Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations.

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations. Research Abstract Details 

Research Abstract Table of Contents

Jump to the:

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations. Abstract Text:

David M Burns,Chunhong He,Yanlong Li,Peggy Scherle,Xiangdong Liu,Cindy A Marando,Mayanne B Covington,Gengjie Yang,Max Pan,Sharon Turner,Jordan S Fridman,Gregory Hollis,Kris Vaddi,Swamy Yeleswaram,Robert Newton,Steve Friedman,Brian Metcalf,Wenqing Yao,David M Burns,Chunhong He,Yanlong Li,Peggy Scherle,Xiangdong Liu,Cindy A Marando,Mayanne B Covington,Gengjie Yang,Max Pan,Sharon Turner,Jordan S Fridman,Gregory Hollis,Kris Vaddi,Swamy Yeleswaram,Robert Newton,Steve Friedman,Brian Metcalf,Wenqing Yao,

A series of beta-sulfonamide piperidine hydroxamates were prepared and shown to be potent inhibitors of the human epidermal growth factor receptor-2 (HER-2) sheddase with excellent selectivity against MMP-1, -2, -3, and -9. This was achieved by exploiting subtle differences within the otherwise highly conserved S(1)(') binding pocket of the active sites within the metalloprotease family. In addition, it was discovered that the introduction of polarity to the P(1) and P(1)(') groups reduced the projected human clearance.

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations. Publishing Authors By Initials

DM Burns,C He,Y Li,P Scherle,X Liu,CA Marando,MB Covington,G Yang,M Pan,S Turner,JS Fridman,G Hollis,K Vaddi,S Yeleswaram,R Newton,S Friedman,B Metcalf,W Yao,DM Burns,C He,Y Li,P Scherle,X Liu,CA Marando,MB Covington,G Yang,M Pan,S Turner,JS Fridman,G Hollis,K Vaddi,S Yeleswaram,R Newton,S Friedman,B Metcalf,W Yao,

For similar abstracts research abstracts see: abstracts research

PUBMED ID PMID:

MEDLINE DATE:

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 18

Page Numbers: 560-4

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 1464-3405

DAY: 28

MONTH: 11

YEAR: 2007

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations. Information

Number of References:

LANGUAGE: eng

NlmUniqueID: 9107377

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations. Keywords Mesh Terms:

KEYWORDS:

MESH TERMS:

Chemical & Substance for Abstract: Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations. Information

Substance Name:

Registry Number:

Grant and Affiliation Information for Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P(1)(') permutations.

AFFILIATION: Department of Medicinal Chemistry, Incyte Corporation, Wilmington, DE 19880, USA.

Country: England

AGENCY:

GRANT:

ACRONYM:

MEDLINETA: Bioorg Med Chem Lett

REFSOURCE:

DATABASENAME:

ACCESSION NUMBER:

Number Hits: 0

Conversion of an MMP-potent scaffold to an MMP-selective HER-2 sheddase inhibitor via scaffold hybridization and subtle P1' permutations Related Publications

• Regulation of secretion of osteoprotegerin in rat dental follicle cells.
• [A case of hemorrhagic fever with renal syndrome]
• [A dual-color fluorescence in situ hybridization study on the detection of inv(16) in acute myeloid leukemia]
• [Applying exponent method of density to amend bone's edge of X-ray image]
• [Clinical study of plasma substitute (Gelofusion) on fluid resuscitation in patients with burned shock]
• [Determination of aluminium in healthman hair by FAAS and FAES]
• [Determination of trace elements in shenrong heixi wan]
• [Development and application of an indirect immunofluorescence assay for the detection of serum immunoglobulin G to human herpesvirus 6]
• [Effectiveness of caring on chronic cases of filariasis in Zhejiang Province]
• [Effects of anticoagulation therapy with low molecular weight heparin in acute pancreatitis.]
• [Effects of esmolol and fentanyl on the hemodynamic and catecholamine response to tracheal intubation in hypertensive patients]
• [Experimental research on tyrosine-kinase inhibitor STI571 and P21WAF gene clone to treat chronic myeloid leukemia]
• [Experimental study on viscoelasticity of spinal lumbar vertebrae (T12-S1) by simulating the operation of excising intervertebral disc and planting bone on back route and the operation of excising intervertebral disc and inserting fusion cage]
• [Induction of apoptosis of HepG2 cells by NDRG2]
• [Pathological changes between HBeAg and anti-HBe in patients with chronic hepatitis B]
• [Progress of surface enhanced Raman spectroscopic studies in nonaqueous systems]
• [Propofol reduces intercellular adhesion molecular-1 expression in lung injury following intestinal ischemia/reperfusion in rats.]
• [Report of a survived neonate born to the mother who had liver transplantation]
• [Retrocaval ureter]
• [Specific humoral immuneresponse in Rhesus monkeys vaccinated immune response with Abeta42 peptide vaccine]
• [Stress on clinical research of primary biliary cirrhosis]
• [Study on laser flash spectroscopy of laser-induced interaction of DNA and polynucleotides with SO4*-]
• [Study on the action force of dimerization of cobalt tetrasulfonate Ph-thalocyanine in aqueous solotion]
• [The detection of serum hepatitis B virus Pre-S1 antigen and its relationship with HBeAg/anti-HBe and HBV DNA by polymerase chain reaction]
• [The diagnosis and treatment of acute necrotizing fascitis in 14 patients]
• [The expression of CXCR4 on acute leukemia cells and its implication for extramedullary infiltration]
• [The implementation of sharing treatment planning system based on DICOM]
• [The progress in inhibitors of Janus kinases/signal transducers and activators of transcription pathway]
• [The recent development of genomic polymorphism in sepsis]
• [X-ray microanalysis of the activity of immobilized L-asparaginase]