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Compounds were synthesized using a facile step convergent sy
2021-02-04
Compounds were synthesized using a facile 8-step convergent synthesis ( and ). Briefly, (Boc)cyclen (compound ) was coupled using TBTU to Fmoc- or Cbz-protected amino alkyl acids (–), followed by deprotection using 20% piperidine in DMF, or H on Pd/C, respectively (–) (). Deprotected linkers were co
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RGFP966 Gliptins have become a part of various therapeutic r
2021-02-04
Gliptins have become a part of various therapeutic regimens to treat type 2 diabetics in recent decades. Gliptins were developed to lower the blood glucose in type 2 diabetes patients and have been shown to be effective [4,5]. More than a dozen gliptins have been developed for the treatment of T2DM,
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The ribosomal synthesis of D proteins is not currently feasi
2021-02-03
The ribosomal synthesis of D-proteins is not currently feasible; the best effort undertaken so far was limited to the translational incorporation of two D-amino acids into the nascent protein chain by means of modified ribosomes (Dedkova et al., 2006). We therefore apply solid-phase peptide synthesi
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As part of a program to explore the key
2021-02-03
As part of a program to explore the key binding interactions between the core of 1 and DGAT-1 a systematic analysis of the aminopyrimidine subunit was initiated. A potential approach to improving passive permeability within this series would be to increase lipophilicity via incorporation of substitu
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NMR was employed for the determination of un ligated
2021-02-03
NMR was employed for the determination of un-ligated domain 1 structure of DDR2 receptor. The collagen-binding site on the same was identified by cross saturation experiment and mutagenesis [40]. Birgit leitinger identified the binding site of collagen with DDR2 receptor, which was three spatially a
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Three DDR binding sites have
2021-02-03
Three DDR2 binding sites have been mapped on the collagen triple helix by us for collagen type 1 and by others using the collagen toolkit for collagen type 2. All of the three reported binding sequences are conserved in the α1 chain of collagen types 1, 2 and 3. The central motif sequence GARGQAGVMG
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It has been shown that DAPK induces
2021-02-03
It has been shown that DAPK induces cell death through an increase in DAPK catalytic activity and subsequent phosphorylation of target proteins (Shang et al., 2005, Yamamoto et al., 2002), but its multidomain structure enables also a close physical interaction with other proteins (Bialik and Kimchi,
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The mutation in Caucasian people
2021-02-03
The Δ32 mutation in Caucasian people of European heritage is quite common but extremely rare in Asian and African countries (Huang et al., 1996). We recently reported the presence of this mutation from India (Husain et al., 1998a) and established the complete inheritance pattern (Husain et al., 1998
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multidrug resistant The importance of G S
2021-02-03
The importance of G1–S phase progression to the formation of malignant tumors has been highlighted by the high incidence of aberrations in the genes involved in this progression in a wide variety of tumors. p27Kip1 is a member of the Cip/Kip family of cyclin-dependent kinase inhibitors (CKI). Its ro
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Other mutations in the SYNE region exons have been implicate
2021-02-03
Other mutations in the SYNE1 3′ region (exons 81–85) have been implicated in an upper motor neuron disease, ARCA1 (Gros-Louis et al., 2007). The disease is characterized by progressive movement, coordination, and balance problems caused by disrupted Purkinje cell function and their impaired signalin
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As mentioned previously dopamine plays a crucial role
2021-02-03
As mentioned previously, dopamine plays a crucial role in reducing prefrontal cortical suppression to the amygdala (Rosenkranz and Grace, 2001) and prefrontal cortex mediated amygdala supression has recently been associated with vagal regulation of HRV (Sakaki et al., 2016). In addition, evidence ha
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It is now known that cholinergic signaling plays a vital
2021-02-03
It is now known that cholinergic signaling plays a vital role in controlling many peripheral functions including skeletal and smooth muscle contraction, autonomic postganglionic neuron activation, parasympathetic end-organ activation (e.g., salivary, lacrimal and bronchial glands), regulation of car
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SS is a high grade malignant soft tissue sarcoma
2021-02-03
SS is a high-grade malignant soft tissue sarcoma accounting for 5%–10% of soft tissue sarcomas. After RMS, SS is the most common sarcoma in children, adolescents and young adults [9]. SS originates primarily in the lower (62%) and upper (21%) extremities but may occur at any anatomic site [9], [10].
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Apart from the ET system
2021-02-03
Apart from the ET system's role in regulating blood vessel tone, it is also involved in a variety of cellular processes that are relevant to DR. For example, the ET receptors influence the survival of retinal ganglion (±)-CPSI 1306 (McGrady et al., 2017; Tonari et al., 2012), development of the reti
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Upon Edn ligand binding endothelin receptors can
2021-02-03
Upon Edn ligand binding, endothelin receptors can induce a variety of intracellular signaling cascades leading to diverse cellular responses such as contraction in the case of smooth muscle cells, or cell growth and mitogenesis. Ednrs are expressed in a variety of cell types and tissues, for example
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