Chemistry & Biology
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#1Brett M. Babin (Stanford University)H-Index: 8
#2Laura J. Keller (Stanford University)H-Index: 3
Last. Matthew Bogyo (Stanford University)H-Index: 88
view all 10 authors...
Summary null The increasing incidence of antibiotic-resistant Mycobacterium tuberculosis infections is a global health threat necessitating the development of new antibiotics. Serine hydrolases (SHs) are a promising class of targets because of their importance for the synthesis of the mycobacterial cell envelope. We screen a library of small molecules containing serine-reactive electrophiles and identify narrow-spectrum inhibitors of M. tuberculosis growth. Using these lead molecules, we perform...
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#1Michael Li (SBU: Stony Brook University)H-Index: 1
#2Hiren V. Patel (SBU: Stony Brook University)H-Index: 5
Last. Benjamin F. Cravatt (Scripps Research Institute)H-Index: 146
view all 11 authors...
The identification and validation of a small molecule's targets is a major bottleneck in the discovery process for tuberculosis antibiotics. Activity-based protein profiling (ABPP) is an efficient tool for determining a small molecule's targets within complex proteomes. However, how target inhibition relates to biological activity is often left unexplored. Here, we study the effects of 1,2,3-triazole ureas on Mycobacterium tuberculosis (Mtb). After screening ∼200 compounds, we focus on 4 compoun...
1 CitationsSource
#1Stella M. K. Glasauer (UCSB: University of California, Santa Barbara)H-Index: 4
#2Therese Triemer (UZH: University of Zurich)H-Index: 3
Last. Nathan W. Luedtke (McGill University)H-Index: 33
view all 5 authors...
Asymmetric inheritance of sister chromatids has long been predicted to be linked to discordant fates of daughter cells and even hypothesized to minimize accumulation of mutations in stem cells. Here, we use (2'S)-2'-deoxy-2'-fluoro-5-ethynyluridine (F-ara-EdU), bromodeoxyuridine (BrdU), and light sheet microscopy to track embryonic DNA in whole zebrafish. Larval development results in rapid depletion of older DNA template strands from stem cell niches in the retina, brain, and intestine. Prolong...
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#1Margaret Elizabeth Brousseau (Novartis)H-Index: 2
#2Kevin Clairmont (Novartis)H-Index: 3
Last. Shari L. Caplan (Novartis)H-Index: 7
view all 42 authors...
Summary null null Proprotein convertase subtilisin/kexin type 9 (PCSK9) regulates plasma low-density lipoprotein cholesterol (LDL-C) levels by promoting hepatic LDL receptor (LDLR) degradation. Therapeutic antibodies that disrupt PCSK9-LDLR binding reduce LDL-C concentrations and cardiovascular disease risk. The epidermal growth factor precursor homology domain A (EGF-A) of the LDLR serves as a primary contact with PCSK9 via a flat interface, presenting a challenge for identifying small molecule...
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#1Martha C. Taubert (Technische Universität Darmstadt)
#2Felix Hausch (Technische Universität Darmstadt)H-Index: 31
Bone morphogenetic protein (BMP) signaling contributes to acute kidney injury (AKI), a common disease without adequate treatment options. In this issue of Cell Chemical Biology, Larraufie, Gao and colleagues (Larraufie et al., 2021) show that FKBP12 inhibition can be a target for treatment of AKI via activation of BMP signaling.
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#1Maximilian Staudt (University of Freiburg)
#2Manfred Jung (University of Freiburg)H-Index: 63
Use of hypoxia-activated prodrugs has emerged as a strategy for selectively targeting tumors in hypoxic conditions harboring reductive environments. In this issue of Cell Chemical Biology, Skwarska et al. (2021) report a hypoxia-activated prodrug targeting histone deacetylases (lysine deacetylases, KDACs) selectively over normoxic cells with activity in an animal model.
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#1Joyce H. Lee (JHUSOM: Johns Hopkins University School of Medicine)H-Index: 3
#2Eric P. Mosher (JHUSOM: Johns Hopkins University School of Medicine)H-Index: 1
Last. James M. Berger (JHUSOM: Johns Hopkins University School of Medicine)H-Index: 81
view all 5 authors...
Summary null null Topoisomerase II (topo II) is essential for disentangling newly replicated chromosomes. DNA unlinking involves the physical passage of one duplex through another and depends on the transient formation of double-stranded DNA breaks, a step exploited by frontline chemotherapeutics to kill cancer cells. Although anti-topo II drugs are efficacious, they also elicit cytotoxic side effects in normal cells; insights into how topo II is regulated in different cellular contexts is essen...
1 CitationsSource
#1R Kunder (NU: Northwestern University)
#2Michelle Velyunskiy (NU: Northwestern University)
Last. Alesia Vialichka (NU: Northwestern University)
view all 20 authors...
Triple-negative breast cancer (TNBC) is the breast cancer subtype with the poorest clinical outcome. The PIM family of kinases has emerged as a factor that is both overexpressed in TNBC and associated with poor outcomes. Preclinical data suggest that TNBC with an elevated MYC expression is sensitive to PIM inhibition. However, clinical observations indicate that the efficacy of PIM inhibitors as single agents may be limited, suggesting the need for combination therapies. Our screening effort ide...
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#1Daisuke Yamane (Institute of Medical Science)H-Index: 21
#2Yuri Hayashi (Ochanomizu University)H-Index: 2
Last. Ikuyo Ichi (Ochanomizu University)H-Index: 17
view all 8 authors...
Summary null null The metabolic oxidative degradation of cellular lipids severely restricts replication of hepatitis C virus (HCV), a leading cause of chronic liver disease, but little is known about the factors regulating this process in infected cells. Here we show that HCV is restricted by an iron-dependent mechanism resembling the one triggering ferroptosis, an iron-dependent form of non-apoptotic cell death, and mediated by the non-canonical desaturation of oleate to Mead acid and other hig...
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#1Rosanne Persaud (UBC: University of British Columbia)
#2Sheena C. Li (U of T: University of Toronto)H-Index: 10
Last. Mami YoshimuraH-Index: 5
view all 16 authors...
The pathogen Mycobacterium tuberculosis (Mtb) evades the innate immune system by interfering with autophagy and phagosomal maturation in macrophages, and, as a result, small molecule stimulation of autophagy represents a host-directed therapeutics (HDTs) approach for treatment of tuberculosis (TB). Here we show the marine natural product clionamines activate autophagy and inhibit Mtb survival in macrophages. A yeast chemical-genetics approach identified Pik1 as target protein of the clionamines....
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