PMID- 22305612
OWN - NLM
STAT- MEDLINE
DCOM- 20120612
LR  - 20220408
IS  - 1768-3254 (Electronic)
IS  - 0223-5234 (Linking)
VI  - 49
DP  - 2012 Mar
TI  - Recent advances in hypoxia-inducible factor (HIF)-1 inhibitors.
PG  - 24-40
LID - 10.1016/j.ejmech.2012.01.033 [doi]
AB  - Tumor hypoxia has been recognized as a common feature of solid tumors and a 
      negative prognostic factor for response to treatment and survival of cancer 
      patients. The discovery of hypoxia-inducible factor-1 (HIF-1), a molecular 
      determinant of responses to hypoxia in mammalian cells, has renewed enthusiasm 
      for discovery and development of targeted therapies exploiting the hypoxic tumor 
      microenvironment. HIF-1 activity in tumors depends on availability of the HIF-1alpha 
      subunit, the levels of which increase under hypoxic conditions and through 
      activation of oncogenes and/or inactivation of tumor suppressor genes. Increased 
      HIF-1 has been correlated with increased angiogenesis, aggressive tumor growth, 
      and poor patient prognosis, leading to current interest in HIF-1 as promising 
      anticancer drug target. In spite of an ever increasing number of putative small 
      molecule inhibitors of HIF-1, only a few are progressing through preclinical and 
      early clinical development. In this review, we will discuss recent advances in 
      discovery and development of small molecule inhibitors that target the HIF-1 
      pathway as potential anticancer agents.
CI  - Copyright A(c) 2012 Elsevier Masson SAS. All rights reserved.
FAU - Xia, Yan
AU  - Xia Y
AD  - College of Pharmacy, Dongguk University-Seoul, Seoul, Republic of Korea.
FAU - Choi, Hyun-Kyung
AU  - Choi HK
FAU - Lee, Kyeong
AU  - Lee K
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PT  - Review
DEP - 20120124
PL  - France
TA  - Eur J Med Chem
JT  - European journal of medicinal chemistry
JID - 0420510
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Hypoxia-Inducible Factor 1)
RN  - 0 (Small Molecule Libraries)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/*chemistry/*pharmacology/therapeutic use
MH  - Drug Discovery
MH  - Gene Expression Regulation, Neoplastic/drug effects
MH  - Humans
MH  - Hypoxia-Inducible Factor 1/*antagonists & 
      inhibitors/chemistry/genetics/*metabolism
MH  - Models, Molecular
MH  - Neoplasms/*drug therapy/genetics/metabolism/pathology
MH  - Neovascularization, Pathologic/drug therapy
MH  - Small Molecule Libraries/*chemistry/*pharmacology/therapeutic use
EDAT- 2012/02/07 06:00
MHDA- 2012/06/13 06:00
CRDT- 2012/02/07 06:00
PHST- 2011/11/01 00:00 [received]
PHST- 2012/01/13 00:00 [revised]
PHST- 2012/01/16 00:00 [accepted]
PHST- 2012/02/07 06:00 [entrez]
PHST- 2012/02/07 06:00 [pubmed]
PHST- 2012/06/13 06:00 [medline]
AID - S0223-5234(12)00048-7 [pii]
AID - 10.1016/j.ejmech.2012.01.033 [doi]
PST - ppublish
SO  - Eur J Med Chem. 2012 Mar;49:24-40. doi: 10.1016/j.ejmech.2012.01.033. Epub 2012 
      Jan 24.