Hemoglobin allostery and pharmacology

A Bellelli, JRH Tame - Molecular Aspects of Medicine, 2022 - Elsevier
The oxygen demands of the human body require the constant circulation of blood carrying
an enormous concentration of hemoglobin (Hb). Oxygen transport depends not only on the …

5‐hydroxymethyl‐2‐furfural modifies intracellular sickle haemoglobin and inhibits sickling of red blood cells†,‡

O Abdulmalik, MK Safo, Q Chen, J Yang… - British journal of …, 2005 - Wiley Online Library
In an attempt to find new types of anti‐sickling agents that specifically bind to intracellular
sickle haemoglobin (HbS) without inhibition by plasma and tissue proteins or other …

Sparing effect of hemoglobin F and hemoglobin A2 on the polymerization of hemoglobin S at physiologic ligand saturations.

WN Poillon, BC Kim, GP Rodgers… - Proceedings of the …, 1993 - National Acad Sciences
Recent interest in therapies for sickle cell anemia based on elevating fetal Hb has made
accurate estimates of the sparing effect of fetal Hb (Hb F) and other non-sickle Hbs on sickle …

6 Rheology of the sickle cell disorders

J Stuart, CS Johnson - Baillière's Clinical Haematology, 1987 - Elsevier
The sickle cell disorders (SCD) comprise homozygous sickle cell anaemia (SS), SS with~ t-
thalassaemia, sickle cell/haemoglobin C disease (SC), sickle cell/fl-thalassaemia, and other …

Tucaresol increases oxygen affinity and reduces haemolysis in subjects with sickle cell anaemia

R Arya, PE Rolan, RW OOTTON… - British journal of …, 1996 - Wiley Online Library
The primary pathophysiological event in sickling is the intracellular polymerization of
deoxygenated haemoglobin S. Tucaresol (589C80; 4 [2‐formyl‐3‐hydroxy‐phenoxymethyl] …

High-throughput assay to screen small molecules for their ability to prevent sickling of red blood cells

A Nakagawa, MK Cooper, M Kost-Alimova… - ACS …, 2022 - ACS Publications
Sickle cell disease (SCD) is an inherited disorder of hemoglobin (Hb); approximately
300,000 babies are born worldwide with SCD each year. In SCD, fibers of polymerized …

Pharmacokinetics and pharmacodynamics of tucaresol, an antisickling agent, in healthy volunteers.

PE Rolan, AJ Mercer, R Wootton… - British journal of clinical …, 1995 - Wiley Online Library
1. Tucaresol is an orally administered antisickling agent which increases the oxygen affinity
of haemoglobin. 2. The pharmacokinetics, effects on moderate graded exercise and …

Effect of BW12C on oxygen affinity of haemoglobin in sickle-cell disease

AJ Keidan, RD White, ER Huehns, IM Franklin, M Joy… - The Lancet, 1986 - Elsevier
Eight subjects with sickle-cell disease in the symptom-free steady-state received a single
one-hour infusion of the new anti-sickling agent BW12C on a total of eleven occasions. A …

Emerging drug targets for sickle cell disease: shedding light on new knowledge and advances at the molecular level

JS Gibson, DC Rees - Expert Opinion on Therapeutic Targets, 2023 - Taylor & Francis
Introduction In sickle cell disease (SCD), a single amino acid substitution at β6 of the
hemoglobin (Hb) chain replaces glutamate with valine, forming HbS instead of the normal …

The pharmacokinetics, tolerability and pharmacodynamics of tucaresol (589C80; 4 [2‐formyl‐3‐hydroxyphenoxymethyl] benzoic acid), a potential anti‐sickling agent …

PE Rolan, JE Parker, SJ Gray… - British journal of …, 1993 - Wiley Online Library
1. Tucaresol (589C80; 4 [2‐formyl‐3‐hydroxyphenoxymethyl] benzoic acid) interacts
stoichiometrically with haemoglobin to increase oxygen affinity. By decreasing the …