C. Metcalf

发表

Targeting protein kinases for bone disease: discovery and development of Src inhibitors.

T. Sawyer, D. Dalgarno, M. R. van Schravendijk, 2002, Current pharmaceutical design.

SAR of Carbon‐Linked, 2‐Substituted Purines: Synthesis and Characterization of AP23451 as a novel Bone‐Targeted Inhibitor of Src Tyrosine Kinase With In Vivo Anti‐Resorptive Activity

R. Bohacek, L. Xing, B. Boyce, 2008, Chemical biology & drug design.

Src Inhibitors in Metastatic Bone Disease

L. Xing, T. Yamashita, B. Boyce, 2006, Clinical Cancer Research.

Future Anti‐Catabolic Therapeutic Targets in Bone Disease

L. Xing, B. Boyce, T. Sawyer, 2006, Annals of the New York Academy of Sciences.

Novel antibacterial agents for the treatment of gram positive infections

C. Metcalf, A. Pearson, Jing Li, 2003 .

Vascular endothelial growth factor receptor-1 mediates migration of human colorectal carcinoma cells by activation of Src family kinases

L. Ellis, F. Fan, D. Hicklin, 2006, British Journal of Cancer.

AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes

J. Trevino, T. Sawyer, W. Shakespeare, 2005, Molecular Cancer Therapeutics.

Identification of Src-specific phosphorylation site on focal adhesion kinase: dissection of the role of Src SH2 and catalytic functions and their consequences for tumor cell behavior.

E. Avizienyte, V. Brunton, M. Frame, 2005, Cancer research.

Anti-proliferative activity of the mTOR inhibitor AP23573 in combination with cytotoxic and targeted agents

T. Clackson, V. Rivera, T. Keenan, 2004 .

Structural Basis of Src Tyrosine Kinase Inhibition with a New Class of Potent and Selective Trisubstituted Purine‐based Compounds

Susan Adams, William Shakespeare, Thilo Stehle, 2006, Chemical biology & drug design.

AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.

T. Clackson, B. Druker, A. Corbin, 2009, Cancer cell.

Novel bone-targeted Src tyrosine kinase inhibitor drug discovery.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, Current opinion in drug discovery & development.

Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.

R. Dolle, Qingyi Yang, T. Moy, 2015, ACS medicinal chemistry letters.

SRC homology-2 inhibitors: peptidomimetic and nonpeptide.

C. Eyermann, R. Bohacek, T. Sawyer, 2002, Mini reviews in medicinal chemistry.

Bone-targeted Src kinase inhibitors: novel pyrrolo- and pyrazolopyrimidine analogues.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, Bioorganic & medicinal chemistry letters.

Novel phosphate ester-linked resins: The solid-phase generation of phenyl phosphate-containing compounds for SH2 inhibition

D. Holt, E. Laborde, Jeremy Green, 1998 .

Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.

Wei-Sheng Huang, Jan Romero, Shuangying Liu, 2010, Journal of medicinal chemistry.

Confirmation by total synthesis of the revised structure of sporol : an application of cyclic thionocarbonate-initiated radical cyclization

G. Schulte, C. Metcalf, F. Ziegler, 1992 .

Structure and total synthesis of sporol and neosporol

G. Schulte, A. Nangia, C. Metcalf, 1993 .

Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance.

Piotr Sliz, Mohammad Azam, Tomi K Sawyer, 2006, Proceedings of the National Academy of Sciences of the United States of America.

Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.

T. Clackson, R. Bohacek, B. Druker, 2004, Blood.

Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma.

Liz Y. Han, A. Sood, C. Landen, 2006, Cancer research.

Novel protein kinase inhibitors: SMART drug design technology.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, BioTechniques.

SMART Drug Design: Novel Phosphopeptide and ATP Mimetic-Based Small Molecule Inhibitors of the Oncogenic Protein Kinase pp60 src (Src)

R. Bohacek, T. Sawyer, W. Shakespeare, 2005 .

Orally Active Inhibitors of the Imatinib Resistant Bcr-Abl Mutant T315I.

T. Clackson, B. Druker, A. Corbin, 2006 .

Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.

Wei-Sheng Huang, Jan Romero, Shuangying Liu, 2011, Bioorganic & medicinal chemistry letters.

In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.

B. Druker, M. Heinrich, A. Corbin, 2005, Blood.

Structure-Activity Relationship Studies of a Series of Semisynthetic Lipopeptides Leading to the Discovery of Surotomycin, a Novel Cyclic Lipopeptide Being Developed for the Treatment of Clostridium difficile-Associated Diarrhea.

L. Mortin, M. Mesleh, D. Citron, 2015, Journal of medicinal chemistry.

Structure-based design of an osteoclast-selective, nonpeptide src homology 2 inhibitor with in vivo antiresorptive activity.

M. Hatada, S. Violette, R. Bohacek, 2000, Proceedings of the National Academy of Sciences of the United States of America.

Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.

M. Mesleh, J. Barker, R. Dolle, 2016, ACS medicinal chemistry letters.

Reduced pulmonary surfactant interaction of daptomycin analogs via tryptophan replacement with alternative amino acids.

Carmela T. M. Mascio, J. Silverman, D. Keith, 2012, Bioorganic & medicinal chemistry letters.

From Theory to Practice: EGFR Mutation Testing in Current Practice and Roadblocks to Its Implementation

Jacqueline M. Bentel, Marc A. Thomas, Agata Sadowska, 2013 .

Discovery of a Novel Cabazitaxel Nanoparticle-Drug Conjugate (CRLX522) with Improved Pharmacokinetic Properties and Anticancer Effects using a β-Cyclodextrin-PEG Copolymer-Based Delivery Platform.

S. Eliasof, S. Svenson, S. Tripathi, 2019, Journal of medicinal chemistry.

Bone-targeted 2,6,9-trisubstituted purines: novel inhibitors of Src tyrosine kinase for the treatment of bone diseases.

R. Bohacek, T. Sawyer, W. Shakespeare, 2003, Bioorganic & medicinal chemistry letters.

Structure-based design of AP23573, a phosphorus-containing analog of rapamycin for anti-tumor therapy.

L. Rozamus, T. Clackson, R. Bohacek, 2004 .

X-Ray structure of citrate bound to Src SH2 leads to a high-affinity, bone-targeted Src SH2 inhibitor.

M. Hatada, S. Violette, R. Bohacek, 2001, Journal of medicinal chemistry.

Structure-based design of novel nonpeptide inhibitors of the Src SH2 domain:phosphotyrosine mimetics exploiting multifunctional group replacement chemistry.

C. Eyermann, R. Bohacek, T. Sawyer, 2003, Biopolymers.

Bone-targeted pyrido[2,3-d]pyrimidin-7-ones: potent inhibitors of Src tyrosine kinase as novel antiresorptive agents.

S. Violette, R. Bohacek, T. Sawyer, 2003, Bioorganic & medicinal chemistry letters.

Vascular endothelial growth factor receptor-1 mediates migration of human colorectal carcinoma cells by activation of Src family kinases

F. Fan, D. Hicklin, G. Gallick, 2006, British Journal of Cancer.