Amide bond bioisosteres: Strategies, synthesis, and successes
The amide functional group plays a key role in the composition of biomolecules, including
many clinically approved drugs. Bioisosterism is widely employed in the rational …
many clinically approved drugs. Bioisosterism is widely employed in the rational …
Aldo-keto reductases and cancer drug resistance
Human aldo-keto reductases (AKRs) catalyze the NADPH-dependent reduction of carbonyl
groups to alcohols for conjugation reactions to proceed. They are implicated in resistance to …
groups to alcohols for conjugation reactions to proceed. They are implicated in resistance to …
Overview of AKR1C3: inhibitor achievements and disease insights
Y Liu, S He, Y Chen, Y Liu, F Feng, W Liu… - Journal of medicinal …, 2020 - ACS Publications
Human aldo-keto reductase family 1 member C3 (AKR1C3) is known as a hormone activity
regulator and prostaglandin F (PGF) synthase that regulates the occupancy of hormone …
regulator and prostaglandin F (PGF) synthase that regulates the occupancy of hormone …
Novel inhibition of AKR1C3 and androgen receptor axis by PTUPB synergizes enzalutamide treatment in advanced prostate cancer
Castration-resistant prostate cancer (CRPC) is the main driving force of mortality in prostate
cancer patients. Among the parameters contributing to the progression of CRPC and …
cancer patients. Among the parameters contributing to the progression of CRPC and …
[HTML][HTML] Bioinformatics analysis of ferroptosis-related gene AKR1C3 as a potential biomarker of asthma and its identification in BEAS-2B cells
Y Wang, J Fan, Y Tong, L Wang, L Wang… - Computers in Biology …, 2023 - Elsevier
Ferroptosis is a newly discovered type of cell death and has recently been shown to be
associated with asthma. However, the relationship between them at the genetic level has not …
associated with asthma. However, the relationship between them at the genetic level has not …
Development of highly potent and specific AKR1C3 inhibitors to restore the chemosensitivity of drug-resistant breast cancer
Y Liu, Y Chen, J Jiang, X Chu, Q Guo, L Zhao… - European journal of …, 2023 - Elsevier
Abstract Aldo-keto reductase 1C3 (AKR1C3) is overexpressed in multiple hormone related
cancers, such as breast and prostate cancer, and is correlated with tumor development and …
cancers, such as breast and prostate cancer, and is correlated with tumor development and …
Development of Biaryl-Containing Aldo-Keto Reductase 1C3 (AKR1C3) Inhibitors for Reversing AKR1C3-Mediated Drug Resistance in Cancer Treatment
S He, X Chu, Y Wu, J Jiang, P Fang… - Journal of Medicinal …, 2023 - ACS Publications
Aldo-keto reductase 1C3 (AKR1C3) is correlated with tumor development and
chemotherapy resistance. The catalytic activity of the enzyme has been recognized as one …
chemotherapy resistance. The catalytic activity of the enzyme has been recognized as one …
Aldo-Keto reductase 1C3 inhibitor prodrug improves pharmacokinetic profile and demonstrates in vivo efficacy in a prostate cancer xenograft model
K Maddeboina, SK Jonnalagadda… - Journal of Medicinal …, 2023 - ACS Publications
Aldo-keto reductase 1C3 (AKR1C3) is overexpressed in castration-resistant prostate cancer
where it acts to drive proliferation and aggressiveness by producing androgens. The …
where it acts to drive proliferation and aggressiveness by producing androgens. The …
Discovery of novel aldo-keto reductase 1C3 inhibitors as chemotherapeutic potentiators for cancer drug resistance
S He, Y Liu, X Chu, Q Li, W Lyu, Y Liu… - ACS medicinal …, 2022 - ACS Publications
As a crucial target which is overexpressed in a variety of cancers, aldo-keto reductase 1C3
(AKR1C3) confers chemotherapeutic resistance to many clinical agents. However, a limited …
(AKR1C3) confers chemotherapeutic resistance to many clinical agents. However, a limited …
[HTML][HTML] Structure-guided optimization of 3-hydroxybenzoisoxazole derivatives as inhibitors of Aldo-keto reductase 1C3 (AKR1C3) to target prostate cancer
AKR1C3 is an enzyme that is overexpressed in several types of radiotherapy-and
chemotherapy-resistant cancers. Despite AKR1C3 is a validated target for drug …
chemotherapy-resistant cancers. Despite AKR1C3 is a validated target for drug …