B. Safina

发表

Immune-stimulating antibody conjugates elicit robust myeloid activation and durable antitumor immunity

Sean C. Bendall, Michael N. Alonso, J. Melrose, 2020, Nature Cancer.

Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors.

Jun Liang, J. Blake, B. Brandhuber, 2012, Journal of medicinal chemistry.

Pyrrolobenzodiazepine Dimer Antibody-Drug Conjugates: Synthesis and Evaluation of Noncleavable Drug-Linkers.

Jeffrey T. Lau, BinQing Wei, S. Spencer, 2017, Journal of medicinal chemistry.

Antibody-Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo.

Jeffrey T. Lau, R. Rowntree, B. Vollmar, 2019, Bioconjugate chemistry.

A mild and selective method for the hydrolysis of esters with trimethyltin hydroxide.

K. Nicolaou, M. Zak, Anthony A Estrada, 2005, Angewandte Chemie.

Combinatorial approach to identification of tyrphostin inhibitors of cytokine signaling.

Xiao-yi Xiao, B. Rich, B. Safina, 2005, Bioorganic & medicinal chemistry.

Potent and selective inhibitors of PI3Kδ: obtaining isoform selectivity from the affinity pocket and tryptophan shelf.

Steve Price, A. Nadin, BinQing Wei, 2013, Bioorganic & medicinal chemistry letters.

Development of a Scalable Strategy for the Synthesis of PI3Kδ Inhibitors: Selective and Efficient Functionalization of Purine Derivatives

Jun Li, R. Angelaud, B. Safina, 2013 .

Total synthesis of thiostrepton. Assembly of key building blocks and completion of the synthesis.

K. Nicolaou, M. Zak, Anthony A Estrada, 2005, Journal of the American Chemical Society.

A biomimetically inspired synthesis of the dehydropiperidine domain of thiostrepton.

K. Nicolaou, M. Zak, M. Nevalainen, 2002, Angewandte Chemie.

Total synthesis of thiostrepton. Retrosynthetic analysis and construction of key building blocks.

Sang Hyup Lee, K C Nicolaou, Mark Zak, 2005, Journal of the American Chemical Society.

Total synthesis of thiostrepton, part 2: construction of the quinaldic acid macrocycle and final stages of the synthesis.

K. Nicolaou, M. Zak, Anthony A. Estrada, 2004, Angewandte Chemie.

Total synthesis of thiostrepton, part 1: construction of the dehydropiperidine/thiazoline-containing macrocycle.

K. Nicolaou, M. Zak, Anthony A. Estrada, 2004, Angewandte Chemie.

Synthetic studies on thiostrepton: construction of thiostrepton analogues with the thiazoline-containing macrocycle.

K. Nicolaou, M. Zak, M. Bella, 2003, Angewandte Chemie.

A pentacyclic aurora kinase inhibitor (AKI-001) with high in vivo potency and oral bioavailability.

Guy Georges, Elizabeth Blackwood, Christian Wiesmann, 2008, Journal of medicinal chemistry.

Total Synthesis of Thiostrepton. Part 1. Construction of the Dehydropiperidine/Thiazoline-Containing Macrocycle.

K. Nicolaou, M. Zak, Anthony A. Estrada, 2004 .

Total synthesis of thiostrepton, part 2: construction of the quinaldic acid macrocycle and final stages of the synthesis.

K. Nicolaou, M. Zak, Anthony A. Estrada, 2004, Angewandte Chemie.

Stereocontrolled synthesis of the quinaldic acid macrocyclic system of thiostrepton.

K. Nicolaou, F. Zécri, M. Zak, 2002, Angewandte Chemie.

A New Photolabile Linker for the Photoactivation of Carboxyl Groups

K. Nicolaou, N. Winssinger, Brian S. Safina, 2001 .

Discovery of novel PI3-kinase δ specific inhibitors for the treatment of rheumatoid arthritis: taming CYP3A4 time-dependent inhibition.

P. Savy, Steve Price, A. Nadin, 2012, Journal of medicinal chemistry.

Selective NaV1.7 Antagonists with Long Residence Time Show Improved Efficacy against Inflammatory and Neuropathic Pain.

D. Sutherlin, D. Hackos, S. Decker, 2018, Cell reports.

Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3- a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain.

D. Sutherlin, D. Hackos, A. D. White, 2018, Journal of medicinal chemistry.

Structural basis of Nav1.7 inhibition by an isoform-selective small-molecule antagonist

Jun Li, Christine Tam, Daniel F. Ortwine, 2015, Science.

Structure- and Ligand-Based Discovery of Chromane Arylsulfonamide Nav1.7 Inhibitors for the Treatment of Chronic Pain.

D. Sutherlin, Jun Chen, D. Hackos, 2019, Journal of medicinal chemistry.

Identification of Selective Acyl Sulfonamide-Cycloalkylether Inhibitors of the Voltage-Gated Sodium Channel (NaV) 1.7 with Potent Analgesic Activity.

Benjamin D. Sellers, D. Sutherlin, D. Hackos, 2018, Journal of medicinal chemistry.

Discovery of Peptidomimetic Antibody-Drug Conjugate Linkers with Enhanced Protease Specificity.

S. Steinbacher, BinQing Wei, C. Eigenbrot, 2017, Journal of medicinal chemistry.

A Non-covalent Ligand Reveals Biased Agonism of the TRPA1 Ion Channel

M. Volgraf, Tianbo Li, A. Rohou, 2020, Neuron.

Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.

M. Volgraf, A. Rohou, Jun Chen, 2021, Journal of medicinal chemistry.

Discovery of Aryl Sulfonamides as Isoform-Selective Inhibitors of NaV1.7 with Efficacy in Rodent Pain Models.

Shifeng Liu, R. Oballa, D. Sutherlin, 2016, ACS medicinal chemistry letters.

Discovery of Acyl-sulfonamide Nav1.7 Inhibitors GDC-0276 and GDC-0310.

D. Sutherlin, Jun Chen, D. Hackos, 2021, Journal of medicinal chemistry.

A TRPA1 inhibitor suppresses neurogenic inflammation and airway contraction for asthma treatment

Simon S. Gao, J. Elstrott, M. Volgraf, 2021, The Journal of experimental medicine.

Design of Selective Benzoxazepin PI3Kδ Inhibitors Through Control of Dihedral Angles.

A. K. Forrest, BinQing Wei, M. Ultsch, 2017, ACS medicinal chemistry letters.

Identification of GNE-293, a potent and selective PI3Kδ inhibitor: navigating in vitro genotoxicity while improving potency and selectivity.

Steve Price, BinQing Wei, D. Sutherlin, 2013, Bioorganic & medicinal chemistry letters.

Discovery of a Potent (4 R,5 S)-4-Fluoro-5-methylproline Sulfonamide Transient Receptor Potential Ankyrin 1 Antagonist and Its Methylene Phosphate Prodrug Guided by Molecular Modeling.

C. Brotherton-Pleiss, M. Volgraf, Jun Chen, 2018, Journal of medicinal chemistry.

Potent and highly selective benzimidazole inhibitors of PI3-kinase delta.

P. Savy, E. Bradley, M. Ultsch, 2012, Journal of medicinal chemistry.

Correction for Chernov-Rogan et al., TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism

D. Hackos, Wienke Lange, H. Deisemann, 2020, Proceedings of the National Academy of Sciences.

TRPA1 modulation by piperidine carboxamides suggests an evolutionarily conserved binding site and gating mechanism

M. Klein, M. Volgraf, V. Carnevale, 2019, Proceedings of the National Academy of Sciences.

Total synthesis of thiostrepton, part 2: construction of the quinaldic acid macrocycle and final stages of the synthesis.

K. Nicolaou, M. Zak, Anthony A. Estrada, 2004, Angewandte Chemie.

A biomimetically inspired synthesis of the dehydropiperidine domain of thiostrepton.

K. Nicolaou, M. Zak, M. Nevalainen, 2002, Angewandte Chemie.