Archives
- 2018-07
- 2018-10
- 2018-11
- 2019-04
- 2019-05
- 2019-06
- 2019-07
- 2019-08
- 2019-09
- 2019-10
- 2019-11
- 2019-12
- 2020-01
- 2020-02
- 2020-03
- 2020-04
- 2020-05
- 2020-06
- 2020-07
- 2020-08
- 2020-09
- 2020-10
- 2020-11
- 2020-12
- 2021-01
- 2021-02
- 2021-03
- 2021-04
- 2021-05
- 2021-06
- 2021-07
- 2021-08
- 2021-09
- 2021-10
- 2021-11
- 2021-12
- 2022-01
- 2022-02
- 2022-03
- 2022-04
- 2022-05
- 2022-06
- 2022-07
- 2022-08
- 2022-09
- 2022-10
- 2022-11
- 2022-12
- 2023-01
- 2023-02
- 2023-03
- 2023-04
- 2023-05
- 2023-06
- 2023-07
- 2023-08
- 2023-09
- 2023-10
- 2023-11
- 2023-12
- 2024-01
- 2024-02
- 2024-03
- 2024-04
- 2024-05
-
Angiotensin 1/2 (1-9) Classical DHFR inhibitors such as meth
2021-09-01
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Angiotensin 1/2 (1-9) residues as well as
-
The aniline R group was extensively explored
2021-09-01
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
-
br Acknowledgements br Membrane bound proton translocating i
2021-09-01
Acknowledgements Membrane-bound proton-translocating inorganic pyrophosphatases (H-PPase; EC 3.6.1.1) belong to a recently identified category of proton pumps, distinct from F-, P-, and V-ATPases, which utilize pyrophosphate hydrolysis as the driving force for H movement across biological membr
-
br Prostaglandin D PGD is
2021-09-01
Prostaglandin D (PGD) is derived from the metabolism of arachidonic lp-pla2 by cyclooxygenases and downstream PGD synthases. In the immune system, PGD is mainly produced by mast cells but also although at lower levels, by macrophages and Th2 lymphocytes. PGD binds to three different receptors, th
-
It is interesting that of
2021-09-01
It is interesting that of the control groups, female TG controls only had significantly higher MB-COMT protein than non-TG male controls (Supplemental Table 9, P = 0.005), while these two groups have almost equal expression of S-COMT protein (8.54- vs. 8.34-fold) and their COMT enzyme activity is al
-
The synthetic routes to the substrates based on the
2021-09-01
The synthetic routes to the substrates based on the 2,3-dihydroxynaphthalene and 6,7-dibromo-2,3-dihydroxynaphthalene cores are depicted in Scheme 3. A Michael-type glycosylation of 2,3-dihydroxynaphthalene 16a gave the acetylated sugar 17a which was deprotected giving the required β-glucosidase sub
-
br Materials and methods br Results and
2021-09-01
Materials and methods Results and discussion Summary Acknowledgments We thank Muhammad Anwar for animal rearing and surgery. We also thank Michael M. Myers for editing. Finally, we thank David Hirschberg for his technical advice. Funding for this project was provided by the Einhorn Famil
-
Pyruvate dehydrogenase multienzyme complex PDHc catalyzes th
2021-09-01
Pyruvate dehydrogenase multienzyme complex (PDHc) catalyzes the oxidative decarboxylation of pyruvate, and subsequently acetylates coenzyme A (CoA) to acetyl-CoA during the tricarboxylic aphidicolin metabolic pathway using thiamine diphosphate (ThDP) and Mg2+ as cofactors. PDHc poses a key role in
-
Acknowledgments We acknowledge the Danish Council
2021-09-01
Acknowledgments We acknowledge the Danish Council for Independent Research (Grant no. 11-105250) and the Carlsberg Foundation (Grant no. 2011-01-0567) for funding this work. Introduction DNA is vital as a biological target to design diagnostic agents as well as therapeutic drugs. The recognitio
-
br DGAT protein interactions Although DGAT and DGAT are memb
2021-08-31
DGAT-protein interactions Although DGAT1 and DGAT2 are membrane proteins of the ER, the ER contains within its extensive three-dimensional network different, unique structural and functional protein domains that arise from the non-uniformity imposed on it by the intracellular structures it intera
-
br Introduction The stroma associated with breast cancer met
2021-08-31
Introduction The stroma associated with breast cancer metastasis consists of extracellular matrix (ECM) proteins, including fibrillar collagens, and a cellular component comprised of mesenchymal stem/multipotent stromal Manidipine 2HCl (MSCs), vessels, and cells of the immune system (Pein and Os
-
Most data regarding fish CXCR functions have accumulated fro
2021-08-31
Most data regarding fish CXCR4 functions have accumulated from work in zebrafish where a range of genetic tools and imaging technologies have been developed. As mentioned above, in teleost fish the two CXCR4s (CXCR4a and 4b) are assumed to interact with two ligands (CXCL12a and 12b) and this differe
-
Acknowledgments br Introduction Various researches have been
2021-08-31
Acknowledgments Introduction Various researches have been made in the field of the treatment of cancer and inflammatory diseases. Different mechanisms are involved in the progression of cellular damage that gives an idea about new drug targets. There are always some efforts to improve efficacy,
-
A phenylacetic acid derivative discovered
2021-08-31
A phenylacetic knowledge derivative (), discovered in a high throughput screen for CRTH2, inhibited the binding of H-PGD to CRTH2 receptors on 293 cells with an IC of 0.010μM, and inhibited the binding of H-PGD to DP receptors with an IC of only 8.3μM (). Compound also inhibited CRTH2 mediated cell
-
With a favorable spectrum of CRTh dependent in
2021-08-31
With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i
14126 records 457/942 page Previous Next First page 上5页 456457458459460 下5页 Last page