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  1. Article ; Online: SARS-CoV-2 Papain-Like Protease: Structure, Function and Inhibition.

    Ullrich, Sven / Nitsche, Christoph

    Chembiochem : a European journal of chemical biology

    2022  Volume 23, Issue 19, Page(s) e202200327

    Abstract: Emerging variants of SARS-CoV-2 and potential novel epidemic coronaviruses underline the importance of investigating various viral proteins as potential drug targets. The papain-like protease of coronaviruses has been less explored than other viral ... ...

    Abstract Emerging variants of SARS-CoV-2 and potential novel epidemic coronaviruses underline the importance of investigating various viral proteins as potential drug targets. The papain-like protease of coronaviruses has been less explored than other viral proteins; however, its substantive role in viral replication and impact on the host immune response make it a suitable target to study. This review article focuses on the structure and function of the papain-like protease (PL
    MeSH term(s) Aniline Compounds ; Antiviral Agents/chemistry ; Benzamides ; COVID-19/drug therapy ; Coronavirus Papain-Like Proteases ; Humans ; Naphthalenes ; Papain/chemistry ; Papain/metabolism ; Peptide Hydrolases/metabolism ; Protease Inhibitors/pharmacology ; SARS-CoV-2 ; Ubiquitin/metabolism ; Viral Proteins/chemistry
    Chemical Substances 5-amino-2-methyl-N-((R)-1-(1-naphthyl)ethyl)benzamide ; Aniline Compounds ; Antiviral Agents ; Benzamides ; Naphthalenes ; Protease Inhibitors ; Ubiquitin ; Viral Proteins ; Peptide Hydrolases (EC 3.4.-) ; Coronavirus Papain-Like Proteases (EC 3.4.22.2) ; Papain (EC 3.4.22.2) ; papain-like protease, SARS-CoV-2 (EC 3.4.22.2)
    Language English
    Publishing date 2022-09-08
    Publishing country Germany
    Document type Journal Article ; Review ; Research Support, Non-U.S. Gov't
    ZDB-ID 2020469-3
    ISSN 1439-7633 ; 1439-4227
    ISSN (online) 1439-7633
    ISSN 1439-4227
    DOI 10.1002/cbic.202200327
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  2. Article ; Online: Design, Synthesis, and Biological Evaluation of Small-Molecule-Based Radioligands with Improved Pharmacokinetic Properties for Imaging of Programmed Death Ligand 1.

    Krutzek, Fabian / Donat, Cornelius K / Ullrich, Martin / Stadlbauer, Sven

    Journal of medicinal chemistry

    2023  Volume 66, Issue 23, Page(s) 15894–15915

    Abstract: Small molecules offer some advantages for developing positron emission tomography (PET) tracers and are therefore a promising approach for imaging and therapy monitoring of programmed death ligand 1 (PD-L1) positive tumors. Here, we report six biphenyl ... ...

    Abstract Small molecules offer some advantages for developing positron emission tomography (PET) tracers and are therefore a promising approach for imaging and therapy monitoring of programmed death ligand 1 (PD-L1) positive tumors. Here, we report six biphenyl PD-L1 radioligands using the NODA-GA-chelator for efficient copper-64 complexation. These radioligands contain varying numbers of sulfonic and/or phosphonic acid groups, serving as hydrophilizing units to lower the log
    MeSH term(s) Animals ; B7-H1 Antigen/metabolism ; Copper ; Positron-Emission Tomography/methods ; Neoplasms ; Cell Line, Tumor
    Chemical Substances B7-H1 Antigen ; Copper (789U1901C5)
    Language English
    Publishing date 2023-12-01
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.3c01355
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    Zs.B 151: Show issues Location:
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  3. Article ; Online: The SARS-CoV-2 main protease as drug target.

    Ullrich, Sven / Nitsche, Christoph

    Bioorganic & medicinal chemistry letters

    2020  Volume 30, Issue 17, Page(s) 127377

    Abstract: The unprecedented pandemic of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is threatening global health. The virus emerged in late 2019 and can cause a severe disease associated with significant mortality. Several vaccine development ... ...

    Abstract The unprecedented pandemic of the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) is threatening global health. The virus emerged in late 2019 and can cause a severe disease associated with significant mortality. Several vaccine development and drug discovery campaigns are underway. The SARS-CoV-2 main protease is considered a promising drug target, as it is dissimilar to human proteases. Sequence and structure of the main protease are closely related to those from other betacoronaviruses, facilitating drug discovery attempts based on previous lead compounds. Covalently binding peptidomimetics and small molecules are investigated. Various compounds show antiviral activity in infected human cells.
    MeSH term(s) Amino Acid Sequence ; Animals ; Antiviral Agents/pharmacokinetics ; Antiviral Agents/pharmacology ; Betacoronavirus/drug effects ; Betacoronavirus/enzymology ; Cell Line ; Coronavirus 3C Proteases ; Cysteine Endopeptidases/chemistry ; Cysteine Proteinase Inhibitors/pharmacokinetics ; Cysteine Proteinase Inhibitors/pharmacology ; Drug Discovery ; Humans ; Peptidomimetics/pharmacokinetics ; Peptidomimetics/pharmacology ; SARS-CoV-2 ; Substrate Specificity ; Viral Nonstructural Proteins/antagonists & inhibitors ; Viral Nonstructural Proteins/chemistry
    Chemical Substances Antiviral Agents ; Cysteine Proteinase Inhibitors ; Peptidomimetics ; Viral Nonstructural Proteins ; Cysteine Endopeptidases (EC 3.4.22.-) ; Coronavirus 3C Proteases (EC 3.4.22.28)
    Keywords covid19
    Language English
    Publishing date 2020-07-02
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't ; Review
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2020.127377
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 3203: Show issues Location:
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  4. Article ; Online: Main protease mutants of SARS-CoV-2 variants remain susceptible to nirmatrelvir.

    Ullrich, Sven / Ekanayake, Kasuni B / Otting, Gottfried / Nitsche, Christoph

    Bioorganic & medicinal chemistry letters

    2022  Volume 62, Page(s) 128629

    Abstract: The COVID-19 pandemic continues to be a public health threat. Multiple mutations in the spike protein of emerging variants of SARS-CoV-2 appear to impact on the effectiveness of available vaccines. Specific antiviral agents are keenly anticipated but ... ...

    Abstract The COVID-19 pandemic continues to be a public health threat. Multiple mutations in the spike protein of emerging variants of SARS-CoV-2 appear to impact on the effectiveness of available vaccines. Specific antiviral agents are keenly anticipated but their efficacy may also be compromised in emerging variants. One of the most attractive coronaviral drug targets is the main protease (M
    MeSH term(s) Antiviral Agents/pharmacology ; Antiviral Agents/therapeutic use ; COVID-19/drug therapy ; Humans ; Lactams ; Leucine ; Nitriles ; Pandemics/prevention & control ; Peptide Hydrolases ; Proline ; Protease Inhibitors ; SARS-CoV-2/genetics
    Chemical Substances Antiviral Agents ; Lactams ; Nitriles ; Protease Inhibitors ; nirmatrelvir (7R9A5P7H32) ; Proline (9DLQ4CIU6V) ; Peptide Hydrolases (EC 3.4.-) ; Leucine (GMW67QNF9C)
    Language English
    Publishing date 2022-02-16
    Publishing country England
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2022.128629
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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3203: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
    bis Jg. 1994: Bestellungen von Artikeln über das Online-Bestellformular
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    ab Jg. 2022: Lesesaal (EG)

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  5. Article: Preparation of

    Craig, Austin / Kogler, Jürgen / Laube, Markus / Ullrich, Martin / Donat, Cornelius K / Wodtke, Robert / Kopka, Klaus / Stadlbauer, Sven

    Pharmaceutics

    2023  Volume 15, Issue 12

    Abstract: Early detection and treatment of cancers can significantly increase patient prognosis and enhance the quality of life of affected patients. The emerging significance of the tumor microenvironment (TME) as a new frontier for cancer diagnosis and therapy ... ...

    Abstract Early detection and treatment of cancers can significantly increase patient prognosis and enhance the quality of life of affected patients. The emerging significance of the tumor microenvironment (TME) as a new frontier for cancer diagnosis and therapy may be exploited by radiolabeled tracers for diagnostic imaging techniques such as positron emission tomography (PET). Cancer-associated fibroblasts (CAFs) within the TME are identified by biomarkers such as fibroblast activation protein alpha (FAPα), which are expressed on their surfaces. Targeting FAPα using small-molecule
    Language English
    Publishing date 2023-12-10
    Publishing country Switzerland
    Document type Journal Article
    ZDB-ID 2527217-2
    ISSN 1999-4923
    ISSN 1999-4923
    DOI 10.3390/pharmaceutics15122749
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  6. Article ; Online: Influence of Backbone Ladderization and Side Chain Variation on the Orientation of Diketopyrrolopyrrole-Based Donor-Acceptor Copolymers

    Sven Bölke / Andreas Früh / Florian Trilling / Michael Forster / Ullrich Scherf / Thomas Chassé / Heiko Peisert

    Molecules, Vol 28, Iss 6435, p

    2023  Volume 6435

    Abstract: Ladder polymers with poly(diketopyrrolopyrrole) (DPP) moieties have recently attracted enormous interest for a large variety of opto-electronic applications. Since the rigidity of the backbone increases with ladderization, a strong influence on the self- ... ...

    Abstract Ladder polymers with poly(diketopyrrolopyrrole) (DPP) moieties have recently attracted enormous interest for a large variety of opto-electronic applications. Since the rigidity of the backbone increases with ladderization, a strong influence on the self-organization of thin films is expected. We study the molecular orientation of DPP-based ladder polymers in about 50 nm thin films using polarization modulation-infrared reflection-absorption spectroscopy (PM-IRRAS). Exemplarily, for one polymer, the orientation in thicker films is qualitatively investigated by infrared spectroscopy in transmission. Further, this method allows us to rule out the effects of a possible azimuthal ordering, which would affect the analysis of the orientation by PM-IRRAS. For all polymers, the long axis of the polymer backbone is preferentially oriented parallel to the substrate surface, pointing to a high degree of ordering. It is suggested that the choice of the side chains might be a promising way to tune for face-on and edge-on orientations. The exemplarily performed investigation of interface properties on substrates with different work functions suggests that the choice of the side chains has a minor effect on the interfacial electronic interface structure.
    Keywords low band gap polymers ; orientation ; UV/vis ; FTIR ; PM-IRRAS ; benzodithiophene ; Organic chemistry ; QD241-441
    Subject code 540
    Language English
    Publishing date 2023-09-01T00:00:00Z
    Publisher MDPI AG
    Document type Article ; Online
    Database BASE - Bielefeld Academic Search Engine (life sciences selection)

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  7. Article ; Online: The SARS-CoV-2 main protease as drug target

    Ullrich, Sven / Nitsche, Christoph

    Bioorganic & Medicinal Chemistry Letters

    2020  Volume 30, Issue 17, Page(s) 127377

    Keywords Organic Chemistry ; Clinical Biochemistry ; Molecular Medicine ; Biochemistry ; Molecular Biology ; Drug Discovery ; Pharmaceutical Science ; covid19
    Language English
    Publisher Elsevier BV
    Publishing country us
    Document type Article ; Online
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2020.127377
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  8. Article ; Online: The Influence of the Side Chain Structure on the Photostability of Low Band Gap Polymers.

    Bölke, Sven / Keller, Tina / Trilling, Florian / Forster, Michael / Scherf, Ullrich / Chassé, Thomas / Peisert, Heiko

    Molecules (Basel, Switzerland)

    2023  Volume 28, Issue 9

    Abstract: Side chains play an important role in the photo-oxidation process of low band gap (LBG) polymers. For example, it has been shown that their photostability can be increased by the introduction of aromatic-oxy-alkyl links. We studied the photostability of ... ...

    Abstract Side chains play an important role in the photo-oxidation process of low band gap (LBG) polymers. For example, it has been shown that their photostability can be increased by the introduction of aromatic-oxy-alkyl links. We studied the photostability of prototypical LBG polymers with alkyl and oxyalkyl side chains during irradiation with white light (AM 1.5 conditions) in dry air using UV/vis and IR spectroscopy. Though its degradation kinetics were distinctly affected by the presence or absence of oxygen in the structure of the side chains, in particular cases, the stability was more affected by the presence of linear or branched side chains. Moreover, we showed that the exact position of the alkyl/oxyalkyl side chain at the polymer backbone could be crucial. Although minor effects of chemical modifications on the electronic parameters (ionization potential and gap) were observed, the molecular orientation, determined by polarization modulation-infrared reflection-absorption spectroscopy (PMIRRAS), could be affected. The aggregation and crystallinity of these polymers may distinctly affect their stability.
    Language English
    Publishing date 2023-05-03
    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/molecules28093858
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  9. Article ; Online: Influence of Backbone Ladderization and Side Chain Variation on the Orientation of Diketopyrrolopyrrole-Based Donor-Acceptor Copolymers.

    Bölke, Sven / Früh, Andreas / Trilling, Florian / Forster, Michael / Scherf, Ullrich / Chassé, Thomas / Peisert, Heiko

    Molecules (Basel, Switzerland)

    2023  Volume 28, Issue 18

    Abstract: Ladder polymers with poly(diketopyrrolopyrrole) (DPP) moieties have recently attracted enormous interest for a large variety of opto-electronic applications. Since the rigidity of the backbone increases with ladderization, a strong influence on the self- ... ...

    Abstract Ladder polymers with poly(diketopyrrolopyrrole) (DPP) moieties have recently attracted enormous interest for a large variety of opto-electronic applications. Since the rigidity of the backbone increases with ladderization, a strong influence on the self-organization of thin films is expected. We study the molecular orientation of DPP-based ladder polymers in about 50 nm thin films using polarization modulation-infrared reflection-absorption spectroscopy (PM-IRRAS). Exemplarily, for one polymer, the orientation in thicker films is qualitatively investigated by infrared spectroscopy in transmission. Further, this method allows us to rule out the effects of a possible azimuthal ordering, which would affect the analysis of the orientation by PM-IRRAS. For all polymers, the long axis of the polymer backbone is preferentially oriented parallel to the substrate surface, pointing to a high degree of ordering. It is suggested that the choice of the side chains might be a promising way to tune for face-on and edge-on orientations. The exemplarily performed investigation of interface properties on substrates with different work functions suggests that the choice of the side chains has a minor effect on the interfacial electronic interface structure.
    Language English
    Publishing date 2023-09-05
    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/molecules28186435
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  10. Article ; Online: Biocompatible and Selective Generation of Bicyclic Peptides.

    Ullrich, Sven / George, Josemon / Coram, Alexandra E / Morewood, Richard / Nitsche, Christoph

    Angewandte Chemie (International ed. in English)

    2022  Volume 61, Issue 43, Page(s) e202208400

    Abstract: Bicyclic peptides possess superior properties for drug discovery; however, their chemical synthesis is not straightforward and often neither biocompatible nor fully orthogonal to all canonical amino acids. The selective reaction between 1,2-aminothiols ... ...

    Abstract Bicyclic peptides possess superior properties for drug discovery; however, their chemical synthesis is not straightforward and often neither biocompatible nor fully orthogonal to all canonical amino acids. The selective reaction between 1,2-aminothiols and 2,6-dicyanopyridine allows direct access to complex bicyclic peptides in high yield. The process can be fully automated using standard solid-phase peptide synthesis. Bicyclization occurs in water at physiological pH within minutes and without the need for a catalyst. The use of various linkers allows tailored bicyclic peptides with qualities such as plasma stability, conformational preorganization, and high target affinity. We demonstrate this for a bicyclic inhibitor of the Zika virus protease NS2B-NS3 as well as for bicyclic versions of the α-helical antimicrobial peptide aurein 1.2.
    MeSH term(s) Amino Acids ; Peptide Hydrolases ; Viral Nonstructural Proteins/chemistry ; Water ; Zika Virus/drug effects ; Peptides, Cyclic/pharmacology
    Chemical Substances Amino Acids ; Peptide Hydrolases (EC 3.4.-) ; Viral Nonstructural Proteins ; Water (059QF0KO0R) ; Peptides, Cyclic
    Language English
    Publishing date 2022-08-22
    Publishing country Germany
    Document type Journal Article ; Research Support, Non-U.S. Gov't
    ZDB-ID 2011836-3
    ISSN 1521-3773 ; 1433-7851
    ISSN (online) 1521-3773
    ISSN 1433-7851
    DOI 10.1002/anie.202208400
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