K. Wilcoxen

发表

Distinctive Roles of Furin and TMPRSS2 in SARS-CoV-2 Infectivity

N. Seidah, B. Coutard, Ursula Andréo, 2022, Journal of virology.

The spîke (S)-protein of SARS-CoV-2 binds ACE2 and requires proteolytic “priming” at PRRAR685↓

N. Seidah, B. Coutard, Ursula Andréo, 2021 .

Implications of Spike-glycoprotein processing at S1/S2 by Furin, at S2’ by Furin and/or TMPRSS2 and shedding of ACE2: cell-to-cell fusion, cell entry and infectivity of SARS-CoV-2

N. Seidah, B. Coutard, Ursula Andréo, 2020, bioRxiv.

Implications of Spike-glycoprotein processing at S1/S2 by Furin, at S2’ by Furin and/or TMPRSS2 and shedding of ACE2: cell-to-cell fusion, cell entry and infectivity of SARS-CoV-2

N. Seidah, B. Coutard, Ursula Andréo, 2020, bioRxiv.

Antiviral cyclic d,l-α-peptides: Targeting a general biochemical pathway in virus infections

Glen R. Nemerow, G. Nemerow, M. Ghadiri, 2005 .

Antibacterial agents based on the cyclic d,l-α-peptide architecture

Juan R. Granja, M. Ghadiri, J. Granja, 2001, Nature.

Practical metabolomics in drug discovery

Yoshiya Oda, Yoshiaki Sato, Y. Oda, 2010, Expert opinion on drug discovery.

Antiviral cyclic D,L-alpha-peptides: targeting a general biochemical pathway in virus infections.

G. Nemerow, M. Ghadiri, C. Wiethoff, 2005, Bioorganic & medicinal chemistry.

TARGET IDENTIFICATION Acceleration of Target Identification and Validation by Human Tumor Genomics

R. Martell, K. Wilcoxen, D. Brooks, 2013 .

Recent advances of MEK inhibitors and their clinical progress.

K. Wilcoxen, K. Nomoto, Sara Wu, 2007, Current topics in medicinal chemistry.

A highly selective, cell-permeable furin inhibitor BOS-318 rescues key features of cystic fibrosis airway disease.

K. Wilcoxen, N. Campobasso, J. Axten, 2022, Cell chemical biology.

Intersectional innovation in biomarker development for patient-centric medicine.

J. Hoppin, K. Wilcoxen, J. Hesterman, 2011, Personalized medicine.

Long-term treatment with the PARP inhibitor niraparib does not increase the mutation load in cell line models and tumour xenografts

Z. Szallasi, I. Csabai, Yonghong Xiao, 2018, British Journal of Cancer.

Discovery of IACS-9779 and IACS-70465 as Potent Inhibitors Targeting Indoleamine 2,3-Dioxygenase 1 (IDO1) Apoenzyme.

P. Mandal, Jason P. Burke, F. Mseeh, 2021, Journal of medicinal chemistry.

Synthetic lethality in malignant pleural mesothelioma with PARP1 inhibition

R. Hromas, T. George, A. Jaiswal, 2017, Cancer Chemotherapy and Pharmacology.

Design of 2,5-dimethyl-3-(6-dimethyl-4-methylpyridin-3-yl)-7-dipropylaminopyrazolo[1,5-a]pyrimidine (NBI 30775/R121919) and structure--activity relationships of a series of potent and orally active corticotropin-releasing factor receptor antagonists.

Xin-jun Liu, D. Grigoriadis, K. Wilcoxen, 2004, Journal of medicinal chemistry.

Discovery of TSR-022, a novel, potent anti-human TIM-3 therapeutic antibody

P. McNeeley, K. Wilcoxen, H. Laken, 2016 .

Antibacterial agents based on the cyclic D,L-alpha-peptide architecture.

M. Ghadiri, H. Kim, J. Granja, 2001, Nature.

Coupling of 2-Substituted 1-Fluorovinylstannanes with Organic Halides Catalyzed by Palladium(0)/Copper(I) Iodide. A Mild and Stereospecific Method to Monofluoroolefins.

K. Wilcoxen, Chen Chen, Yun-fei Zhu, 1999, The Journal of organic chemistry.

N-aroyloxy-2-thiopyridones as efficient oxygen-radical generators: novel time-controlled DNA photocleaving reagents

K. Wilcoxen, E. Theodorakis, 1996 .

Phase (Ph) 1/2 study of TSR-011, a potent inhibitor of ALK and TRK, including crizotinib-resistant ALK mutations.

G. Weiss, J. Infante, R. Martell, 2014 .

Abstract P5-06-04: The PARP inhibitor niraparib demonstrated activity in patient-derived triple-negative breast cancer xenograft models with high homologous recombination deficiency (HRD) score

S. Cairo, A. Gutin, J. Lanchbury, 2015 .

Optimization of 3-phenylpyrazolo[1,5-a]pyrimidines as potent corticotropin-releasing factor-1 antagonists with adequate lipophilicity and water solubility.

D. Grigoriadis, K. Wilcoxen, Chen Chen, 2004, Bioorganic & medicinal chemistry letters.

New methods for the synthesis of fluoroolefins via the palladium catalyzed cross-coupling reaction of 1-fluorovinyl halides with organoboranes and organostannanes

C. Chen, K. Wilcoxen, J. Mccarthy, 2000 .

Design and synthesis of 3-(2-pyridyl)pyrazolo[1,5-a]pyrimidines as potent CRF1 receptor antagonists.

D. Grigoriadis, K. Wilcoxen, Chen Chen, 2004, Bioorganic & medicinal chemistry letters.

SYNTHESIS OF FLUORINATED OLEFINS VIA THE PALLADIUM CATALYZED CROSS-COUPLING REACTION OF 1-FLUOROVINYL HALIDES WITH ORGANOBORANES

K. Wilcoxen, Chen Chen, J. Mccarthy, 1999 .

Quinoline-carboxylic acids are potent inhibitors that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins.

N. Ling, K. Wilcoxen, Chen Chen, 2003, Bioorganic & medicinal chemistry letters.

Palladium/Copper (I) halide-cocatalyzed stereospecific coupling of 1-fluorovinylstannanes with aryl iodides and acyl chlorides

C. Chen, K. Wilcoxen, J. Mccarthy, 1997 .

A convenient one-pot synthesis of 4-amino-3-arylpyrazoles from α-phthaloylaminoacetophenones

C. Chen, K. Wilcoxen, J. Mccarthy, 1998 .

6,7-dihydroxyisoquinoline-3-carboxylic acids are potent inhibitors on the binding of insulin-like growth factor (IGF) to IGF-binding proteins: optimization of the 1-position benzoyl side chain.

N. Ling, K. Wilcoxen, Chen Chen, 2003, Bioorganic & medicinal chemistry letters.

Biomimetic catalysis of intermodular aminoacyl transfer.

M. Ghadiri, K. Wilcoxen, L. Leman, 2007, Journal of the American Chemical Society.

In vivo anti-tumor activity of the PARP inhibitor niraparib in homologous recombination deficient and proficient ovarian carcinoma.

A. Oberg, E. Swisher, K. Flatten, 2016, Gynecologic oncology.

Discovery of IACS-9439, a potent, exquisitely selective and orally bioavailable inhibitor of CSF1R.

P. Mandal, Jason P. Burke, F. Mseeh, 2020, Journal of medicinal chemistry.

Niraparib: A Poly(ADP-ribose) Polymerase (PARP) Inhibitor for the Treatment of Tumors with Defective Homologous Recombination.

C. Toniatti, M. Rowley, K. Wilcoxen, 2015, Journal of medicinal chemistry.

Synthesis and SAR of 8-arylquinolines as potent corticotropin-releasing factor1 (CRF1) receptor antagonists.

D. Grigoriadis, K. Wilcoxen, T. Webb, 2003, Bioorganic & medicinal chemistry letters.

Discovery of novel drugs for promising targets.

R. Martell, K. Wilcoxen, D. Brooks, 2013, Clinical therapeutics.

Recent advances of MEK inhibitors and their clinical progress.

Kenichi Nomoto, K. Wilcoxen, K. Nomoto, 2007, Current topics in medicinal chemistry.

Identification and characterization of TSR-042, a novel anti-human PD-1 therapeutic antibody

P. McNeeley, K. Wilcoxen, M. Kehry, 2016 .

Erratum for Essalmani et al., “Distinctive Roles of Furin and TMPRSS2 in SARS-CoV-2 Infectivity”

N. Seidah, B. Coutard, Ursula Andréo, 2022, Journal of Virology.

Abstract A258: The PARP inhibitor niraparib demonstrates synergy with chemotherapy in treatment of patient derived Ewing's sarcoma tumorGraft models.

E. Bruckheimer, K. Wilcoxen, T. Khor, 2013 .

Abstract B168: The PARP inhibitor, niraparib, crosses the blood brain barrier in rodents and is efficacious in a BRCA2-mutant intracranial tumor model

K. Wilcoxen, K. Mikule, 2015 .

A phase I study of niraparib in combination with temozolomide (TMZ) in patients with advanced cancer.

R. Kurzrock, E. Galanis, R. Martell, 2014 .

FOUR-ATOM-LINKED CAPPED PORPHYRINS : SYNTHESIS AND CHARACTERIZATION

Martin R. Johnson, J. Ibers, K. Wilcoxen, 1996 .

Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.

John Saunders, Yinghong Gao, N. Ling, 2002, Bioorganic & medicinal chemistry letters.

Automated mass spectrometric sequence determination of cyclic peptide library members.

M Reza Ghadiri, M. Ghadiri, K. Wilcoxen, 2003, Journal of combinatorial chemistry.

Synthesis of 3-phenylpyrazolo[4,3-b]pyridines via a convenient synthesis of 4-amino-3-arylpyrazoles and SAR of corticotropin-releasing factor receptor type-1 antagonists.

D. Grigoriadis, K. Wilcoxen, Chen Chen, 2003, Bioorganic & medicinal chemistry letters.

An improved synthesis of selectively protected L-dopa derivatives from L-tyrosine.

Y. Zhu, K. Wilcoxen, C. Chen, 2000, The Journal of organic chemistry.

Long-term treatment with the PARP inhibitor niraparib does not increase the mutation load in cell line models and tumour xenografts

Z. Szallasi, I. Csabai, Yonghong Xiao, 2018, British Journal of Cancer.

Furin cleaves SARS-CoV-2 spike-glycoprotein at S1/S2 and S2'for viral fusion/entry: indirect role for TMPRSS2

N. Seidah, B. Coutard, Ursula Andréo, 2020 .

Functional and mechanistic analyses of biomimetic aminoacyl transfer reactions in de novo designed coiled coil peptides via rational active site engineering.

M. Ghadiri, K. Wilcoxen, L. Leman, 2007, Journal of the American Chemical Society.

Abstract 1795: Characterization of a novel series of potent, selective inhibitors of wild type and mutant/fusion anaplastic lymphoma kinase

D. Whittington, P. Andrews, K. Wilcoxen, 2012 .

A novel synthesis of 2-arylpyrrolo[1,2-a]pyrimid-7-ones and their structure-activity relationships as potent GnRH receptor antagonists.

Zhiqian Guo, K. Wilcoxen, Chen Chen, 2002, Bioorganic & medicinal chemistry letters.