Thomas S. Peat
YOU?
Author Swipe
View article: An ureido-substituted benzenesulfonamide carbonic anhydrase inhibitor exerts a potent antitumor effect in vitro and in vivo
An ureido-substituted benzenesulfonamide carbonic anhydrase inhibitor exerts a potent antitumor effect in vitro and in vivo Open
View article: Structural insights into the enzymatic breakdown of azomycin-derived antibiotics by 2-nitroimdazole hydrolase (NnhA)
Structural insights into the enzymatic breakdown of azomycin-derived antibiotics by 2-nitroimdazole hydrolase (NnhA) Open
View article: 4-(Pyrazolyl)benzenesulfonamide Ureas as Carbonic Anhydrases Inhibitors and Hypoxia-Mediated Chemo-Sensitizing Agents in Colorectal Cancer Cells
4-(Pyrazolyl)benzenesulfonamide Ureas as Carbonic Anhydrases Inhibitors and Hypoxia-Mediated Chemo-Sensitizing Agents in Colorectal Cancer Cells Open
Hypoxia in tumors contributes to chemotherapy resistance, worsened by acidosis driven by carbonic anhydrases (hCA IX and XII). Targeting these enzymes can mitigate acidosis, thus enhancing tumor sensitivity to cytotoxic drugs. Herei…
View article: Vγ9Vδ2 T cells recognize butyrophilin 2A1 and 3A1 heteromers
Vγ9Vδ2 T cells recognize butyrophilin 2A1 and 3A1 heteromers Open
View article: Enhancing the Imine Reductase Activity of a Promiscuous Glucose Dehydrogenase for Scalable Manufacturing of a Chiral Neprilysin Inhibitor Precursor
Enhancing the Imine Reductase Activity of a Promiscuous Glucose Dehydrogenase for Scalable Manufacturing of a Chiral Neprilysin Inhibitor Precursor Open
Imine reductases (IREDs) have been identified as an important class of biocatalysts to synthesize chiral secondary amines with substantial promise for industrial application. Here, we report the promiscuous imine reductase activity of a gl…
View article: Enhancing PET Degrading Enzymes: A Combinatory Approach
Enhancing PET Degrading Enzymes: A Combinatory Approach Open
Plastic waste has become a substantial environmental issue. A potential strategy to mitigate this problem is to use enzymatic hydrolysis of plastics to depolymerize post‐consumer waste and allow it to be reused. Over the last few decades, …
View article: Characterization of novel mevalonate kinases from the tardigrade <i>Ramazzottius varieornatus</i> and the psychrophilic archaeon <i>Methanococcoides burtonii</i>
Characterization of novel mevalonate kinases from the tardigrade <i>Ramazzottius varieornatus</i> and the psychrophilic archaeon <i>Methanococcoides burtonii</i> Open
Mevalonate kinase is central to the isoprenoid biosynthesis pathway. Here, high-resolution X-ray crystal structures of two mevalonate kinases are presented: a eukaryotic protein from Ramazzottius varieornatus and an archaeal protein from M…
View article: Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer Open
View article: Data from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i>
Data from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i> Open
Elevated expression of insulin-like growth factor-II (IGF-II) is frequently observed in a variety of human malignancies, including breast, colon, and liver cancer. As IGF-II can deliver a mitogenic signal through both IGF-IR and an alterna…
View article: Supplementary Table from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i>
Supplementary Table from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i> Open
Supplementary Table from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines In vitro and In vivo
View article: Data from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i>
Data from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i> Open
Elevated expression of insulin-like growth factor-II (IGF-II) is frequently observed in a variety of human malignancies, including breast, colon, and liver cancer. As IGF-II can deliver a mitogenic signal through both IGF-IR and an alterna…
View article: Supplementary Table from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i>
Supplementary Table from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines <i>In vitro</i> and <i>In vivo</i> Open
Supplementary Table from A Human Monoclonal Antibody against Insulin-Like Growth Factor-II Blocks the Growth of Human Hepatocellular Carcinoma Cell Lines In vitro and In vivo
View article: Molecular characterization of cyanobacterial short‐chain prenyltransferases and discovery of a novel <scp>GGPP</scp> phosphatase
Molecular characterization of cyanobacterial short‐chain prenyltransferases and discovery of a novel <span>GGPP</span> phosphatase Open
Cyanobacteria are photosynthetic prokaryotes with strong potential to be used for industrial terpenoid production. However, the key enzymes forming the principal terpenoid building blocks, called short‐chain prenyltransferases (SPTs), are …
View article: Design of a methotrexate-controlled chemical dimerization system and its use in bio-electronic devices
Design of a methotrexate-controlled chemical dimerization system and its use in bio-electronic devices Open
Natural evolution produced polypeptides that selectively recognize chemical entities and their polymers, ranging from ions to proteins and nucleic acids. Such selective interactions serve as entry points to biological signaling and metabol…
View article: Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors
Privileged scaffolds in medicinal chemistry: Studies on pyrazolo[1,5-a]pyrimidines on sulfonamide containing Carbonic Anhydrase inhibitors Open
View article: Abstract 1130: First-in-class KAT6A/KAT6B inhibitor CTx-648 (PF-9363) demonstrates potent anti-tumor activity in ER+ breast cancer with KAT6A dysregulation
Abstract 1130: First-in-class KAT6A/KAT6B inhibitor CTx-648 (PF-9363) demonstrates potent anti-tumor activity in ER+ breast cancer with KAT6A dysregulation Open
KAT6A is a lysine histone acetyltransferase (HAT) of the MYST family of HATs. KAT6A, and its paralog KAT6B, have been shown to acetylate histone H3K23Ac and regulate diverse biological processes, including transcription, cell-cycle progres…
View article: The Glitazone Class of Drugs as Carbonic Anhydrase Inhibitors—A Spin-Off Discovery from Fragment Screening
The Glitazone Class of Drugs as Carbonic Anhydrase Inhibitors—A Spin-Off Discovery from Fragment Screening Open
The approved drugs that target carbonic anhydrases (CA, EC 4.2.1.1), a family of zinc metalloenzymes, comprise almost exclusively of primary sulfonamides (R-SO2NH2) as the zinc binding chemotype. New clinical applications for CA inhibitors…
View article: Structure-guided selection of puromycin N-acetyltransferase mutants with enhanced selection stringency for deriving mammalian cell lines expressing recombinant proteins
Structure-guided selection of puromycin N-acetyltransferase mutants with enhanced selection stringency for deriving mammalian cell lines expressing recombinant proteins Open
View article: The X-ray crystal structure of the N-terminal domain of Ssr4, a <i>Schizosaccharomyces pombe</i> chromatin-remodelling protein
The X-ray crystal structure of the N-terminal domain of Ssr4, a <i>Schizosaccharomyces pombe</i> chromatin-remodelling protein Open
Ssr4 is a yeast protein from Schizosaccharomyces pombe and is an essential part of the chromatin-remodelling [SWI/SNF and RSC (remodelling the structure of chromatin)] complexes found in S. pombe . These complexes (or their homologues) reg…
View article: Crystal structures of human ENPP1 in apo and bound forms
Crystal structures of human ENPP1 in apo and bound forms Open
Cancer is one of the leading causes of mortality in humans, and recent work has focused on the area of immuno-oncology, in which the immune system is used to specifically target cancerous cells. Ectonucleotide pyrophosphatase/phosphodieste…
View article: Azidothymidine “Clicked” into 1,2,3-Triazoles: First Report on Carbonic Anhydrase–Telomerase Dual-Hybrid Inhibitors
Azidothymidine “Clicked” into 1,2,3-Triazoles: First Report on Carbonic Anhydrase–Telomerase Dual-Hybrid Inhibitors Open
Cancer cells rely on the enzyme telomerase (EC 2.7.7.49) to promote cellular immortality. Telomerase inhibitors (i.e., azidothymidine) can represent promising antitumor agents, although showing high toxicity when administered alone. Better…
View article: Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action
Discovery of Potent Dual-Tailed Benzenesulfonamide Inhibitors of Human Carbonic Anhydrases Implicated in Glaucoma and in Vivo Profiling of Their Intraocular Pressure-Lowering Action Open
The design of three dual-tailed sulfonamide series 11a-11g, 14a-14h, and 16a-16e as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors are presented. All compounds were evaluated for inhibitory action against pharmacologic…
View article: HBO1 is required for the maintenance of leukaemia stem cells
HBO1 is required for the maintenance of leukaemia stem cells Open
View article: Fragment screening for a protein-protein interaction inhibitor to WDR5
Fragment screening for a protein-protein interaction inhibitor to WDR5 Open
The WD40-repeat protein WDR5 scaffolds various epigenetic writers and is a critical component of the mammalian SET/MLL histone methyltransferase complex. Dysregulation of the MLL1 catalytic function is associated with mixed-lineage leukemi…
View article: The evolving story of AtzT, a periplasmic binding protein
The evolving story of AtzT, a periplasmic binding protein Open
Atrazine is an s -triazine-based herbicide that is used in many countries around the world in many millions of tons per year. A small number of organisms, such as Pseudomonas sp. strain ADP, have evolved to use this modified s -triazine as…
View article: Structural basis for the allosteric regulation of the SbtA bicarbonate transporter by the P<sub>II</sub>-like protein, SbtB, from<i>Cyanobium</i>sp. PCC7001
Structural basis for the allosteric regulation of the SbtA bicarbonate transporter by the P<sub>II</sub>-like protein, SbtB, from<i>Cyanobium</i>sp. PCC7001 Open
Cyanobacteria have evolved a suite of enzymes and inorganic carbon (C i ) transporters that improve photosynthetic performance by increasing the localized concentration of CO 2 around the primary CO 2 -fixating enzyme, Rubisco. This CO 2 -…
View article: Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity
Synthesis of novel tellurides bearing benzensulfonamide moiety as carbonic anhydrase inhibitors with antitumor activity Open
View article: Structures of the transcriptional regulator BgaR, a lactose sensor
Structures of the transcriptional regulator BgaR, a lactose sensor Open
The structure of BgaR, a transcriptional regulator of the lactose operon in Clostridium perfringens , has been solved by SAD phasing using a mercury derivative. BgaR is an exquisite sensor of lactose, with a binding affinity in the low-mic…
View article: Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects
Benzensulfonamides bearing spyrohydantoin moieties act as potent inhibitors of human carbonic anhydrases II and VII and show neuropathic pain attenuating effects Open
View article: Development of small molecule STING agonists that can evoke host anti-cancer immune defences following local or systemic delivery
Development of small molecule STING agonists that can evoke host anti-cancer immune defences following local or systemic delivery Open
Background:\n\nSTING is a ubiquitously expressed innate immune sensor which is essential for the production of host defence-related proteins including type I interferons and proinflammatory cytokines that promote the recruitment and effect…