T. Johnson

发表

PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.

Shibing Deng, Hui Wang, Shinji Yamazaki, 2015, Cancer cell.

Using the Golden Triangle to optimize clearance and oral absorption.

M. Edwards, T. Johnson, Ted W Johnson, 2009, Bioorganic & medicinal chemistry letters.

Lipophilic efficiency: the most important efficiency metric in medicinal chemistry.

Kevin D Freeman-Cook, T. Johnson, Ted W Johnson, 2013, Future medicinal chemistry.

Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.

D. Knighton, K. Liu, M. Yin, 2010, ACS medicinal chemistry letters.

PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations

M. McTigue, Sergei L Timofeevski, Qiuhua Li, 2015, Proceedings of the National Academy of Sciences.

Analysis of lorlatinib analogs reveals a roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer

T. R. Johnson, M. Mino‐Kenudson, B. Yeap, 2022, Nature Cancer.

Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expos

Wei Liu, Huichun Zhu, Dac Dinh, 2014, Journal of medicinal chemistry.

LTK fusions: A new target emerges in non-small cell lung cancer.

L. Sequist, T. Johnson, Jessica J. Lin, 2022, Cancer cell.

Discovery of (10R)-7-Amino-12-Fluoro-2,10,16-Trimethyl-15-Oxo-10,15,16,17-Tetrahydro-2H-8,4-(Metheno)Pyrazolo[4,3-H][2,5,11]Benzoxadiazacyclotetradecine-3-Carbonitrile (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant

Huichun Zhu, Benjamin J. Burke, John Charles Kath, 2014 .

Conformational Studies and Atropisomerism Kinetics of the ALK Clinical Candidate Lorlatinib (PF-06463922) and Desmethyl Congeners.

N. Sach, M. Collins, P. Richardson, 2016, Angewandte Chemie.

The Axl kinase domain in complex with a macrocyclic inhibitor offers first structural insights into an active TAM receptor kinase

K. Gajiwala, N. Grodsky, Sergei L Timofeevski, 2017, The Journal of Biological Chemistry.

Syntheses and stereochemical revision of pseudopterosin G-J aglycon and helioporin E.

E. Corey, T. Johnson, S. Lazerwith, 2000, Organic letters.

Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.

G. Getz, A. Iafrate, J. Engelman, 2016, The New England journal of medicine.

Enantiospecific synthesis of the proposed structure of the antitubercular marine diterpenoid pseudopteroxazole: revision of stereochemistry.

E. Corey, T. Johnson, 2001, Journal of the American Chemical Society.

First total synthesis of xestobergsterol A and active structural analogues of the xestobergsterols.

M. Jung, T. Johnson, 1999, Organic letters.

Synthesis of 7-Deoxyxestobergsterol A, a Novel Pentacyclic Steroid of the Xestobergsterol Class1

M. Jung, T. Johnson, 1997 .

Azaindole Hydroxamic Acids are HIV‐1 Integrase Inhibitors

T. Johnson, Plewe Michael Bruno, 2011 .

Azaindole hydroxamic acids are potent HIV-1 integrase inhibitors.

A. Kuki, S. Butler, S. V. Rahavendran, 2009, Journal of medicinal chemistry.

Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.

A. Kuki, S. Butler, Buwen Huang, 2010, Bioorganic & medicinal chemistry letters.

The ALK inhibitor PF-06463922 is effective as a single agent in neuroblastoma driven by expression of ALK and MYCN

S. Robinson, R. Palmer, B. Hallberg, 2016, Disease Models & Mechanisms.

Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

N. Sach, Hong Shen, M. McTigue, 2014, Journal of medicinal chemistry.

Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer.

M. Lawrence, A. Iafrate, M. Mino‐Kenudson, 2018, Cancer discovery.

Spectrum of Mechanisms of Resistance to Crizotinib and Lorlatinib in ROS1 Fusion–Positive Lung Cancer

M. Lawrence, S. Digumarthy, A. Drilon, 2021, Clinical Cancer Research.

Discovery and Pharmacokinetic–Pharmacodynamic Evaluation of an Orally Available Novel Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase and c‐Ros Oncogene 1

S. Yamazaki, Justine L. Lam, T. Johnson, 2017 .

Reviving B-Factors: Activating ALK Mutations Increase Protein Dynamics of the Unphosphorylated Kinase.

D. Gehlhaar, M. McTigue, Sergei L Timofeevski, 2018, ACS medicinal chemistry letters.

Lipophilic Efficiency as an Important Metric in Drug Design.

M. Edwards, T. Johnson, Ted W Johnson, 2018, Journal of medicinal chemistry.

UNUSUAL CYCLIZATION PRODUCTS DERIVED FROM PHOTOLYSIS OF BRESLOW'S STEROIDAL BENZOPHENONE ESTERS

M. Jung, T. Johnson, 1999 .

Structural and functional analysis of lorlatinib analogs reveals roadmap for targeting diverse compound resistance mutations in ALK-positive lung cancer

T. R. Johnson, M. Mino‐Kenudson, B. Yeap, 2021, bioRxiv.

Reviving B-Factors: Retrospective Normalized B-Factor Analysis of c-ros Oncogene 1 Receptor Tyrosine Kinase and Anaplastic Lymphoma Kinase L1196M with Crizotinib and Lorlatinib.

D. Gehlhaar, M. McTigue, A. Brooun, 2018, ACS medicinal chemistry letters.

Design and Synthesis of Functionally Active 5-Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1.

N. Sach, M. McTigue, Sergei L Timofeevski, 2023, Journal of medicinal chemistry.

Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation

M. McTigue, Sergei L Timofeevski, R. Kania, 2019, The Journal of Biological Chemistry.

Enantiospecific synthesis of the proposed structure of the antitubercular marine diterpenoid pseudopteroxazole: revision of stereochemistry.

E. Corey, T. Johnson, Ted W. Johnson, 2001, Journal of the American Chemical Society.

Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors.

A. Kuki, S. Butler, Guy A. McClellan, 2011, Journal of medicinal chemistry.

Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.

G. Getz, A. Iafrate, J. Engelman, 2016, The New England journal of medicine.

Sequential ALK Inhibitors Can Select for Lorlatinib-Resistant Compound ALK Mutations in ALK-Positive Lung Cancer.

A. Iafrate, M. Mino‐Kenudson, J. Engelman, 2018, Cancer discovery.

Abstract PR10: Is CNS availability for oncology a no-brainer? Discovery of PF-06463922, a novel small molecule inhibitor of ALK/ROS1 with preclinical brain availability and broad spectrum potency against ALK-resistant mutations.

N. Sach, M. McTigue, H. Zou, 2013 .

Abstract C253: PF-06463922, a novel brain-penetrating small molecule inhibitor of ALK/ROS1 with potent activity against a broad spectrum of ALK resistant mutations in preclinical models in vitro and in vivo.

Sergei L Timofeevski, S. Yamazaki, Qiuhua Li, 2013 .

Effect of water solvation on the lipophilicity of isomeric pyrimidine-carboxamides.

K. Gajiwala, B. Burke, S. Ninkovic, 2015, Bioorganic & medicinal chemistry.

N. Sach, H. Zou, R. Kania, 2014 .