Evolution-inspired engineering of nonribosomal peptide synthetases
Editor’s summary Many clinically used drugs are derived from natural microbial products that are assembled in a stepwise fashion by the condensation of amino acids
Editor’s summary Many clinically used drugs are derived from natural microbial products that are assembled in a stepwise fashion by the condensation of amino acids
Abstract K-Ras is the most commonly mutated oncogene in human cancer. The recently approved non-small cell lung cancer drugs sotorasib and adagrasib covalently capture an
Abstract Background The first-in-class brain-penetrating synthetic hydroxylated lipid idroxioleic acid (2-OHOA; sodium 2-hydroxyoleate), activates sphingomyelin synthase expression and regulates membrane-lipid composition and mitochondrial energy production,
Editor’s summary Many small-molecule antibiotics target the bacterial ribosome, and there are many corresponding ribosome modifications that confer resistance by reducing the binding affinity of
Abstract SLC15A4 is an endolysosome-resident transporter linked with autoinflammation and autoimmunity. Specifically, SLC15A4 is critical for Toll-like receptors (TLRs) 7–9 as well as nucleotide-binding oligomerization
Highlights Summary Drug-resistant Mycobacterium tuberculosis (Mtb) remains a major public health concern requiring complementary approaches to standard anti-tuberculous regimens. Anti-virulence molecules or compounds that enhance the activity
Abstract Teixobactin is a cyclic undecadepsipeptide that has shown excellent potency against multidrug-resistant pathogens, such as methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococci (VRE). In this article, we
Abstract Myeloid cells are known to suppress antitumour immunity1. However, the molecular drivers of immunosuppressive myeloid cell states are not well defined. Here we used
Some people in hospital die not from the illness or accident that got them admitted but from germs they catch once there. In the United
Summary Inspired by nature, modern nanotechnology has enabled the bottom-up construction of molecular machines and nanorobots using two different biomolecular building blocks, DNAs or peptides. As an
Significance Streptococcus pneumoniae is an important bacterial pathogen responsible for many serious infections worldwide. Infections are often treated with penicillin antibiotics. This provides a selection pressure
Abstract Increasing levels of artemisinin and partner drug resistance threaten malaria control and elimination globally. Triple artemisinin-based combination therapies (TACTs) which combine artemisinin derivatives with
Abstract Pseudomonas aeruginosa is an opportunistic pathogen that causes serious illness, especially in immunocompromised individuals. P. aeruginosa forms biofilms that contribute to growth and persistence in a wide
Abstract The peripheral T cell repertoire of healthy individuals contains self-reactive T cells1,2. Checkpoint receptors such as PD-1 are thought to enable the induction of
Highlights Summary CDK2 is a core cell-cycle kinase that phosphorylates many substrates to drive progression through the cell cycle. CDK2 is hyperactivated in multiple cancers
Abstract Escherichia coli is a leading cause of invasive bacterial infections in humans. Capsule polysaccharide has an important role in bacterial pathogenesis, and the K1 capsule
Abstract Lymphangioleiomyomatosis (LAM) is a rare, progressive lung disease that predominantly affects women. LAM cells carry TSC1/TSC2 mutations, causing mTORC1 hyperactivation and uncontrolled cell growth. mTORC1 inhibitors
Abstract The development of new immunotherapies to treat the inflammatory mechanisms that sustain atherosclerotic cardiovascular disease (ASCVD) is urgently needed. Herein, we present a path
Significance In time and money, one of the most expensive steps of the drug discovery pipeline is the experimental screening of small molecules to determine
Summary Background Valbenazine is a highly selective vesicular monoamine transporter 2 (VMAT2) inhibitor approved for treatment of tardive dyskinesia. To address the ongoing need for
Abstract Antibiotic resistance is a pressing healthcare challenge and is mediated by various mechanisms, including the active export of drugs via multidrug efflux systems, which
Abstract Background We aimed to establish the causal effects of lowering sclerostin, target of the anti-osteoporosis drug romosozumab, on atherosclerosis and its risk factors. Methods
Abstract Dysfunction of either the right or left ventricle can lead to heart failure (HF) and subsequent morbidity and mortality. We performed a genome-wide association
Abstract Proliferating Cell Nuclear Antigen (PCNA) is a highly conserved protein essential for DNA replication, repair and scaffold functions in the cytosol. Specific inhibition of
Abstract A substantial proportion of cancer patients do not benefit from platinum-based chemotherapy (CT) due to the emergence of drug resistance. Here, we apply elemental
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