Blue Ridge Institute for Medical Research

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Comments on the papers

Roskoski, R. Jr. (2016) Ibrutinib inhibition of Bruton protein-tyrosine kinase in the treatment of B cell neoplasms. Pharmacol. Res. 113, 395-408.  This paper describes BTK and the development of ibrutinib, a covalent antagonist, used in the treatment of mantle cell lymphoma, chronic lymphoblastic leukemia, and Waldenstrom macroglobulinemia. 
Roskoski, R. Jr. (2016) Janus kinase (JAK) inhibitors in the treatment of inflammatory and neoplastic diseases. Pharmacol. Res. 111, 784-803. This paper describes the development of first generation inhibitors including the FDA-approved tofacitinib and ruxolitinib. 
Roskoski, R. Jr. (2016) Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs. Pharmacol. Res. 107, 249-275. A review of CDKs and the development of palbociclib. 
Roskoski, R. Jr. (2016) Classification of small molecule protein kinase inhibitors based upon the structures of the drug-enzyme complexes. Pharmacol. Res. 103, 26-48. This paper depicts all of the known drug-enzyme structures of all FDA-approved protein kinase inhibitors at the time of submission (25 October 2015). Two additional protein kinase inhibitors have been approved subsequently, but X-ray structures for them are not in the public domain. See www.brimr.org/PKI/PKIs.htm for updates. 
Roskoski, R. Jr. (2015) A historical overview of protein kinases and their targeted small molecule inhibitors. Pharmacol. Res. 100, 1-23.   Beginning with Fritz Lipmann's discovery of protein phosphoserine at the Rockefeller Institute (1932) and Eugene P. Kennedy's discovery of protein kinase activity at the Ben May Laboratory for Cancer Research at the University of Chicago (1954) to the present. This was the top down-loaded article from July through September 2015 and October through December 2015.
Roskoski, R. Jr. (2015) Src protein-tyrosine kinase structure, mechanism, and small molecule inhibitors. Pharmacol. Res. 94 9-25. This paper was dedicated to the memory of Prof. Donald F. Steiner - advisor, mentor, and discoverer of proinsulin. For a retrospective about him, click here. This was the sixth most downloaded paper in Pharmacological Research from April-June 2015
Roskoski, R. Jr. (2014) ErbB/HER protein-tyrosine kinases: Structure and small molecule inhibitors.  Pharmacol. Res. 87, 42-59. This paper considers the structure and mechanism of the EGFR family in detail. It also contains a review of small molecule ErbB1/2/4 inhibitors approved by the FDA or in clinical trials. This was the 22nd most downloaded paper in Pharmacological Research from Jan-Mar 2015
Roskoski, R. Jr. (2014) The ErbB/HER family of protein-tyrosine kinases and cancer.  Pharmacol. Res. 79, 34-74. This paper was dedicated to the memory of Dr. John W. Haycock, a colleague at LSU Health Sciences Center in New Orleans. This was the second most downloaded paper in Pharmacological Research in April-June 2015.
Roskoski, R. Jr. (2013) The preclinical profile of crizotinib for the treatment of non-small-cell lung cancer and other neoplastic disorders. Expert Opin Drug Discov. 8, 1165-1179. Crizotinib
Anaplastic lymphoma kinase (ALK): Structure, oncogenic activation, and pharmacological inhibition, Pharmacol. Res. 68 (2013) 68-94. This is the 12th article from the Blue Ridge Institute for Medical Research. To see the complete list, click here. This article was the 8th most downloaded Pharmacological Research paper from January-March 2013, the 23rd most download paper from April-June 2013, and the 14th most downloaded paper from Pharmacological Research in 2013
ERK1/2 MAP kinases: Structure, function, and regulation, Pharmacol. Res. 66 (2012) 105-143. This paper was the third most downloaded paper for the year 2012, the most downloaded paper for the year 2013, and the third most downloaded paper for the year 2014. It was the top downloaded paper for April-June 2015 and the second ranked download for July-Sept 2016
MEK1/2 dual-specificity protein kinases: Structure and regulation, Biochem. Biophys. Res. Commun. 417 (2012) 5-10. This paper is dedicated to the memory of Dr. Jack D. Herbert, a founding member of the Board of Directors of the Blue Ridge Institute for Medical Research
RAF protein-serine/threonine kinases: Structure and regulation, Biochem. Biophys. Res. Commun. 399 (2010) 313-317. This is the ninth article from the Blue Ridge Institute for Medical Research. To see the complete list, click here.
VEGF receptor protein-tyrosine kinases: Structure and regulation, Biochem. Biophys. Res. Commun. 375 (2008) 287-291.  Ranked the second most down-loaded paper of Biochemical Biophysical Research Communications from October/2008-March/2009.
Sunitinib: a VEGF and PDGF receptor protein kinase and angiogenesis inhibitor, Biochem. Biophys. Res. Commun, 356 (2007) 323-328. Ranked the third most down-loaded paper of Biochemical Biophysical Research Communications from April-June 2007. 
Vascular endothelial growth factor (VEGF) signaling in tumor progression, Crit. Rev. Hematol, Oncol. 62 (2007) 179-213. First journal article accepted from the Blue Ridge Institute for Medical Research; ranked in the top 25 most down-loaded papers of Critical Reviews of Hematology/Oncology from January 2007- June 2008. 
Biological Oxidation, In: McGraw-Hill Encyclopedia of Science and Technology, 10th edition, 2007, 2, 51-53..  .
Structure and regulation of Kit protein-tyrosine kinase--the stem cell factor receptor, Biochem. Biophys. Res. Commun. 338 (2005) 1307-1315. Ranked in the top 25 most down-loaded papers of Biochemical Biophysical Research Communications from October 2005-September 2006. 
Signaling by Kit protein-tyrosine kinase--the stem cell factor receptor, Biochem Biophys Res Commun. 337 (2005) 1-13. Ranked the 11th most down-loaded paper of Biochemical Biophysical Research Communications from October-December 2005. 
Src kinase regulation by phosphorylation and dephosphorylation, Biochem. Biophys. Res. Commun. 331 (2005) 1-14.

Src protein-tyrosine kinase structure and regulation, Biochem. Biophys Res. Commun.  324 (2004) 1155-1164.

The ErbB/HER receptor protein-tyrosine kinases and cancer, Biochem. Biophys. Res. Commun. 319 (2004) 1-11. This paper was ranked 13th in Biochemical Biophysical Research Communications downloads for the academic year from October 2009-September 2010. To see the complete list, click here.

STI-571: an anticancer protein-tyrosine kinase inhibitor, Biochem. Biophys. Res. Commun. 309 (2003) 709-717. .
Protein prenylation-a pivotal post-translational process, Biochem. Biophys. Res. Commun. 303 (2003) 1-7. .

 

Top 25 downloaded articles from Biochemical Biophysical Research Communications: July-Sept 2004; Oct-Dec 2004; Jan-Mar 2005April-June 2005; July-Sept 2005; Oct-Dec 2005; Jan-Mar 2006; April-June 2006; July-Sept 2006; Oct-Dec 2006; April-June 2007; Oct-Dec 2008; Jan-Mar 2009; July-Sept 2009; Oct-Dec 2009; Jan-March 2010; April-June 2010; July-Sept 2010; Oct-Dec 2010; Oct-Dec 2011; July-Sept 2012
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Top 25 downloaded articles from Pharmacological Research: July-Sept 2012; Oct-Dec 2012; Jan-Dec_2012; Jan-Mar_2013; April-June 2013; July-Sept 2013; Oct-Dec 2013; Jan-Dec_2013; Jan-Mar 2014; April-June 2014; July-Sept_2014; Oct-Dec 2014; Jan-Dec 2014; Jan-Mar 2015; April-June 2015; July-Sept 2015; Oct-Dec 2015. 
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Top 25 downloaded articles from Critical Reviews of Hematology/Oncology: Jan-Mar_2007; April-June 2007; July-Sept 2007 ; Oct-Dec 2007; Jan-Mar 2008; April-June_2008. 
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Today biochemistry is the dominant basic science of medicine in the sense that it outstrips all the others in terms of the number of publications per year. Ulf Lagerkvist
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Updated 09/22/2016