TY - JOUR
T1 - Targeting BCL-2 in Hematologic Malignancies
AU - Khan, Nadia
AU - Kahl, Brad
N1 - Funding Information:
Dr. Kahl has consulted for Abbvie and Pharamcyclics. Dr. Khan has consulted for Gilead and Abbvie.
Publisher Copyright:
© 2018, Springer International Publishing AG, part of Springer Nature.
PY - 2018/6/1
Y1 - 2018/6/1
N2 - Resistance to apoptosis is one of the hallmarks of cancer and members of the B-cell lymphoma 2 (BCL-2) family of proteins are central regulators of apoptosis. Many cancers become resistant to chemotherapy and apoptosis by up-regulating BCL-2 and other family members, making these proteins attractive targets for cancer therapy. Venetoclax is an orally administered, small-molecule apoptosis stimulant that targets BCL-2 proteins by acting as a BCL-2 homology domain 3 (BH3) mimetic. The drug is approved in the USA and EU as a monotherapy for the for the treatment of certain patients with chronic lymphocytic leukemia (CLL) and is in phase III clinical development for multiple myeloma (MM), and in phase II or I/II clinical trials for acute myeloid leukemia, and several B-cell malignancies, including diffuse large B-cell lymphoma, Waldenstrom's macroglobulinaemia, follicular lymphoma, and mantle-cell lymphoma.
AB - Resistance to apoptosis is one of the hallmarks of cancer and members of the B-cell lymphoma 2 (BCL-2) family of proteins are central regulators of apoptosis. Many cancers become resistant to chemotherapy and apoptosis by up-regulating BCL-2 and other family members, making these proteins attractive targets for cancer therapy. Venetoclax is an orally administered, small-molecule apoptosis stimulant that targets BCL-2 proteins by acting as a BCL-2 homology domain 3 (BH3) mimetic. The drug is approved in the USA and EU as a monotherapy for the for the treatment of certain patients with chronic lymphocytic leukemia (CLL) and is in phase III clinical development for multiple myeloma (MM), and in phase II or I/II clinical trials for acute myeloid leukemia, and several B-cell malignancies, including diffuse large B-cell lymphoma, Waldenstrom's macroglobulinaemia, follicular lymphoma, and mantle-cell lymphoma.
UR - http://www.scopus.com/inward/record.url?scp=85043396380&partnerID=8YFLogxK
U2 - 10.1007/s11523-018-0560-7
DO - 10.1007/s11523-018-0560-7
M3 - Review article
C2 - 29520705
AN - SCOPUS:85043396380
SN - 1776-2596
VL - 13
SP - 257
EP - 267
JO - Targeted Oncology
JF - Targeted Oncology
IS - 3
ER -