Wang, Chao / Shen, Wei / Lin, Yuanlong / Shu, Dan / Zhu, Zhenhong / Kotoi, Olivia / Kerwin, Lisa / Han, Qing / Chumakova, Ludmila / Teijaro, John / Royal, Mike / Brunswick, Mark / Allen, Robert / Ji, Henry / Lu, Hongzhou / Xu, Xiao

    Med (New York, N.Y.)

    2024  Volume 5, Issue 2, Page(s) 169–171

    Language English
    Publishing date 2024-02-02
    Publishing country United States
    Document type Published Erratum
    ISSN 2666-6340
    ISSN (online) 2666-6340
    DOI 10.1016/j.medj.2024.01.013
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article: Heterogeneity in the M. tuberculosis β-Lactamase Inhibition by Sulbactam.

    Schmidt, Marius / Malla, Tek Narsingh / Zielinski, Kara / Aldama, Luis / Bajt, Sasa / Feliz, Denisse / Hayes, Brandon / Hunter, Mark / Kupitz, Christopher / Lisova, Stella / Knoska, Juraj / Martin-Garcia, Jose / Mariani, Valerio / Pandey, Suraj / Poudyal, Ishwor / Sierra, Raymond / Tolstikova, Alexandra / Yefanov, Oleksandr / Yoon, Ching Hong /
    Ourmazd, Abbas / Fromme, Petra / Schwander, Peter / Barty, Anton / Chapman, Henry / Stojković, Emina / Batyuk, Alexander / Boutet, Sébastien / Phillips, George / Pollack, Lois

    Research square

    2023  

    Abstract: For decades, researchers have been determined to elucidate essential enzymatic functions on the atomic lengths scale by tracing atomic positions in real time. Our work builds on new possibilities unleashed by mix-and-inject serial crystallography (MISC) ...

    Abstract For decades, researchers have been determined to elucidate essential enzymatic functions on the atomic lengths scale by tracing atomic positions in real time. Our work builds on new possibilities unleashed by mix-and-inject serial crystallography (MISC)
    Language English
    Publishing date 2023-01-10
    Publishing country United States
    Document type Preprint
    DOI 10.21203/rs.3.rs-2334665/v1
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Heterogeneity in M. tuberculosis β-lactamase inhibition by Sulbactam.

    Malla, Tek Narsingh / Zielinski, Kara / Aldama, Luis / Bajt, Sasa / Feliz, Denisse / Hayes, Brendon / Hunter, Mark / Kupitz, Christopher / Lisova, Stella / Knoska, Juraj / Martin-Garcia, Jose Manuel / Mariani, Valerio / Pandey, Suraj / Poudyal, Ishwor / Sierra, Raymond G / Tolstikova, Alexandra / Yefanov, Oleksandr / Yoon, Chung Hong / Ourmazd, Abbas /
    Fromme, Petra / Schwander, Peter / Barty, Anton / Chapman, Henry N / Stojkovic, Emina A / Batyuk, Alexander / Boutet, Sébastien / Phillips, George N / Pollack, Lois / Schmidt, Marius

    Nature communications

    2023  Volume 14, Issue 1, Page(s) 5507

    Abstract: For decades, researchers have elucidated essential enzymatic functions on the atomic length scale by tracing atomic positions in real-time. Our work builds on possibilities unleashed by mix-and-inject serial crystallography (MISC) at X-ray free electron ... ...

    Abstract For decades, researchers have elucidated essential enzymatic functions on the atomic length scale by tracing atomic positions in real-time. Our work builds on possibilities unleashed by mix-and-inject serial crystallography (MISC) at X-ray free electron laser facilities. In this approach, enzymatic reactions are triggered by mixing substrate or ligand solutions with enzyme microcrystals. Here, we report in atomic detail (between 2.2 and 2.7 Å resolution) by room-temperature, time-resolved crystallography with millisecond time-resolution (with timepoints between 3 ms and 700 ms) how the Mycobacterium tuberculosis enzyme BlaC is inhibited by sulbactam (SUB). Our results reveal ligand binding heterogeneity, ligand gating, cooperativity, induced fit, and conformational selection all from the same set of MISC data, detailing how SUB approaches the catalytic clefts and binds to the enzyme noncovalently before reacting to a trans-enamine. This was made possible in part by the application of singular value decomposition to the MISC data using a program that remains functional even if unit cell parameters change up to 3 Å during the reaction.
    MeSH term(s) Humans ; Ligands ; Mycobacterium tuberculosis ; Sulbactam/pharmacology ; beta-Lactamases ; Tuberculosis
    Chemical Substances Ligands ; Sulbactam (S4TF6I2330) ; beta-Lactamases (EC 3.5.2.6)
    Language English
    Publishing date 2023-09-07
    Publishing country England
    Document type Journal Article ; Research Support, N.I.H., Extramural ; Research Support, Non-U.S. Gov't ; Research Support, U.S. Gov't, Non-P.H.S.
    ZDB-ID 2553671-0
    ISSN 2041-1723 ; 2041-1723
    ISSN (online) 2041-1723
    ISSN 2041-1723
    DOI 10.1038/s41467-023-41246-1
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article: Discovery of SARS-CoV-2 M

    Chan, H T Henry / Moesser, Marc A / Walters, Rebecca K / Malla, Tika R / Twidale, Rebecca M / John, Tobias / Deeks, Helen M / Johnston-Wood, Tristan / Mikhailov, Victor / Sessions, Richard B / Dawson, William / Salah, Eidarus / Lukacik, Petra / Strain-Damerell, Claire / Owen, C David / Nakajima, Takahito / Świderek, Katarzyna / Lodola, Alessio / Moliner, Vicent /
    Glowacki, David R / Spencer, James / Walsh, Martin A / Schofield, Christopher J / Genovese, Luigi / Shoemark, Deborah K / Mulholland, Adrian J / Duarte, Fernanda / Morris, Garrett M

    Chemical science

    2021  Volume 12, Issue 41, Page(s) 13686–13703

    Abstract: The main protease (M ...

    Abstract The main protease (M
    Language English
    Publishing date 2021-09-06
    Publishing country England
    Document type Journal Article
    ZDB-ID 2559110-1
    ISSN 2041-6539 ; 2041-6520
    ISSN (online) 2041-6539
    ISSN 2041-6520
    DOI 10.1039/d1sc03628a
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article: Single M-Line Is as Reliable as Multiple M-Line Ultrasound for Carotid Artery Screening.

    Malik, Afrah E F / Delhaas, Tammo / Spronck, Bart / Henry, Ronald M A / Joseph, Jayaraj / Stehouwer, Coen D A / Mess, Werner H / Reesink, Koen D

    Frontiers in physiology

    2021  Volume 12, Page(s) 787083

    Abstract: Purpose: ...

    Abstract Purpose:
    Language English
    Publishing date 2021-12-20
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2564217-0
    ISSN 1664-042X
    ISSN 1664-042X
    DOI 10.3389/fphys.2021.787083
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  7. Article ; Online: Progression of atypical parkinsonian syndromes: PROSPECT-M-UK study implications for clinical trials.

    Street, Duncan / Jabbari, Edwin / Costantini, Alyssa / Jones, P Simon / Holland, Negin / Rittman, Timothy / Jensen, Marte T / Chelban, Viorica / Goh, Yen Y / Guo, Tong / Heslegrave, Amanda J / Roncaroli, Federico / Klein, Johannes C / Ansorge, Olaf / Allinson, Kieren S J / Jaunmuktane, Zane / Revesz, Tamas / Warner, Thomas T / Lees, Andrew J /
    Zetterberg, Henrik / Russell, Lucy L / Bocchetta, Martina / Rohrer, Jonathan D / Burn, David J / Pavese, Nicola / Gerhard, Alexander / Kobylecki, Christopher / Leigh, P Nigel / Church, Alistair / Hu, Michele T M / Houlden, Henry / Morris, Huw / Rowe, James B

    Brain : a journal of neurology

    2023  Volume 146, Issue 8, Page(s) 3232–3242

    Abstract: ... the need for evidence-based end point selection. Here we report the longitudinal PROSPECT-M-UK study ...

    Abstract The advent of clinical trials of disease-modifying agents for neurodegenerative disease highlights the need for evidence-based end point selection. Here we report the longitudinal PROSPECT-M-UK study of progressive supranuclear palsy (PSP), corticobasal syndrome (CBS), multiple system atrophy (MSA) and related disorders, to compare candidate clinical trial end points. In this multicentre UK study, participants were assessed with serial questionnaires, motor examination, neuropsychiatric and MRI assessments at baseline, 6 and 12 months. Participants were classified by diagnosis at baseline and study end, into Richardson syndrome, PSP-subcortical (PSP-parkinsonism and progressive gait freezing subtypes), PSP-cortical (PSP-frontal, PSP-speech and language and PSP-CBS subtypes), MSA-parkinsonism, MSA-cerebellar, CBS with and without evidence of Alzheimer's disease pathology and indeterminate syndromes. We calculated annual rate of change, with linear mixed modelling and sample sizes for clinical trials of disease-modifying agents, according to group and assessment type. Two hundred forty-three people were recruited [117 PSP, 68 CBS, 42 MSA and 16 indeterminate; 138 (56.8%) male; age at recruitment 68.7 ± 8.61 years]. One hundred and fifty-nine completed the 6-month assessment (82 PSP, 27 CBS, 40 MSA and 10 indeterminate) and 153 completed the 12-month assessment (80 PSP, 29 CBS, 35 MSA and nine indeterminate). Questionnaire, motor examination, neuropsychiatric and neuroimaging measures declined in all groups, with differences in longitudinal change between groups. Neuroimaging metrics would enable lower sample sizes to achieve equivalent power for clinical trials than cognitive and functional measures, often achieving N < 100 required for 1-year two-arm trials (with 80% power to detect 50% slowing). However, optimal outcome measures were disease-specific. In conclusion, phenotypic variance within PSP, CBS and MSA is a major challenge to clinical trial design. Our findings provide an evidence base for selection of clinical trial end points, from potential functional, cognitive, clinical or neuroimaging measures of disease progression.
    MeSH term(s) Male ; Humans ; Middle Aged ; Aged ; Female ; Parkinsonian Disorders/diagnostic imaging ; Parkinsonian Disorders/drug therapy ; Supranuclear Palsy, Progressive/diagnostic imaging ; Supranuclear Palsy, Progressive/pathology ; Multiple System Atrophy/diagnostic imaging ; Multiple System Atrophy/pathology ; Magnetic Resonance Imaging ; United Kingdom
    Language English
    Publishing date 2023-03-28
    Publishing country England
    Document type Multicenter Study ; Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 80072-7
    ISSN 1460-2156 ; 0006-8950
    ISSN (online) 1460-2156
    ISSN 0006-8950
    DOI 10.1093/brain/awad105
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    Ui II Zs.26: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 2021: Bestellungen von Artikeln über das Online-Bestellformular
    ab Jg. 2022: Lesesaal (EG)

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  8. Article ; Online: Letter to editor concerning "Luciano, A., Andrada, M., Rafael, P. F., Franco, S., Lucio, O., & Federico, M. (2022). Pregnancy After Sleeve Gastrectomy: Time Matters?. Obesity Surgery, 1-7."

    Taher, Malak / Catheline, Jean Marc / Henry, Carole / Cohen, Regis

    Obesity surgery

    2022  Volume 32, Issue 11, Page(s) 3785–3786

    MeSH term(s) Humans ; Pregnancy ; Female ; Obesity, Morbid/surgery ; Gastrectomy ; Bariatric Surgery ; Laparoscopy
    Language English
    Publishing date 2022-09-19
    Publishing country United States
    Document type Letter ; Comment
    ZDB-ID 1070827-3
    ISSN 1708-0428 ; 0960-8923
    ISSN (online) 1708-0428
    ISSN 0960-8923
    DOI 10.1007/s11695-022-06279-3
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    Full text online

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    Zs.A 3381: Show issues Location:
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    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
    Jg. 1995 - 2021: Lesesall (2.OG)
    ab Jg. 2022: Lesesaal (EG)

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  9. Article ; Online: Identification of Human Host Substrates of the SARS-CoV-2 M

    Luo, Shu Y / Moussa, Eman W / Lopez-Orozco, Joaquin / Felix-Lopez, Alberto / Ishida, Ray / Fayad, Nawell / Gomez-Cardona, Erik / Wang, Henry / Wilson, Joyce A / Kumar, Anil / Hobman, Tom C / Julien, Olivier

    ACS infectious diseases

    2023  Volume 9, Issue 4, Page(s) 749–761

    Abstract: ... encodes two proteases, M ...

    Abstract The recent emergence of SARS-CoV-2 in the human population has caused a global pandemic. The virus encodes two proteases, M
    MeSH term(s) Humans ; SARS-CoV-2/metabolism ; COVID-19 ; Peptide Synthases ; Peptide Hydrolases/metabolism
    Chemical Substances subtiligase (EC 6.3.2.-) ; Peptide Synthases (EC 6.3.2.-) ; Peptide Hydrolases (EC 3.4.-)
    Language English
    Publishing date 2023-04-03
    Publishing country United States
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ISSN 2373-8227
    ISSN (online) 2373-8227
    DOI 10.1021/acsinfecdis.2c00458
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  10. Article ; Online: Author Correction: Diploid mint (M. longifolia) can produce spearmint type oil with a high yield potential.

    Kippes, Nestor / Tsai, Helen / Lieberman, Meric / Culp, Darrin / McCormack, Brian / Wilson, Rob G / Dowd, Eric / Comai, Luca / Henry, Isabelle M

    Scientific reports

    2022  Volume 12, Issue 1, Page(s) 1006

    Language English
    Publishing date 2022-01-13
    Publishing country England
    Document type Published Erratum
    ZDB-ID 2615211-3
    ISSN 2045-2322 ; 2045-2322
    ISSN (online) 2045-2322
    ISSN 2045-2322
    DOI 10.1038/s41598-022-05238-3
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