Birinapant, a smac-mimetic with improved tolerability for the treatment of solid tumors and hematological malignancies

SM Condon, Y Mitsuuchi, Y Deng, MG LaPorte… - 2014 - ACS Publications
Birinapant (1) is a second-generation bivalent antagonist of IAP proteins that is currently
undergoing clinical development for the treatment of cancer. Using a range of assays that …

Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists

KS Kim, L Zhang, D Williams, HL Perez, E Stang… - Bioorganic & Medicinal …, 2014 - Elsevier
Bivalent heterodimeric IAP antagonists that incorporate (R)-tetrahydroisoquinoline in the
P3′ subunit show high affinity for the BIR2 domain and demonstrated potent IAP inhibitory …

Direct, reagentless electrochemical detection of the BIR3 domain of X-linked inhibitor of apoptosis protein using a peptide-based conducting polymer sensor

X Wang, B Piro, S Reisberg, G Anquetin… - Biosensors and …, 2014 - Elsevier
In this work, we report a reagentless electrochemical peptide (AVPFAQKG) sensor to directly
detect the BIR3 domain of X-linked inhibitor of apoptosis protein (XIAP-BIR3). The …

[HTML][HTML] Discovery of Sanggenon G as a natural cell-permeable small-molecular weight inhibitor of X-linked inhibitor of apoptosis protein (XIAP)

MA Seiter, S Salcher, M Rupp, J Hagenbuchner… - FEBS Open bio, 2014 - Elsevier
Defects in the regulation of apoptosis are one main cause of cancer development and may
result from overexpression of anti-apoptotic proteins such as the X-linked inhibitor of …

Inhibitors of IAP

JA Flygare, F Cohen, K Deshayes, MFT Koehler… - US Patent …, 2014 - Google Patents
The invention provides novel inhibitors of IAP that are useful as therapeutic agents for
treating malignancies where the compounds having the general formula U1-M-U2 wherein …

Antagonists of IAP proteins: novel anti-tumor agents

Y Wan, T Liu, X Hou, Y Dun, P Guan… - Current Medicinal …, 2014 - ingentaconnect.com
Evasion of apoptosis is an important reason for tumor cells to resist the anticancer drugs in
cancer therapy. As a critical regulator, the inhibitor of apoptosis proteins (IAPs) can block the …

[图书][B] Indolizidine and quinolizidine motifs for the synthesis of conformationally constrained smac mimetics and chloroquine conjugates

Y Lu - 2014 - ddd.uab.cat
L'esquelet d'indolizidina o quinolizidina és present a molts productes naturals i sintètics,
alguns del quals presenten activitats biològiques diverses. Aquesta tesi es centra en la …