Discovery of Dinaciclib (SCH 727965): A Potent and Selective
Inhibitor of Cyclin-Dependent Kinases.

J 2010

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

PARUCH, Kamil, Michael DWYER, Carmen ALVAREZ, Courtney BROWN, Tin-Yau CHAN et. al.

Základní údaje

Originální název

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Název česky

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Autoři

PARUCH, Kamil (203 Česká republika, garant, domácí), Michael DWYER (840 Spojené státy), Carmen ALVAREZ (840 Spojené státy), Courtney BROWN (840 Spojené státy), Tin-Yau CHAN (840 Spojené státy), Ronald DOLL (840 Spojené státy), Kerry KEERTIKAR (840 Spojené státy), Chad KNUTSON (840 Spojené státy), Brian MCKITTRICK (840 Spojené státy), Jocelyn RIVERA (840 Spojené státy), Randall ROSSMAN (840 Spojené státy), Greg TUCKER (840 Spojené státy), Thierry FISCHMANN (840 Spojené státy), Alan HRUZA (840 Spojené státy), Vincent MADISON (840 Spojené státy), Amin NOMEIR (840 Spojené státy), Yaolin WANG (840 Spojené státy), Paul KIRSCHMEIER (840 Spojené státy), Emma LEES (840 Spojené státy), David PARRY (840 Spojené státy), Nicole SGAMBELLONE (840 Spojené státy), Wolfgang SEGHEZZI (840 Spojené státy), Lesley SCHULTZ (840 Spojené státy), Frances SHANAHAN (840 Spojené státy), derek WISWELL (840 Spojené státy), Xiaoying XU (840 Spojené státy), Quiao ZHOU (840 Spojené státy), Ray JAMES (840 Spojené státy), Vidyadhar PARADKAR (840 Spojené státy), Haengsoon PARK (840 Spojené státy), Laura ROKOSZ (840 Spojené státy), Tara STAUFFER (840 Spojené státy) a Timothy GUZI (840 Spojené státy)

Vydání

ACS Medicinal Chemistry Letters, USA, American Chemical Society, 2010, 1948-5875

Další údaje

Jazyk

angličtina

Typ výsledku

Článek v odborném periodiku

Obor

10401 Organic chemistry

Stát vydavatele

Spojené státy

Utajení

není předmětem státního či obchodního tajemství

Kód RIV

RIV/00216224:14310/10:00045046

Organizační jednotka

Přírodovědecká fakulta

UT WoS

000280919100004

Klíčová slova anglicky

cdk; kinase; inhibitor; cancer

Příznaky

Mezinárodní význam

Změněno: 21. 4. 2011 10:36, doc. Mgr. Kamil Paruch, Ph.D.

Anotace

V originále

Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncol. therapeutics. Herein is described the utilization of an in vivo screening approach with integrated efficacy and tolerability parameters to identify candidate CDK inhibitors with a suitable balance of activity and tolerability. This approach has resulted in the identification of SCH 727965, a potent and selective CDK inhibitor that is currently undergoing clin. evaluation.

Citovat

PARUCH, Kamil, Michael DWYER, Carmen ALVAREZ, Courtney BROWN, Tin-Yau CHAN, Ronald DOLL, Kerry KEERTIKAR, Chad KNUTSON, Brian MCKITTRICK, Jocelyn RIVERA, Randall ROSSMAN, Greg TUCKER, Thierry FISCHMANN, Alan HRUZA, Vincent MADISON, Amin NOMEIR, Yaolin WANG, Paul KIRSCHMEIER, Emma LEES, David PARRY, Nicole SGAMBELLONE, Wolfgang SEGHEZZI, Lesley SCHULTZ, Frances SHANAHAN, derek WISWELL, Xiaoying XU, Quiao ZHOU, Ray JAMES, Vidyadhar PARADKAR, Haengsoon PARK, Laura ROKOSZ, Tara STAUFFER a Timothy GUZI. Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases. ACS Medicinal Chemistry Letters. USA: American Chemical Society, 2010, roč. 2010, č. 5, s. 204-208. ISSN 1948-5875.

@article{902365,
   author = {Paruch, Kamil and Dwyer, Michael and Alvarez, Carmen and Brown, Courtney and Chan, TinandYau and Doll, Ronald and Keertikar, Kerry and Knutson, Chad and McKittrick, Brian and Rivera, Jocelyn and Rossman, Randall and Tucker, Greg and Fischmann, Thierry and Hruza, Alan and Madison, Vincent and Nomeir, Amin and Wang, Yaolin and Kirschmeier, Paul and Lees, Emma and Parry, David and Sgambellone, Nicole and Seghezzi, Wolfgang and Schultz, Lesley and Shanahan, Frances and Wiswell, derek and Xu, Xiaoying and Zhou, Quiao and James, Ray and Paradkar, Vidyadhar and Park, Haengsoon and Rokosz, Laura and Stauffer, Tara and Guzi, Timothy},
   article_location = {USA},
   article_number = {5},
   keywords = {cdk; kinase; inhibitor; cancer},
   language = {eng},
   issn = {1948-5875},
   journal = {ACS Medicinal Chemistry Letters},
   title = {Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.},
   volume = {2010},
   year = {2010}
}

TY  - JOUR
ID  - 902365
AU  - Paruch, Kamil - Dwyer, Michael - Alvarez, Carmen - Brown, Courtney - Chan, Tin-Yau - Doll, Ronald - Keertikar, Kerry - Knutson, Chad - McKittrick, Brian - Rivera, Jocelyn - Rossman, Randall - Tucker, Greg - Fischmann, Thierry - Hruza, Alan - Madison, Vincent - Nomeir, Amin - Wang, Yaolin - Kirschmeier, Paul - Lees, Emma - Parry, David - Sgambellone, Nicole - Seghezzi, Wolfgang - Schultz, Lesley - Shanahan, Frances - Wiswell, derek - Xu, Xiaoying - Zhou, Quiao - James, Ray - Paradkar, Vidyadhar - Park, Haengsoon - Rokosz, Laura - Stauffer, Tara - Guzi, Timothy
PY  - 2010
TI  - Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.
JF  - ACS Medicinal Chemistry Letters
VL  - 2010
IS  - 5
SP  - 204-208
EP  - 204-208
PB  - American Chemical Society
SN  - 19485875
KW  - cdk
KW  - kinase
KW  - inhibitor
KW  - cancer
N2  - Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncol. therapeutics. Herein is described the utilization of an in vivo screening approach with integrated efficacy and tolerability parameters to identify candidate CDK inhibitors with a suitable balance of activity and tolerability. This approach has resulted in the identification of SCH 727965, a potent and selective CDK inhibitor that is currently undergoing clin. evaluation.
ER  -

PARUCH, Kamil, Michael DWYER, Carmen ALVAREZ, Courtney BROWN, Tin-Yau CHAN, Ronald DOLL, Kerry KEERTIKAR, Chad KNUTSON, Brian MCKITTRICK, Jocelyn RIVERA, Randall ROSSMAN, Greg TUCKER, Thierry FISCHMANN, Alan HRUZA, Vincent MADISON, Amin NOMEIR, Yaolin WANG, Paul KIRSCHMEIER, Emma LEES, David PARRY, Nicole SGAMBELLONE, Wolfgang SEGHEZZI, Lesley SCHULTZ, Frances SHANAHAN, derek WISWELL, Xiaoying XU, Quiao ZHOU, Ray JAMES, Vidyadhar PARADKAR, Haengsoon PARK, Laura ROKOSZ, Tara STAUFFER a Timothy GUZI. Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases. \textit{ACS Medicinal Chemistry Letters}. USA: American Chemical Society, 2010, roč.~2010, č.~5, s.~204-208. ISSN~1948-5875.

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