PF-07059013: a noncovalent modulator of hemoglobin for treatment of sickle cell disease
A Gopalsamy, AE Aulabaugh, A Barakat… - Journal of Medicinal …, 2020 - ACS Publications
Sickle cell disease (SCD) is a genetic disorder caused by a single point mutation (β6 Glu→
Val) on the β-chain of adult hemoglobin (HbA) that results in sickled hemoglobin (HbS). In …
Val) on the β-chain of adult hemoglobin (HbA) that results in sickled hemoglobin (HbS). In …
[HTML][HTML] GBT440, a potent anti-sickling hemoglobin modifier reduces hemolysis, improves anemia and nearly eliminates sickle cells in peripheral blood of patients with …
J Lehrer-Graiwer, J Howard, CJ Hemmaway… - Blood, 2015 - Elsevier
Background: Sickle cell disease (SCD) is caused by polymerization of Hemoglobin S,
resulting in red blood cell (RBC) sickling, RBC destruction, vaso-occlusive episodes and …
resulting in red blood cell (RBC) sickling, RBC destruction, vaso-occlusive episodes and …
Interactions of an anti-sickling drug with hemoglobin in red blood cells from a patient with sickle cell anemia
MB Strader, H Liang, F Meng, J Harper… - Bioconjugate …, 2019 - ACS Publications
The pathophysiology associated with sickle cell disease (SCD) includes hemolytic anemia,
vaso-occlusive events, and ultimately end organ damage set off by the polymerization of …
vaso-occlusive events, and ultimately end organ damage set off by the polymerization of …
Rational design of pyridyl derivatives of vanillin for the treatment of sickle cell disease
PP Pagare, MS Ghatge, FN Musayev… - Bioorganic & medicinal …, 2018 - Elsevier
Hypoxia-induced polymerization of sickle hemoglobin (Hb S) is the principal phenomenon
that underlays the pathophysiology and morbidity associated with sickle cell disease (SCD) …
that underlays the pathophysiology and morbidity associated with sickle cell disease (SCD) …
Discovery of GBT440, an orally bioavailable R-state stabilizer of sickle cell hemoglobin
B Metcalf, C Chuang, K Dufu, MP Patel… - ACS medicinal …, 2017 - ACS Publications
We report the discovery of a new potent allosteric effector of sickle cell hemoglobin, GBT440
(36), that increases the affinity of hemoglobin for oxygen and consequently inhibits its …
(36), that increases the affinity of hemoglobin for oxygen and consequently inhibits its …
A triazole disulfide compound increases the affinity of hemoglobin for oxygen and reduces the sickling of human sickle cells
A Nakagawa, M Ferrari, G Schleifer… - Molecular …, 2018 - ACS Publications
Sickle cell disease is an inherited disorder of hemoglobin (Hb). During a sickle cell crisis,
deoxygenated sickle hemoglobin (deoxyHbS) polymerizes to form fibers in red blood cells …
deoxygenated sickle hemoglobin (deoxyHbS) polymerizes to form fibers in red blood cells …
Identification of a novel class of covalent modifiers of hemoglobin as potential antisickling agents
Aromatic aldehydes and ethacrynic acid (ECA) exhibit antipolymerization properties that are
beneficial for sickle cell disease therapy. Based on the ECA pharmacophore and its atomic …
beneficial for sickle cell disease therapy. Based on the ECA pharmacophore and its atomic …
Rational drug design of peptide-based therapies for sickle cell disease
OO Olubiyi, MO Olagunju, B Strodel - Molecules, 2019 - mdpi.com
Sickle cell disease (SCD) is a group of inherited disorders affecting red blood cells, which is
caused by a single mutation that results in substitution of the amino acid valine for glutamic …
caused by a single mutation that results in substitution of the amino acid valine for glutamic …
Design, synthesis, and biological evaluation of ester and ether derivatives of antisickling agent 5-HMF for the treatment of sickle cell disease
GG Xu, PP Pagare, MS Ghatge, RP Safo… - Molecular …, 2017 - ACS Publications
Candidate drugs to counter intracellular polymerization of deoxygenated sickle hemoglobin
(Hb S) continue to represent a promising approach to mitigating the primary cause of the …
(Hb S) continue to represent a promising approach to mitigating the primary cause of the …
Pyridyl derivatives of benzaldehyde as potential antisickling agents
IN Nnamani, GS Joshi, R Danso‐Danquah… - Chemistry & …, 2008 - Wiley Online Library
Compounds that bind to sickle hemoglobin (Hb S) producing an allosteric shift to the high‐
affinity Hb S that does not polymerize are being developed to treat sickle cell anemia (SCA) …
affinity Hb S that does not polymerize are being developed to treat sickle cell anemia (SCA) …
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