Bradley L. Pentelute
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Biochemist
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Bradley L. Pentelutebiology Degrees
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Biology
Bradley L. Pentelute's Degrees
- PhD Chemistry University of California, Berkeley
- Bachelors Chemistry University of California, Berkeley
Why Is Bradley L. Pentelute Influential?
(Suggest an Edit or Addition)According to Wikipedia, Bradley Lether Pentelute is currently a professor of chemistry at the Massachusetts Institute of Technology . His research program lies at the intersection of chemistry and biology and develops bioconjugation strategies, cytosolic delivery platforms, and rapid flow synthesis technologies to optimize the production, achieve site-specific modification, enhance stability, and modulate function of a variety of bioactive agents. His laboratory successfully modified proteins via cysteine-containing “pi-clamps” made up of a short sequence of amino acids, and delivered large biomolecules, such as various proteins and drugs, into cells via the anthrax delivery vehicle. Pentelute has also made several key contributions to automated synthesis technologies in flow. These advances includes the invention of the world's fastest polypeptide synthesizer. This system is able to form amide bonds at a more efficient rate than standard commercial equipment and has helped in the process of understanding protein folding and its mechanisms. This automated flow technology was recently used to achieve total chemical synthesis of protein chains up to 164 amino acids in length that retained the structure and function of native variants obtained by recombinant expression. The primary goal of his endeavor is to use these processes to create designer biologics that can be used to treat diseases and solve the manufacturing problem for on-demand personalized therapies, such as cancer vaccines.
Bradley L. Pentelute's Published Works
Number of citations in a given year to any of this author's works
Total number of citations to an author for the works they published in a given year. This highlights publication of the most important work(s) by the author
Published Works
- Evidence for a Common Mechanism of SIRT1 Regulation by Allosteric Activators (2013) (558)
- A perfluoroaryl-cysteine S(N)Ar chemistry approach to unprotected peptide stapling. (2013) (293)
- Organometallic Palladium Reagents for Cysteine Bioconjugation (2015) (274)
- Kinetically controlled ligation for the convergent chemical synthesis of proteins. (2006) (228)
- X-ray structure of snow flea antifreeze protein determined by racemic crystallization of synthetic protein enantiomers. (2008) (200)
- Killing by Bactericidal Antibiotics Does Not Depend on Reactive Oxygen Species (195)
- Blood-brain-barrier spheroids as an in vitro screening platform for brain-penetrating agents (2017) (182)
- A fully automated flow-based approach for accelerated peptide synthesis. (2017) (175)
- Personal neoantigen vaccines induce persistent memory T cell responses and epitope spreading in patients with melanoma (2021) (168)
- π-Clamp-mediated cysteine conjugation (2015) (164)
- Selective desulfurization of cysteine in the presence of Cys(Acm) in polypeptides obtained by native chemical ligation. (2007) (163)
- Blood–brain-barrier organoids for investigating the permeability of CNS therapeutics (2018) (149)
- Atomic structure of anthrax PA pore elucidates toxin translocation (2015) (118)
- Affinity-based capture and identification of protein effectors of the growth regulator ppGpp (2018) (117)
- Rapid Flow‐Based Peptide Synthesis (2014) (111)
- Arylation Chemistry for Bioconjugation. (2019) (107)
- Synthesis of proteins by automated flow chemistry (2020) (105)
- Investigation of ACE2 N-terminal fragments binding to SARS-CoV-2 Spike RBD (2020) (93)
- Atomic structure of anthrax protective antigen pore elucidates toxin translocation (2015) (90)
- The first-in-class peptide binder to the SARS-CoV-2 spike protein (2020) (87)
- Nitrogen Arylation for Macrocyclization of Unprotected Peptides. (2016) (84)
- Delivery of Antibody Mimics into Mammalian Cells via Anthrax Toxin Protective Antigen (2014) (78)
- Palladium-Mediated Arylation of Lysine in Unprotected Peptides. (2017) (76)
- Cholesterol-binding site of the influenza M2 protein in lipid bilayers from solid-state NMR (2017) (68)
- Mirror image forms of snow flea antifreeze protein prepared by total chemical synthesis have identical antifreeze activities. (2008) (64)
- Convergent chemical synthesis of [lysine(24,38,83)] human erythropoietin. (2012) (61)
- Protein thioester synthesis enabled by sortase. (2012) (60)
- Systematic Investigation of EDC/sNHS-Mediated Bioconjugation Reactions for Carboxylated Peptide Substrates. (2016) (57)
- Palladium Oxidative Addition Complexes for Peptide and Protein Cross-linking. (2018) (55)
- Divergent unprotected peptide macrocyclisation by palladium-mediated cysteine arylation† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c6sc05454d Click here for additional data file. (2016) (54)
- An Umpolung Approach for the Chemoselective Arylation of Selenocysteine in Unprotected Peptides (2015) (54)
- A chemoselective strategy for late-stage functionalization of complex small molecules with polypeptides and proteins (2018) (54)
- Convergent diversity-oriented side-chain macrocyclization scan for unprotected polypeptides. (2013) (54)
- Risk of rapid evolutionary escape from biomedical interventions targeting SARS-CoV-2 spike protein (2021) (51)
- Water-Soluble Palladium Reagents for Cysteine S-Arylation under Ambient Aqueous Conditions. (2017) (51)
- Flow-based enzymatic ligation by sortase A. (2014) (50)
- Perfluoroaryl Bicyclic Cell-Penetrating Peptides for Delivery of Antisense Oligonucleotides. (2018) (50)
- Enzymatic "click" ligation: selective cysteine modification in polypeptides enabled by promiscuous glutathione S-transferase. (2013) (49)
- Machine Learning To Predict Cell-Penetrating Peptides for Antisense Delivery (2018) (48)
- Site-Selective Cysteine-Cyclooctyne Conjugation. (2018) (47)
- Ultra-large chemical libraries for the discovery of high-affinity peptide binders (2020) (46)
- In-solution enrichment identifies peptide inhibitors of protein–protein interactions (2019) (45)
- Delivery of Non-Native Cargo into Mammalian Cells Using Anthrax Lethal Toxin. (2016) (44)
- Comparative properties of insulin-like growth factor 1 (IGF-1) and [Gly7D-Ala]IGF-1 prepared by total chemical synthesis. (2008) (43)
- Direct on-resin synthesis of peptide-alphathiophenylesters for use in native chemical ligation. (2006) (43)
- Perfluoroarene-Based Peptide Macrocycles to Enhance Penetration Across the Blood-Brain Barrier. (2017) (43)
- De Novo Discovery of High-Affinity Peptide Binders for the SARS-CoV-2 Spike Protein (2020) (41)
- A functional role of Rv1738 in Mycobacterium tuberculosis persistence suggested by racemic protein crystallography (2015) (40)
- Total chemical synthesis and X-ray structure of kaliotoxin by racemic protein crystallography. (2010) (40)
- Atomic Structures of Closed and Open Influenza B M2 Proton Channel Reveal the Conduction Mechanism (2020) (39)
- Design, total chemical synthesis, and X-ray structure of a protein having a novel linear-loop polypeptide chain topology. (2012) (38)
- Enzyme-Catalyzed Macrocyclization of Long Unprotected Peptides (2014) (38)
- X-ray structure of native scorpion toxin BmBKTx1 by racemic protein crystallography using direct methods. (2009) (38)
- Ultrasensitive detection of protein translocated through toxin pores in droplet-interface bilayers (2011) (36)
- A semisynthesis platform for investigating structure-function relationships in the N-terminal domain of the anthrax Lethal Factor. (2010) (36)
- Through the looking glass – a new world of proteins enabled by chemical synthesis (2012) (35)
- Enhancement of Peptide Vaccine Immunogenicity by Increasing Lymphatic Drainage and Boosting Serum Stability (2018) (34)
- Chemical dissection of protein translocation through the anthrax toxin pore. (2011) (34)
- Xenoprotein engineering via synthetic libraries (2018) (32)
- Three dimensional structure of the anthrax toxin translocon–lethal factor complex by cryo‐electron microscopy (2013) (31)
- Rapid Total Synthesis of DARPin pE59 and Barnase (2014) (31)
- Salt Effect Accelerates Site-Selective Cysteine Bioconjugation (2016) (29)
- d-Amino Acid Scan of Two Small Proteins. (2016) (28)
- Assembly of anthrax toxin pore: Lethal‐factor complexes into lipid nanodiscs (2013) (26)
- Use of model peptide reactions for the characterization of kinetically controlled ligation. (2011) (26)
- Library Design-Facilitated High-Throughput Sequencing of Synthetic Peptide Libraries. (2017) (25)
- A perfluoroaromatic abiotic analog of H2 relaxin enabled by rapid flow-based peptide synthesis. (2016) (25)
- Protein-Protein Cross-Coupling via Palladium-Protein Oxidative Addition Complexes from Cysteine Residues. (2020) (24)
- A d-Amino Acid at the N-Terminus of a Protein Abrogates Its Degradation by the N-End Rule Pathway (2015) (23)
- Translocation of Non-Canonical Polypeptides into Cells Using Protective Antigen (2015) (22)
- Delivery of mirror image polypeptides into cells† †Electronic supplementary information (ESI) available. See DOI: 10.1039/c4sc02078b Click here for additional data file. (2014) (21)
- Structure of HIV TAR in complex with a Lab-Evolved RRM provides insight into duplex RNA recognition and synthesis of a constrained peptide that impairs transcription (2018) (21)
- Risk of evolutionary escape from neutralizing antibodies targeting SARS-CoV-2 spike protein (2020) (21)
- Substrate Recognition of MARTX Ras/Rap1-Specific Endopeptidase. (2017) (21)
- Insights from atomic-resolution X-ray structures of chemically synthesized HIV-1 protease in complex with inhibitors. (2007) (20)
- Monitoring the kinetics of the pH-driven transition of the anthrax toxin prepore to the pore by biolayer interferometry and surface plasmon resonance. (2013) (20)
- Deep learning to design nuclear-targeting abiotic miniproteins (2021) (19)
- Mutations in pmrB Confer Cross-Resistance between the LptD Inhibitor POL7080 and Colistin in Pseudomonas aeruginosa (2019) (18)
- C-Terminal Modification of Fully Unprotected Peptide Hydrazides via in Situ Generation of Isocyanates. (2016) (18)
- Designing Well-Structured Cyclic Pentapeptides Based on Sequence-Structure Relationships. (2018) (18)
- Deep Learning for Prediction and Optimization of Fast-Flow Peptide Synthesis (2020) (16)
- Macrocyclization of Unprotected Peptide Isocyanates. (2016) (16)
- A structural and mechanistic study of π-clamp-mediated cysteine perfluoroarylation (2017) (15)
- Antibody–Bactericidal Macrocyclic Peptide Conjugates To Target Gram‐Negative Bacteria (2018) (15)
- Mucosal absorption of therapeutic peptides by harnessing the endogenous sorting of glycosphingolipids (2018) (15)
- Automated Flow Synthesis of Tumor Neoantigen Peptides for Personalized Immunotherapy (2020) (14)
- Discovery of a 29-Amino-Acid Reactive Abiotic Peptide for Selective Cysteine Arylation. (2018) (14)
- Discovery of Nucleic Acid Binding Molecules from Combinatorial Biohybrid Nucleobase Peptide Libraries. (2020) (13)
- A Perfluoroaryl-Cysteine S[subscript N]Ar Chemistry Approach to Unprotected Peptide Stapling (2013) (13)
- Amide-forming chemical ligation via O-acyl hydroxamic acids (2018) (13)
- A novel, safe, fast and efficient treatment for Her2‐positive and negative bladder cancer utilizing an EGF‐anthrax toxin chimera (2019) (13)
- A Platinum(IV) Prodrug - Perfluoroaryl Macrocyclic Peptide Conjugate Enhances Platinum Uptake in the Brain. (2020) (12)
- Palladium-Protein Oxidative Addition Complexes by Amine-Selective Acylation. (2020) (12)
- Following Natures Lead: On the Construction of Membrane-Inserted Toxins in Lipid Bilayer Nanodiscs (2015) (12)
- Total synthesis and biochemical characterization of mirror image barnase† †Electronic supplementary information (ESI) available: Materials, methods, and detailed experimental procedures. See DOI: 10.1039/c4sc03877k (2015) (12)
- Fully automated fast-flow synthesis of antisense phosphorodiamidate morpholino oligomers (2020) (12)
- Automated Flow Synthesis of Peptide–PNA Conjugates (2021) (10)
- Chimeras of Cell-Penetrating Peptides Demonstrate Synergistic Improvement in Antisense Efficacy. (2019) (10)
- Anthrax Protective Antigen Retargeted with Single‐Chain Variable Fragments Delivers Enzymes to Pancreatic Cancer Cells (2020) (10)
- Heterochiral Knottin Protein: Folding and Solution Structure. (2017) (10)
- Oligonucleotide Bioconjugation with Bifunctional Palladium Reagents. (2021) (8)
- Anthrax toxins regulate pain signaling and can deliver molecular cargoes into ANTXR2+ DRG sensory neurons (2021) (8)
- Single-wavelength phasing strategy for quasi-racemic protein crystal diffraction data. (2012) (8)
- Cell-penetrating peptides enhance peptide vaccine accumulation and persistence in lymph nodes to drive immunogenicity (2022) (8)
- Engineering Bioactive Dimeric Transcription Factor Analogs via Palladium Rebound Reagents. (2021) (8)
- Deep Learning Enables Discovery of a Short Nuclear Targeting Peptide for Efficient Delivery of Antisense Oligomers (2021) (7)
- Conformational Stabilization and Rapid Labeling of a 29-Residue Peptide by a Small Molecule Reaction Partner. (2019) (7)
- IgG-Engineered Protective Antigen for Cytosolic Delivery of Proteins into Cancer Cells (2021) (6)
- Total synthesis of himastatin (2021) (6)
- Targeting cancer gene dependencies with anthrax-mediated delivery of peptide nucleic acids. (2020) (6)
- Quantifying residue-specific conformational dynamics of a highly reactive 29-mer peptide (2020) (6)
- Total synthesis and biochemical characterization of mirror image barnase (2015) (6)
- Targeting Glioblastoma Using a Novel Peptide Specific to a Deglycosylated Isoform of Brevican (2021) (6)
- Parallel Automated Flow Synthesis of Covalent Protein Complexes That Can Inhibit MYC-Driven Transcription (2021) (5)
- Characterization of Novel Piperidine-Based Inhibitor of Cathepsin B-Dependent Bacterial Toxins and Viruses. (2018) (5)
- Conformational dynamics in extended RGD-containing peptides. (2020) (5)
- Through the Looking Glass —A New World of Proteins Enabled by Chemical Synthesis (2012) (5)
- Studies on a landscape of perfluoroaromatic-reactive peptides. (2018) (4)
- Interpretable Deep Learning for De Novo Design of Cell-Penetrating Abiotic Polymers (2020) (4)
- Rapid de novo discovery of peptidomimetic affinity reagents for human angiotensin converting enzyme 2 (2022) (4)
- Palladium-Mediated Incorporation of Carboranes into Small Molecules, Peptides, and Proteins. (2022) (4)
- Secondary Amino Alcohols: Traceless Cleavable Linkers for Use in Affinity Capture and Release. (2020) (4)
- A Tumor-Homing Peptide Platform Enhances Drug Solubility, Improves Blood–Brain Barrier Permeability and Targets Glioblastoma (2022) (3)
- Author Correction: Affinity-based capture and identification of protein effectors of the growth regulator ppGpp (2019) (3)
- tected peptide macrocyclisation by palladium-mediated cysteine arylation † (2017) (3)
- Synthesis of Peptide-αThiophenylesters for Native Chemical Ligation (2006) (3)
- Analyzing Dynamic Protein Complexes Assembled On and Released From Biolayer Interferometry Biosensor Using Mass Spectrometry and Electron Microscopy (2018) (3)
- Abstract A010: Personalized neoantigen-targeting vaccines for high-risk melanoma generate epitope spreading (2019) (2)
- Crystal Structure of the Snow Flea Antifreeze Protein (2008) (2)
- Palladium Mediated Synthesis of Protein-Polyarene Conjugates. (2022) (2)
- New chemical methods for the synthesis of proteins and their application to the elucidation of protein structure by racemic protein crystallography (2008) (2)
- Identification of N-Terminally Diversified GLP-1R Agonists Using Saturation Mutagenesis and Chemical Design. (2020) (2)
- Cell-Penetrating d-Peptides Retain Antisense Morpholino Oligomer Delivery Activity (2021) (2)
- Selective N-Arylation of p-Aminophenylalanine in Unprotected Peptides with Organometallic Palladium Reagents. (2021) (2)
- Introduction: Peptide Chemistry. (2020) (2)
- Efficient flow synthesis of human antimicrobial peptides. (2020) (2)
- Oligonucleotide Bioconjugation with Bifunctional Palladium Reagents (2021) (1)
- An in vivo selection-derived d-peptide for engineering erythrocyte-binding antigens that promote immune tolerance (2021) (1)
- DDIS-19. NOVEL PEPTIDE HOMING TO GLIOMA-SPECIFIC ISOFORM OF BREVICAN SELECTIVELY TARGETS MALIGNANT BRAIN TUMORS (2017) (1)
- Binary combinatorial scanning reveals potent poly-alanine-substituted inhibitors of protein-protein interactions (2022) (1)
- Anthrax Toxin as a Molecular Platform to Target Nociceptive Neurons and Modulate Pain (2020) (1)
- Author Correction: In-solution enrichment identifies peptide inhibitors of protein–protein interactions (2019) (1)
- Machine Learning Guides Peptide Nucleic Acid Flow Synthesis and Sequence Design (2021) (1)
- Editorial overview: Chemistry for biopolymers to investigate and even move beyond nature. (2016) (1)
- Erythrocyte-targeted immunomodulatory antigens enabled by in vivo selection of D-peptides (2020) (1)
- Automated affinity selection for rapid discovery of peptide binders (2021) (1)
- BTP-7, a novel peptide for therapeutic targeting of malignant brain tumors (2020) (1)
- Deep Alanine Scanning Reveals Potent Multi-alanine-substituted Protein–protein Interaction Inhibitors (2021) (1)
- Abiotic peptides as carriers of information for the encoding of small-molecule library synthesis (2023) (1)
- Quantifying residue-specific conformational dynamics of a highly reactive 29-mer peptide (2020) (0)
- Rapid Single-Shot Synthesis of the 217 Amino Acid-Long N-Terminal Domain of Pyocin S2 (2022) (0)
- Influenza B M2 Proton Channel in the Closed State - SSNMR Structure at pH 7.5 (2020) (0)
- Development of an antibody fused with an antimicrobial peptide targeting Pseudomonas aeruginosa: a new approach to prevent and treat bacterial infections (2022) (0)
- Protein Thioester Synthesis Enabled by Sortase Citation (2012) (0)
- A Pt(IV)-conjugated brain penetrant macrocyclic peptide shows pre-clinical efficacy in glioblastoma. (2022) (0)
- 504: Development of a novel antibiotic class that overcomes intrinsic gram-negative antibiotic resistance (2021) (0)
- 544 Oligomerization mediates mammalian cell toxicity of the human antimicrobial peptide LL-37 (2022) (0)
- Snow Flea Antifreeze Protein Quasi-racemate (2008) (0)
- C-Terminal Modification of Fully Unprotected Peptide Hydrazides (2016) (0)
- A reactive peptide interface for site-selective cysteine bioconjugation. (2021) (0)
- Titelbild: Kinetically Controlled Ligation for the Convergent Chemical Synthesis of Proteins (Angew. Chem. 24/2006) (2006) (0)
- DDRE-47. ASSESSMENT OF BRAIN PENETRANCE, BIODISTRIBUTION, AND EFFICACY OF PLATINUM (IV)-CONJUGATED FLUORINATED MACROCYCLIC CELL-PENETRATING PEPTIDES IN A MURINE GLIOBLASTOMA MODEL (2021) (0)
- d biochemical characterization of mirror image barnase † (2015) (0)
- Rapid Total Synthesis of DARPin pE59 and RNase B. a (2014) (0)
- PS2 - 178 Brevican-Specific Peptides for the Development of Next-Generation Targeted Theranostics for High Grade Gliomas (2016) (0)
- Cover Picture: Kinetically Controlled Ligation for the Convergent Chemical Synthesis of Proteins (Angew. Chem. Int. Ed. 24/2006) (2006) (0)
- Correction to "Palladium-Mediated Incorporation of Carboranes into Small Molecules, Peptides, and Proteins". (2022) (0)
- X-ray Crystal Structure of L-Plectasin (2009) (0)
- Snow Flea Antifreeze Protein Racemate (2008) (0)
- Blood–brain-barrier organoids for investigating the permeability of CNS therapeutics (2018) (0)
- Selective N‐Arylation of p ‐Aminophenylalanine in Unprotected Peptides with Organometallic Palladium Reagents (2021) (0)
- X-ray Crystal Structure of Racemic Plectasin (2009) (0)
- A transferrin receptor 1-targeted PNA-peptide conjugate inhibits microRNA-21 expression in cardiac and other mouse tissues (2023) (0)
- Influenza B M2 Proton Channel in the Open State - SSNMR Structure at pH 4.5 (2020) (0)
- Structure of HIV-1 TAR in complex with a lab-evolved protein provides insight into RNA recognition and synthesis of a constrained peptide that impairs transcription (2018) (0)
- Xray structure of scorpion toxin BmBKTx1 (2009) (0)
- Branched multimeric peptides as affinity reagents for detection of α-Klotho protein (2023) (0)
- ATPS-08DISCOVERY OF NOVEL GLIOMA-TARGETING PEPTIDES USING A HIGH-THROUGHPUT MICROFLUIDIC MAGNETIC-ACTIVATED SORTER (2015) (0)
- Ultra-large chemical libraries for the discovery of high-affinity peptide binders (2020) (0)
- A structural and mechanistic study of π-clamp-mediated cysteine perfluoroarylation (2017) (0)
- CryoEM single particle reconstruction of anthrax toxin protective antigen pore at 2.9 Angstrom resolution (2015) (0)
- Pd-mediated Arylation of Lysine in Unprotected Peptides (2017) (0)
- Automated Fast-Flow Synthesis of Peptide Nucleic Acid Conjugates (2021) (0)
- X-ray structure of kaliotoxin by racemic protein crystallography (2010) (0)
- Automated Flow Synthesis of Tumor Neoantigen Peptides for Personalized Immunotherapy (2020) (0)
- Mutations in pmrB confer cross-resistance to the LptD inhibitor POL7080 and colistin in Pseudomonas aeruginosa (2019) (0)
- Following Natures Lead: On the Construction of Membrane-Inserted Toxins in Lipid Bilayer Nanodiscs (2015) (0)
- Palladium–peptide oxidative addition complexes for bioconjugation (2022) (0)
- EXTH-51. BREVICAN-SPECIFIC PEPTIDES FOR THE DEVELOPMENT OF NEXT-GENERATION TARGETED THERANOSTICS FOR MALIGNANT GLIOMAS (2016) (0)
- In-cell penetration selection—mass spectrometry produces noncanonical peptides for antisense delivery (2022) (0)
- Studies on a landscape of per fl uoroaromatic-reactive peptides † (2018) (0)
- DDIS-12. A FACILE, ROBUST AND PREDICTIVE IN VITRO BLOOD-BRAIN-BARRIER MODEL FOR HIGH-THROUGHPUT SCREENING AND DISCOVERY OF BRAIN-PENETRATING AGENTS (2016) (0)
- image polypeptides into cells † (2014) (0)
- Correction to "Protein-Protein Cross-Coupling via Palladium-Protein Oxidative Addition Complexes from Cysteine Residues". (2020) (0)
- Atomic structures of closed and open influenza B M2 proton channel reveal the conduction mechanism (2020) (0)
- X-ray crystal structure of a novel topological analogue of crambin (2012) (0)
- Automated Fast Flow Peptide Synthesis (2021) (0)
- 2.9-Å Resolution Structure of Anthrax Protective Antigen Pore Determined by Cryo Electron Microscopy (2016) (0)
- DDIS-36. BTP-7, A NOVEL PEPTIDE FOR THERAPEUTIC TARGETING OF MALIGNANT BRAIN TUMORS (2019) (0)
- DDIS-26. BTP-7, A NOVEL PEPTIDE FOR THERAPEUTIC TARGETING OF MALIGNANT BRAIN TUMORS (2018) (0)
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