Timothy A. Hill

Experimenteller Nachweis der metallbezogenen Funktion eines Cyanobactins

Philipp Baur, Timothy A. Hill, Kai‐Chen Wu, Junxian Lim et autres

ZUSAMMENFASSUNG Das Cyanobakterium Prochloron didemni produziert makrozyklische Oktapeptide mit Thiazol‐ und Oxazolin‐Heterozyklen, die als Patellamide bezeichnet werden. Interessanterweise konnte beobachtet werden, dass die Koordination von Cu 2+ an die Patellamide wahrscheinlich mit ihrer biologischen Funktion zusammenhängt. Zunächst zeigen wir, dass die Injektion …

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Experimental Evidence for a Metal‐Related Function of a Cyanobactin

Philipp Baur, Timothy A. Hill, Kai‐Chen Wu, Junxian Lim et autres

ABSTRACT The cyanobacterium Prochloron didemni produces macrocyclic octapeptides with thiazole and oxazoline heterocycles, known as patellamides. An interesting observation is that Cu 2+ binding to the patellamides is likely to be related to their biological function. First, we show that Cu 2 …

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Liver microsome stability of N-methylated cyclic hexapeptides is decreased by the presence of cis-amide bonds

Huy N. Hoang, David P. Fairlie, Timothy A. Hill

N-methylation of cyclic peptides is a widely used strategy to enhance membrane permeability; however, it can also influence metabolic stability. In celebration of Professor David Craik’s scientific achievements – particularly in the field of peptide research – we were fortunate to gain …

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How Isomer and Conformer Structures Impact Dissociation Dynamics of Alkane Radical Cations

Madison K. Minvielle, Mikaela Aftel, Timothy A. Hill, Hugo A. López Peña et autres

High Resolution Image Download MS PowerPoint Slide Ionization of alkanes to form radical cations activates their otherwise unreactive C–H bonds, facilitating important chemical processes such as hydrocarbon cracking. This work investigates the radical cation dissociation dynamics of hexane (C 6 H 14 …

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Wnt dose escalation during the exit from pluripotency identifies tranilast as a regulator of cardiac mesoderm

Zhixuan Wu, Sophie Shen, Dalia Mizikovsky, Yuanzhao Cao et autres

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Protease-activated receptor 2 attenuates doxorubicin-induced apoptosis in colon cancer cells

Himani Shah, Timothy A. Hill, Junxian Lim, David P. Fairlie

Drug resistance represents a major problem in cancer treatment. Doxorubicin (adriamycin) is an injectable DNA intercalating drug that halts cancer cell growth by inhibiting topoisomerase 2, but its long-term effectiveness is compromised by onset of resistance. This study demonstrates that expression of …

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CCDC 1002286: Experimental Crystal Structure Determination

Timothy A. Hill, Rink‐Jan Lohman, Huy N. Hoang, Daniel S. Nielsen et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

Wollamide Cyclic Hexapeptides Synergize with Established and New Tuberculosis Antibiotics in Targeting Mycobacterium tuberculosis

Rachel F. Rollo, Giorgia Mori, Timothy A. Hill, Doris Hillemann et autres

Tuberculosis (TB) is an infectious disease that affects millions of people globally, with 1.6 million deaths annually. TB treatment requires combinations of multiple different antibiotics for many months, and toxic side effects can occur. Therefore, shorter, safer, more effective TB therapies are …

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Data from A Novel Class of Anticancer Compounds Targets the Actin Cytoskeleton in Tumor Cells

Justine Stehn, Nikolas K. Haass, Teresa Bonello, Melissa Desouza et autres

Abstract The actin cytoskeleton is a potentially vulnerable property of cancer cells, yet chemotherapeutic targeting attempts have been hampered by unacceptable toxicity. In this study, we have shown that it is possible to disrupt specific actin filament populations by targeting isoforms of …

Supplementary Methods from A Novel Class of Anticancer Compounds Targets the Actin Cytoskeleton in Tumor Cells

Justine Stehn, Nikolas K. Haass, Teresa Bonello, Melissa Desouza et autres

PDF file - 129K, Supplementary Experimental Methods: Animal studies: Detailed methods outlining the in vivo TR100 animal studies. Tropomyosin compound modeling: Detailed method outlining the in silico modeling of Tm5NM1.

Supplementary Figures 1 - 7, Table 1 from A Novel Class of Anticancer Compounds Targets the Actin Cytoskeleton in Tumor Cells

Justine Stehn, Nikolas K. Haass, Teresa Bonello, Melissa Desouza et autres

PDF file - 1137K, Supplementary Figure 1: Tropomyosin siRNA knockdown is isoform specific and does not result in any compensation. Supplementary Figure 2: TR100 nullifies the impact of Tm5NM1 on actin filament depolymerization kinetics. Supplementary Figure 3: Anti-Tropomyosin compound impact on the …

Supplementary Methods from A Novel Class of Anticancer Compounds Targets the Actin Cytoskeleton in Tumor Cells

Justine Stehn, Nikolas K. Haass, Teresa Bonello, Melissa Desouza et autres

PDF file - 129K, Supplementary Experimental Methods: Animal studies: Detailed methods outlining the in vivo TR100 animal studies. Tropomyosin compound modeling: Detailed method outlining the in silico modeling of Tm5NM1.